Patent Publication Number: US-11642361-B2

Title: Nucleoside phosphoramidate prodrugs

Description:
CROSS REFERENCE TO RELATED APPLICATIONS 
     This application is a continuation of U.S. patent application Ser. No. 14/817,318, filed Mar. 12, 2020, now abandoned, which is a continuation of U.S. patent application Ser. No. 16/516,192, filed Jul. 18, 2019, now abandoned, which is a continuation of U.S. patent application Ser. No. 16/169,878, filed Oct. 24, 2018, now abandoned, which is a continuation of U.S. patent application Ser. No. 15/411,506, filed Jan. 20, 2017, now U.S. Pat. No. 10,183,037, which is a continuation of U.S. patent application Ser. No. 14/656,546, filed Mar. 12, 2015, now U.S. Pat. No. 9,585,906, which is a continuation of U.S. patent application Ser. No. 14/013,237, filed Aug. 29, 2013, now U.S. Pat. No. 9,085,573, which is a continuation of U.S. patent application Ser. No. 13/609,614, filed Sep. 11, 2012, now U.S. Pat. No. 8,580,765, which is a continuation of U.S. patent application Ser. No. 13/099,671, filed May 3, 2011, now U.S. Pat. No. 8,334,270, which is a continuation of U.S. patent application Ser. No. 12/053,015, filed Mar. 21, 2008, now U.S. Pat. No. 7,964,580, which claims the benefit under 35 U.S.C. § 119(e) to U.S. Provisional Application Nos. 60/909,315, filed Mar. 30, 2007, and 60/982,309, filed Oct. 24, 2007, all of which are hereby incorporated by reference in their entireties. 
     SEQUENCE LISTING 
     The instant application contains a Sequence Listing which has been submitted electronically in ASCII format and is hereby incorporated by reference in its entirety. 
    
    
     FIELD OF INVENTION 
     The present invention pertains to nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals. The invention provides novel chemical compounds, and the use of these compounds alone or in combination with other antiviral agents for treating HCV infection. 
     BACKGROUND 
     Hepatitis C virus (HCV) infection is a major health problem that leads to chronic liver disease, such as cirrhosis and hepatocellular carcinoma, in a substantial number of infected individuals, estimated to be 2-15% of the world&#39;s population. There are an estimated 4.5 million infected people in the United States alone, according to the U.S. Center for Disease Control. According to the World Health Organization, there are more than 200 million infected individuals worldwide, with at least 3 to 4 million people being infected each year. Once infected, about 20% of people clear the virus, but the rest can harbor HCV the rest of their lives. Ten to twenty percent of chronically infected individuals eventually develop liver-destroying cirrhosis or cancer. The viral disease is transmitted parenterally by contaminated blood and blood products, contaminated needles, or sexually and vertically from infected mothers or carrier mothers to their offspring. Current treatments for HCV infection, which are restricted to immunotherapy with recombinant interferon-α alone or in combination with the nucleoside analog ribavirin, are of limited clinical benefit. Moreover, there is no established vaccine for HCV. Consequently, there is an urgent need for improved therapeutic agents that effectively combat chronic HCV infection. 
     The HCV virion is an enveloped positive-strand RNA virus with a single oligoribonucleotide genomic sequence of about 9600 bases which encodes a polyprotein of about 3,010 amino acids. The protein products of the HCV gene consist of the structural proteins C, E1, and E2, and the non-structural proteins NS2, NS3, NS4A and NS4B, and NS5A and NS5B. The nonstructural (NS) proteins are believed to provide the catalytic machinery for viral replication. The NS3 protease releases NS5B, the RNA-dependent RNA polymerase from the polyprotein chain. HCV NS5B polymerase is required for the synthesis of a double-stranded RNA from a single-stranded viral RNA that serves as a template in the replication cycle of HCV. Therefore, NS5B polymerase is considered to be an essential component in the HCV replication complex (K. Ishi, et al,  Heptology,  1999, 29: 1227-1235; V. Lohmann, et al.,  Virology,  1998, 249: 108-118). Inhibition of HCV NS5B polymerase prevents formation of the double-stranded HCV RNA and therefore constitutes an attractive approach to the development of HCV-specific antiviral therapies. 
     HCV belongs to a much larger family of viruses that share many common features. 
     Flaviviridae Viruses 
     The Flaviviridae family of viruses comprises at least three distinct genera: pestiviruses, which cause disease in cattle and pigs; flavivruses, which are the primary cause of diseases such as dengue fever and yellow fever; and hepaciviruses, whose sole member is HCV. The flavivirus genus includes more than 68 members separated into groups on the basis of serological relatedness (Calisher et al.,  J. Gen. Virol,  1993, 70, 37-43). Clinical symptoms vary and include fever, encephalitis and hemorrhagic fever ( Fields Virology , Editors: Fields, B. N., Knipe, D. M., and Howley, P. M., Lippincott-Raven Publishers, Philadelphia, Pa., 1996, Chapter 31, 931-959). Flaviviruses of global concern that are associated with human disease include the Dengue Hemorrhagic Fever viruses (DHF), yellow fever virus, shock syndrome and Japanese encephalitis virus (Halstead, S. B.,  Rev. Infect. Dis.,  1984, 6, 251-264; Halstead, S. B.,  Science,  239:476-481, 1988; Monath, T. P.,  New Eng. J. Med,  1988, 319, 641-643). 
     The pestivirus genus includes bovine viral diarrhea virus (BVDV), classical swine fever virus (CSFV, also called hog cholera virus) and border disease virus (BDV) of sheep (Moennig, V. et al.  Adv. Vir. Res.  1992, 41, 53-98). Pestivirus infections of domesticated livestock (cattle, pigs and sheep) cause significant economic losses worldwide. BVDV causes mucosal disease in cattle and is of significant economic importance to the livestock industry (Meyers, G. and Thiel, H. J., Advances in Virus Research, 1996, 47, 53-118; Moennig V., et al, Adv. Vir. Res. 1992, 41, 53-98). Human pestiviruses have not been as extensively characterized as the animal pestiviruses. However, serological surveys indicate considerable pestivirus exposure in humans. 
     Pestiviruses and hepaciviruses are closely related virus groups within the Flaviviridae family. Other closely related viruses in this family include the GB virus A, GB virus A-like agents, GB virus-B and GB virus-C (also called hepatitis G virus, HGV). The hepacivirus group (hepatitis C virus; HCV) consists of a number of closely related but genotypically distinguishable viruses that infect humans. There are at least 6 HCV genotypes and more than 50 subtypes. Due to the similarities between pestiviruses and hepaciviruses, combined with the poor ability of hepaciviruses to grow efficiently in cell culture, bovine viral diarrhea virus (BVDV) is often used as a surrogate to study the HCV virus. 
     The genetic organization of pestiviruses and hepaciviruses is very similar. These positive stranded RNA viruses possess a single large open reading frame (ORF) encoding all the viral proteins necessary for virus replication. These proteins are expressed as a polyprotein that is co- and post-translationally processed by both cellular and virus-encoded proteinases to yield the mature viral proteins. The viral proteins responsible for the replication of the viral genome RNA are located within approximately the carboxy-terminal. Two-thirds of the ORF are termed nonstructural (NS) proteins. The genetic organization and polyprotein processing of the nonstructural protein portion of the ORF for pestiviruses and hepaciviruses is very similar. For both the pestiviruses and hepaciviruses, the mature nonstructural (NS) proteins, in sequential order from the amino-terminus of the nonstructural protein coding region to the carboxy-terminus of the ORF, consist of p7, NS2, NS3, NS4A, NS4B, NS5A, and NS5B. 
     The NS proteins of pestiviruses and hepaciviruses share sequence domains that are characteristic of specific protein functions. For example, the NS3 proteins of viruses in both groups possess amino acid sequence motifs characteristic of serine proteinases and of helicases (Gorbalenya et al.,  Nature,  1988, 333, 22; Bazan and Fletterick  Virology,  1989, 171, 637-639; Gorbalenya et al.,  Nucleic Acid Res.,  1989, 17, 3889-3897). Similarly, the NS5B proteins of pestiviruses and hepaciviruses have the motifs characteristic of RNA-directed RNA polymerases (Koonin, E. V. and Dolja, V. V.,  Crir. Rev. Biochem. Molec. Biol.  1993, 28, 375-430). 
     The actual roles and functions of the NS proteins of pestiviruses and hepaciviruses in the lifecycle of the viruses are directly analogous. In both cases, the NS3 serine proteinase is responsible for all proteolytic processing of polyprotein precursors downstream of its position in the ORF (Wiskerchen and Collett,  Virology,  1991, 184, 341-350; Bartenschlager et al.,  J. Virol.  1993, 67, 3835-3844; Eckart et al.  Biochem. Biophys. Res. Comm.  1993, 192, 399-406; Grakoui et al.,  J. Virol.  1993, 67, 2832-2843; Grakoui et al.,  Proc. Natl. Acad Sci. USA  1993, 90, 10583-10587; Hijikata et al.,  J. Virol.  1993, 67, 4665-4675; Tome et al.,  J. Virol.,  1993, 67, 4017-4026). The NS4A protein, in both cases, acts as a cofactor with the NS3 serine protease (Bartenschlager et al.,  J. Virol.  1994, 68, 5045-5055; Failla et al.,  J. Virol.  1994, 68, 3753-3760; Xu et al.,  J. Virol.,  1997, 71:53 12-5322). The NS3 protein of both viruses also functions as a helicase (Kim et al.,  Biochem. Biophys. Res. Comm.,  1995, 215, 160-166; Jin and Peterson,  Arch. Biochem. Biophys.,  1995, 323, 47-53; Warrener and Collett,  J. Virol.  1995, 69, 1720-1726). Finally, the NS5B proteins of pestiviruses and hepaciviruses have the predicted RNA-directed RNA polymerases activity (Behrens et al., EMBO, 1996, 15, 12-22; Lechmann et al.,  J. Virol.,  1997, 71, 8416-8428; Yuan et al.,  Biochem. Biophys. Res. Comm.  1997, 232, 231-235; Hagedorn, PCT WO 97/12033; Zhong et al,  J. Virol.,  1998, 72, 9365-9369). 
     Currently, there are limited treatment options for individuals infected with hepatitis C virus. The current approved therapeutic option is the use of immunotherapy with recombinant interferon-α alone or in combination with the nucleoside analog ribavirin. This therapy is limited in its clinical effectiveness and only 50% of treated patients respond to therapy. Therefore, there is significant need for more effective and novel therapies to address the unmet medical need posed by HCV infection. 
     A number of potential molecular targets for drug development of direct acting antivirals as anti-HCV therapeutics have now been identified including, but not limited to, the NS2-NS3 autoprotease, the N3 protease, the N3 helicase and the NS5B polymerase. The RNA-dependent RNA polymerase is absolutely essential for replication of the single-stranded, positive sense, RNA genome and this enzyme has elicited significant interest among medicinal chemists. 
     Inhibitors of HCV NS5B as potential therapies for HCV infection have been reviewed: Tan, S.-L., et al.,  Nature Rev. Drug Discov.,  2002, 1, 867-881; Walker, M. P. et al.,  Ep. Opin. Investigational Drugs,  2003, 12, 1269-1280; Ni, Z-J., et al.,  Current Opinion in Drug Discovery and Development,  2004, 7, 446-459; Beaulieu, P. L., et al.,  Current Opinion in Investigational Drugs,  2004, 5, 838-850; Wu, J., et al.,  Current Drug Targets - Infectious Disorders,  2003, 3, 207-219; Griffith, R. C., et al,  Annual Reports in Medicinal Chemistry,  2004, 39, 223-237; Carrol, S., et al.,  Infectious Disorders - Drug Targets,  2006, 6, 17-29. The potential for the emergence of resistant HCV strains and the need to identify agents with broad genotype coverage supports the need for continuing efforts to identify novel and more effective nucleosides as HCV NS5B inhibitors. 
     Nucleoside inhibitors of NS5B polymerase can act either as a non-natural substrate that results in chain termination or as a competitive inhibitor which competes with nucleotide binding to the polymerase. To function as a chain terminator the nucleoside analog must be taken up by the cell and converted in vivo to a triphosphate to compete for the polymerase nucleotide binding site. This conversion to the triphosphate is commonly mediated by cellular kinases which imparts additional structural requirements on a potential nucleoside polymerase inhibitor. Unfortunately, this limits the direct evaluation of nucleosides as inhibitors of HCV replication to cell-based assays capable of in situ phosphorylation. 
     In some cases, the biological activity of a nucleoside is hampered by its poor substrate characteristics for one or more of the kinases needed to convert it to the active triphosphate form. Formation of the monophosphate by a nucleoside kinase is generally viewed as the rate limiting step of the three phosphorylation events. To circumvent the need for the initial phosphorylation step in the metabolism of a nucleoside to the active triphosphate analog, the preparation of stable phosphate prodrugs has been reported. Nucleoside phosphoramidate prodrugs have been shown to be precursors of the active nucleoside triphosphate and to inhibit viral replication when administered to viral infected whole cells (McGuigan, C., et al.,  J. Med. Chem.,  1996, 39, 1748-1753; Valette, G., et al.,  J. Med Chem.,  1996, 39, 1981-1990; Balzarini, J., et al.,  Proc. National Acad Sci USA,  1996, 93, 7295-7299; Siddiqui, A. Q., et al.,  J. Med. Chem.,  1999, 42, 4122-4128; Eisenberg, E. J., et al., Nucleosides,  Nucleotides and Nucleic Acids,  2001, 20, 1091-1098; Lee, W. A., et al.,  Antimicrobial Agents and Chemotherapy,  2005, 49, 1898); US 2006/0241064; and WO 2007/095269. 
     Also limiting the utility of nucleosides as viable therapeutic agents is their sometimes poor physicochemical and pharmacokinetic properties. These poor properties can limit the intestinal absorption of an agent and limit uptake into the target tissue or cell. To improve on their properties prodrugs of nucleosides have been employed. It has been demonstrated that preparation of nucleoside phosphoramidates improves the systemic absorption of a nucleoside and furthermore, the phosphoramidate moiety of these “pronucleotides” is masked with neutral lipophilic groups to obtain a suitable partition coefficient to optimize uptake and transport into the cell dramatically enhancing the intracellular concentration of the nucleoside monophosphate analog relative to administering the parent nucleoside alone. Enzyme-mediated hydrolysis of the phosphate ester moiety produces a nucleoside monophosphate wherein the rate limiting initial phosphorylation is unnecessary. 
     SUMMARY OF THE INVENTION 
     The present invention is directed toward novel phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof, represented by the following structure: 
     
       
         
         
             
             
         
       
         
         
           
             wherein 
           
         
       
    
     (a) R 1  is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  alkoxy, F, Cl, Br, I, nitro, cyano, C 1-6  haloalkyl, —N(R 1′ ) 2 , C 2-6  acylamino, —NHSO 2 C 1-6  alkyl, —SO 2 N(R 1′ ) 2 , COR 1″ , and —SO 2 C 1-6  alkyl; (R 1′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 1″  is —OR′ or —N(R 1′ ) 2 ); 
     (b) R 2  is hydrogen, C 1-10  alkyl, R 3a  or R 3b  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms, C(O)CR 3a R 3b NHR 1 , where n is 2 to 4 and R 1 , R 3a , and R 3b ; 
     (c) R 3a  and R 3b  are (i) independently selected from hydrogen, C 1-10  alkyl, cycloalkyl, —(CH 2 ) c (NR 3′ ) 2 , C 1-6  hydroxyalkyl, —CH 2 SH, —(CH 2 ) 2 S(O) d Me, —(CH 2 ) 3 NHC(═NH)NH 2 , (1H-indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, —(CH 2 ) e COR 3″ , aryl and aryl C 1-3  alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, C 1-10  alkyl, C 1-6  alkoxy, halogen, nitro and cyano; (ii) R 3a  and R 3b  both are C 1-6  alkyl; (iii) R 3a  and R 3b  together are (CH 2 ) f  so as to form a spiro ring; (iv) R 3a  is hydrogen and R 3b  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms (v) R 3b  is hydrogen and R 3a  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R 3′  is independently hydrogen or C 1-6  alkyl and R 3″  is —OR′ or —N(R 3′ ) 2 ); (vi) R 3a  is H and R 3b  is H, CH 3 , CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; or (viii) R 3a  is CH 3 , —CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl and R 3b  is H, where R 3′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 3″  is —OR′ or —N(R 3′ ) 2 ); 
     (d) R 4  is hydrogen, C 1-10  alkyl, C 1-10  alkyl optionally substituted with a lower alkyl, alkoxy, di(lower alkyl)-amino, or halogen, C 1-10  haloalkyl, C 3-10  cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; 
     (e) R 5  is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower alkyl, i.e., —(CH 2 ) p OH, where p is 1-6, including hydroxyl methyl (CH 2 OH), CH 2 F, N 3 , CH 2 CN, CH 2 NH 2 , CH 2 NHCH 3 , CH 2 N(CH 3 ) 2 , alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R 6  is H, R 5  cannot be N 3  and when X is OH, R 6  is CH 3  or CH 2 F and B is a purine base, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OMe, halogen, NH 2 , or N 3 ; 
     (h) Y is OH, H, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, vinyl, N 3 , CN, Cl, Br, F, I, NO 2 , OC(O)O(C 1-4  alkyl), OC(O)O(C 1-4  alkyl), OC(O)O(C 2-4  alkynyl), OC(O)O(C 2-4  alkenyl), OC 1-10  haloalkyl, O(aminoacyl), O(C 1-10  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-18  acyl) 2 , wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N 3 , CN, one to three halogen (Cl, Br, F, I), NO 2 , C(O)O(C 1-4  alkyl), C(O)O(C 1-4  alkyl), C(O)O(C 2-4  alkynyl), C(O)O(C 2-4  alkenyl), O(C 1-4  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-4  acyl) 2 ; 
     the base is a naturally occurring or modified purine or pyrimidine base represented by the following structures: 
     
       
         
         
             
             
         
       
         
         
           
             wherein 
           
         
       
    
     Z is N or CR 12 ; 
     R 7 , R 8 , R 9 , R 10 , and R 11  are independently H, F, Cl, Br, I, OH, OR′, SH, SR′, NH 2 , NHR′, NR′ 2 , lower alkyl of C 1 -C 6 , halogenated (F, Cl, Br, I) lower alkyl of C 1 -C 6 , lower alkenyl of C 2 -C 6 , halogenated (F, Cl, Br, I) lower alkenyl of C 2 -C 6 , lower alkynyl of C 2 -C 6  such as C≡CH, halogenated (F, Cl, Br, I) lower alkynyl of C 2 -C 6 , lower alkoxy of C 1 -C 6 , halogenated (F, Cl, Br, I) lower alkoxy of C 1 -C 6 , CO 2 H, CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, 
     wherein R′ is an optionally substituted alkyl, which includes, but is not limited to, an optionally substituted C 1-20  alkyl, an optionally substituted C 1-10  alkyl, an optionally substituted lower alkyl; an optionally substituted cycloalkyl; an optionally substituted alkynyl of C 2 -C 6 , an optionally substituted lower alkenyl of C 2 -C 6 , or optionally substituted acyl, which includes but is not limited to C(O) alkyl, C(O)(C 1-20  alkyl), C(O)(C 1-10  alkyl), or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     R 12  is H, halogen (including F, Cl, Br, I), OH, OR′, SH, SR′, NH 2 , NHR′, NR′ 2 , NO 2  lower alkyl of C 1 -C 6 , halogenated (F, Cl, Br, I) lower alkyl of C 1 -C 6 , lower alkenyl of C 2 -C 6 , halogenated (F, Cl, Br, I) lower alkenyl of C 2 -C 6 , lower alkynyl of C 2 -C 6 , halogenated (F, Cl, Br, I) lower alkynyl of C 2 -C 6 , lower alkoxy of C 1 -C 6 , halogenated (F, Cl, Br, I) lower alkoxy of C 1 -C 6 , CO 2 H, CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′; with the proviso that when base is represented by the structure c with R 11  being hydrogen, R 12  is not a: (i) —C≡C—H, (ii) —C═CH 2 , or (iii) —NO 2 . 
     Definitions 
     The phrase “a” or “an” entity as used herein refers to one or more of that entity; for example, a compound refers to one or more compounds or at least one compound. As such, the terms “a” (or “an”), “one or more”, and “at least one” can be used interchangeably herein. 
     The phrase “as defined herein above” refers to the first definition provided in the Summary of the Invention. 
     The terms “optional” or “optionally” as used herein means that a subsequently described event or circumstance may but need not occur, and that the description includes instances where the event or circumstance occurs and instances in which it does not. For example, “optional bond” means that the bond may or may not be present, and that the description includes single, double, or triple bonds. 
     The term “independently” is used herein to indicate that a variable is applied in any one instance without regard to the presence or absence of a variable having that same or a different definition within the same compound. Thus, in a compound in which R appears twice and is defined as “independently carbon or nitrogen”, both R&#39;s can be carbon, both R&#39;s can be nitrogen, or one R′ can be carbon and the other nitrogen. 
     The term “alkenyl” refers to an unsubstituted hydrocarbon chain radical having from 2 to 10 carbon atoms having one or two olefinic double bonds, preferably one olefinic double bond. The term “C 2-N  alkenyl” refers to an alkenyl comprising 2 to N carbon atoms, where N is an integer having the following values: 3, 4, 5, 6, 7, 8, 9, or 10. The term “C 2-10  alkenyl” refers to an alkenyl comprising 2 to 10 carbon atoms. The term “C 2-4  alkenyl” refers to an alkenyl comprising 2 to 4 carbon atoms. Examples include, but are not limited to, vinyl, 1-propenyl, 2-propenyl (allyl) or 2-butenyl (crotyl). 
     The term “halogenated alkenyl” refers to an alkenyl comprising at least one of F, Cl, Br, and I. 
     The term “alkyl” refers to an unbranched or branched chain, saturated, monovalent hydrocarbon residue containing 1 to 30 carbon atoms. The term “C 1-M  alkyl” refers to an alkyl comprising 1 to M carbon atoms, where M is an integer having the following values: 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, or 30. The term “C 1-4  alkyl” refers to an alkyl containing 1 to 4 carbon atoms. The term “lower alkyl” denotes a straight or branched chain hydrocarbon residue comprising 1 to 6 carbon atoms. “C 1-20  alkyl” as used herein refers to an alkyl comprising 1 to 20 carbon atoms. “C 1-10  alkyl” as used herein refers to an alkyl comprising 1 to 10 carbons. Examples of alkyl groups include, but are not limited to, lower alkyl groups include methyl, ethyl, propyl, i-propyl, n-butyl, i-butyl, t-butyl or pentyl, isopentyl, neopentyl, hexyl, heptyl, and octyl. The term (ar)alkyl or (heteroaryl)alkyl indicate the alkyl group is optionally substituted by an aryl or a heteroaryl group respectively. 
     The term “cycloalkyl” refers to an unsubstituted or substituted carbocycle, in which the carbocycle contains 3 to 10 carbon atoms; preferably 3 to 8 carbon atoms; more preferably 3 to 6 carbon atoms (i.e., lower cycloalkyls). Examples of cycloalkyl groups include, but are not limited to, cyclopropyl, 2-methyl-cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl. 
     The term “cycloalkyl alkyl” refers to an additionally unsubstituted or substituted alkyl substituted by a lower cycloalkyl. Examples of cycloalkyl alkyls include, but are not limited to, any one of methyl, ethyl, propyl, i-propyl, n-butyl, i-butyl, t-butyl or pentyl, isopentyl, neopentyl, hexyl, heptyl, and octyl that is substituted with cyclopropyl, 2-methyl-cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl. 
     The term “cycloheteroalkyl” refers to an unsubstituted or substituted heterocycle, in which the heterocycle contains 2 to 9 carbon atoms; preferably 2 to 7 carbon atoms; more preferably 2 to 5 carbon atoms. Examples of cycloheteroalkyls include, but are not limited to, aziridin-2-yl, N—C 1-3 -alkyl-aziridin-2-yl, azetidinyl, N—C 1-3 -alkyl-azetidin-m′-yl, pyrrolidin-m′-yl, N—C 1-3 -alkyl-pyrrolidin-m′-yl, piperidin-m′-yl, and N—C 1-3 -alkyl-piperidin-m′-yl, where m′ is 2, 3, or 4 depending on the cycloheteroalkyl. Specific examples of N—C 1-3 -alkyl-cycloheteroalkyls include, but are not limited to, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-2-yl, N-methyl-piperidin-3-yl, and N-methyl-piperidin-4-yl. In the instance of R 4 , the point of attachment between the cycloheteroalkyl ring carbon and the oxygen occurs at any one of m′ 
     The term “heterocycle” refers to an unsubstituted or substituted heterocycle containing carbon, hydrogen, and at least one of N, O, and S, where the C and N can be trivalent or tetravalent, i.e., sp 2 - or sp 3 -hybridized. Examples of heterocycles include, but are not limited to, aziridine, azetidine, pyrrolidine, piperidine, imidazole, oxazole, piperazine, etc. In the instance of piperazine, as related to R 10  for NR′ 2 , the corresponding opposite nitrogen atom of the piperazinyl is substituted by a lower alkyl represented by the following structure: 
                         
Preferably, the opposite nitrogen of the piperazinyl is substituted by a methyl group.
 
     The term “halogenated alkyl” (or “haloalkyl”) refers to an unbranched or branched chain alkyl comprising at least one of F, Cl, Br, and I. The term “C 1-M  haloalkyl” refers to an alkyl comprising 1 to M carbon atoms that comprises at least one of F, Cl, Br, and I, where M is an integer having the following values: 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, or 30. “C 1-3  haloalkyl” refers to a haloalkyl comprising 1 to 3 carbons and at least one of F, Cl, Br, and I. The term “halogenated lower alkyl” (or “lower haloalkyl”) refers to a haloalkyl comprising 1 to 6 carbon atoms and at least one of F, Cl, Br, and I. Examples include, but are not limited to, fluoromethyl, chloromethyl, bromomethyl, iodomethyl, difluoromethyl, dichloromethyl, dibromomethyl, diiodomethyl, trifluoromethyl, trichloromethyl, tribromomethyl, triiodomethyl, 1-fluoroethyl, 1-chloroethyl, 1-bromoethyl, 1-iodoethyl, 2-fluoroethyl, 2-chloroethyl, 2-bromoethyl, 2-iodoethyl, 2,2-difluoroethyl, 2,2-dichloroethyl, 2,2-dibromomethyl, 2-2-diiodomethyl, 3-fluoropropyl, 3-chloropropyl, 3-bromopropyl, 2,2,2-trifluoroethyl or 1,1,2,2,2-pentafluoroethyl. 
     The term “alkynyl” refers to an unbranched or branched hydrocarbon chain radical having from 2 to 10 carbon atoms, preferably 2 to 5 carbon atoms, and having one triple bond. The term “C 2-N  alkynyl” refers to an alkynyl comprising 2 to N carbon atoms, where N is an integer having the following values: 3, 4, 5, 6, 7, 8, 9, or 10. The term “C C 2-4  alkynyl” refers to an alkynyl comprising 2 to 4 carbon atoms. The term “C 2-10  alkynyl” refers to an alkynyl comprising 2 to 10 carbons. Examples include, but are limited to, ethynyl, 1-propynyl, 2-propynyl, 1-butynyl, 2-butynyl or 3-butynyl. 
     The term “halogenated alkynyl” refers to an unbranched or branched hydrocarbon chain radical having from 2 to 10 carbon atoms, preferably 2 to 5 carbon atoms, and having one triple bond and at least one of F, Cl, Br, and I. 
     The term “cycloalkyl” refers to a saturated carbocyclic ring comprising 3 to 8 carbon atoms, i.e. cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl. The term “C 3-7  cycloalkyl” as used herein refers to a cycloalkyl comprising 3 to 7 carbons in the carbocyclic ring. 
     The term “alkoxy” refers to an —O-alkyl group or an —O-cycloalkyl group, wherein alkyl and cycloalkyl are as defined above. Examples of —O-alkyl groups include, but are not limited to, methoxy, ethoxy, n-propyloxy, i-propyloxy, n-butyloxy, i-butyloxy, t-butyloxy. “Lower alkoxy” as used herein denotes an alkoxy group with a “lower alkyl” group as previously defined. “C 1-10  alkoxy” refers to an —O-alkyl wherein alkyl is C 1-10 . Examples of —O-cycloalkyl groups include, but are not limited to, —O-c-propyl, —O-c-butyl, —O-c-pentyl, and —O-c-hexyl. 
     The term “halogenated alkoxy” refers to an —O-alkyl group in which the alkyl group comprises at least one of F, Cl, Br, and I. 
     The term “halogenated lower alkoxy” refers to an —O-(lower alkyl) group in which the lower alkyl group comprises at least one of F, Cl, Br, and I. 
     The term “amino acid” includes naturally occurring and synthetic α, β γ or δ amino acids, and includes but is not limited to, amino acids found in proteins, i.e. glycine, alanine, valine, leucine, isoleucine, methionine, phenylalanine, tryptophan, proline, serine, threonine, cysteine, tyrosine, asparagine, glutamine, aspartate, glutamate, lysine, arginine and histidine. In a preferred embodiment, the amino acid is in the L-configuration. Alternatively, the amino acid can be a derivative of alanyl, valinyl, leucinyl, isoleucinyl, prolinyl, phenylalaninyl, tryptophanyl, methioninyl, glycinyl, serinyl, threoninyl, cysteinyl, tyrosinyl, asparaginyl, glutaminyl, aspartoyl, glutaroyl, lysinyl, argininyl, histidinyl, β-alanyl, β-valinyl, β-leucinyl, ρ-isoleucinyl, β-prolinyl, β-phenylalaninyl, β-tryptophanyl, β-methioninyl, β-glycinyl, β-serinyl, β-threoninyl, β-cysteinyl, β-tyrosinyl, β-asparaginyl, β-glutaminyl, β-aspartoyl, β-glutaroyl, β-lysinyl, β-argininyl or β-histidinyl. When the term amino acid is used, it is considered to be a specific and independent disclosure of each of the esters of α, β γ or δ glycine, alanine, valine, leucine, isoleucine, methionine, phenylalanine, tryptophan, proline, serine, threonine, cysteine, tyrosine, asparagine, glutamine, aspartate, glutamate, lysine, arginine and histidine in the D and L-configurations. 
     The term “aminoacyl” includes N,N-unsubstituted, N,N-monosubstituted, and N,N-disubstituted derivatives of naturally occurring and synthetic α, β γ or δ amino acyls, where the amino acyls are derived from amino acids. The amino-nitrogen can be substituted or unsubstituted. When the amino-nitrogen is substituted, the nitrogen is either mono- or di-substituted, where the substituent bound to the amino-nitrogen is a lower alkyl or an alkaryl. In the instance of its use for Y, the expression “O(aminoacyl)” is used. It is understood that the C3′ carbon of the ribose is bound to the oxygen “O”, which is then bound to the carbonyl carbon of the aminoacyl. 
     The terms “alkylamino” or “arylamino” refer to an amino group that has one or two alkyl or aryl substituents, respectively. 
     The term “protected,” as used herein and unless otherwise defined, refers to a group that is added to an oxygen, nitrogen, or phosphorus atom to prevent its further reaction or for other purposes. A wide variety of oxygen and nitrogen protecting groups are known to those skilled in the art of organic synthesis. Non-limiting examples include: C(O)-alkyl, C(O)Ph, C(O)aryl, CH 3 , CH 2 -alkyl, CH 2 -alkenyl, CH 2 Ph, CH 2 -aryl, CH 2 O-alkyl, CH 2 O-aryl, SO 2 -alkyl, SO 2 -aryl, tert-butyldimethylsilyl, tert-butyldiphenylsilyl, and 1,3-(1,1,3,3-tetraisopropyldisiloxanylidene). 
     The term “aryl,” as used herein, and unless otherwise specified, refers to substituted or unsubstituted phenyl (Ph), biphenyl, or naphthyl, preferably the term aryl refers to substituted or unsubstituted phenyl. The aryl group can be substituted with one or more moieties selected from among hydroxyl, F, Cl, Br, I, amino, alkylamino, arylamino, alkoxy, aryloxy, nitro, cyano, sulfonic acid, sulfate, phosphonic acid, phosphate, and phosphonate, either unprotected, or protected as necessary, as known to those skilled in the art, for example, as taught in T. W. Greene and P. G. M. Wuts, “Protective Groups in Organic Synthesis,” 3rd ed., John Wiley &amp; Sons, 1999. 
     The terms “alkaryl” or “alkylaryl” refer to an alkyl group with an aryl substituent, such as benzyl. The terms “aralkyl” or “arylalkyl” refer to an aryl group with an alkyl substituent. 
     The term “di(lower alkyl)amino-lower alkyl” refers to a lower alkyl substituted by an amino group that is itself substituted by two lower alkyl groups. Examples include, but are not limited to, (CH 3 ) 2 NCH 2 , (CH 3 ) 2 NCH 2 CH 2 , (CH 3 ) 2 NCH 2 CH 2 CH 2 , etc. The examples above show lower alkyls substituted at the terminus carbon atom with an N,N-dimethyl-amino substituent. These are intended as examples only and are not intended to limit the meaning of the term “di(lower alkyl)amino-lower alkyl” so as to require the same. It is contemplated that the lower alkyl chain can be substituted with an N,N-di(lower alkyl)-amino at any point along the chain, e.g., CH 3 CH(N-(lower alkyl) 2 )CH 2 CH 2 . 
     The term “halo,” as used herein, includes chloro, bromo, iodo and fluoro. 
     The term “acyl” refers to a substituent containing a carbonyl moiety and a non-carbonyl moiety. The carbonyl moiety contains a double-bond between the carbonyl carbon and a heteroatom, where the heteroatom is selected from among O, N and S. When the heteroatom is N, the N is substituted by a lower alkyl. The non-carbonyl moiety is selected from straight, branched, and cyclic alkyl, which includes, but is not limited to, a straight, branched, or cyclic C 1-20  alkyl, C 1-10  alkyl, or lower alkyl; alkoxyalkyl, including methoxymethyl; aralkyl, including benzyl; aryloxyalkyl, such as phenoxymethyl; or aryl, including phenyl optionally substituted with halogen (F, Cl, Br, I), hydroxyl, C 1  to C 4  alkyl, or C 1  to C 4  alkoxy, sulfonate esters, such as alkyl or aralkyl sulphonyl, including methanesulfonyl, the mono, di or triphosphate ester, trityl or monomethoxytrityl, substituted benzyl, trialkylsilyl (e.g. dimethyl-t-butylsilyl) or diphenylmethylsilyl. When at least one aryl group is present in the non-carbonyl moiety, it is preferred that the aryl group comprises a phenyl group. 
     The term “lower acyl” refers to an acyl group in which the non-carbonyl moiety is lower alkyl. 
     The term “purine” or “pyrimidine” base includes, but is not limited to, adenine, N 6 -alkylpurines, N 6 -acylpurines (wherein acyl is C(O)(alkyl, aryl, alkylaryl, or arylalkyl), N 6 -benzylpurine, N 6 -halopurine, N 6 -vinylpurine, N 6 -acetylenic purine, N 6 -acyl purine, N 6 -hydroxyalkyl purine, N 6 -allcylaminopurine, N 6 -thioallcyl purine, N 2 -alkylpurines, N 2 -alkyl-6-thiopurines, thymine, cytosine, 5-fluorocytosine, 5-methylcytosine, 6-azapyrimidine, including 6-azacytosine, 2- and/or 4-mercaptopyrmidine, uracil, 5-halouracil, including 5-fluorouracil, C 5 -alkylpyrimidines, C 5 -benzylpyrimidines, C 5 -halopyrimidines, C 5 -vinylpyrimidine, C 5 -acetylenic pyrimidine, C 5 -acyl pyrimidine, C 5 -hydroxyalkyl purine, C 5 -amidopyrimidine, C 5 -cyanopyrimidine, C 5 -iodopyrimidine, C 6 -lodo-pyrimidine, C 5 —Br-vinyl pyrimidine, C 6 —Br-vinyl pyrimidine, C 5 -nitropyrimidine, C 5 -amino-pyrimidine, N 2 -alkylpurines, N 2 -alkyl-6-thiopurines, 5-azacytidinyl, 5-azauracilyl, triazolopyridinyl, imidazolopyridinyl, pyrrolopyrimidinyl, and pyrazolopyrimidinyl. Purine bases include, but are not limited to, guanine, adenine, hypoxanthine, 2,6-diaminopurine, and 6-chloropurine. Functional oxygen and nitrogen groups on the base can be protected as necessary or desired. Suitable protecting groups are well known to those skilled in the art, and include trimethylsilyl, dimethylhexylsilyl, t-butyldimethylsilyl, and t-butyldiphenylsilyl, trityl, alkyl groups, and acyl groups such as acetyl and propionyl, methanesulfonyl, and p-toluenesulfonyl. 
     The term “tautomerism” and “tautomers” have their accepted plain meanings. 
     The term “P*” means that the phosphorous atom is chiral and that it has a corresponding Cahn-Ingold-Prelog designation of “R” or “S” which have their accepted plain meanings. It is contemplated that compounds of the formula I are racemic because the chirality at phosphorous. Applicants contemplate use of the racemate and/or the resolved enantiomers. In some instances, an asterisk does not appear next to the phosphoroamidate phosphorous atom. In these instances, it is understood that the phosphorous atom is chiral and that one of ordinary skill understands this to be so unless the substituents bound to the phosphorous exclude the possibility of chirality at phosphorous, such as in P(O)Cl 3 . 
    
    
     DETAILED DESCRIPTION OF THE INVENTION 
     An aspect of the invention is directed to a compound, its salts, hydrates, solvates, crystalline forms, and the like represented by formula I: 
     
       
         
         
             
             
         
       
         
         
           
             wherein 
           
         
       
    
     (a) R 1  is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  alkoxy, F, Cl, Br, I, nitro, cyano, C 1-6  haloalkyl, —N(R 1′ ) 2 , C 1-6  acylamino, —NHSO 2 C 1-6  alkyl, —SO 2 N(R 1′ ) 2 , COR 1″ , and —SO 2 C 1-6  alkyl; (R 1′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 1″  is —OR′ or —N(R 1′ ) 2 ); 
     (b) R 2  is hydrogen, C 1-10  alkyl, R 3a  or R 3b  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms, C(O)CR 3a R 3b NHR 1 , where n is 2 to 4 and R 1 , R 3a , and R 3b ; 
     (c) R 3a  and R 3b  are (i) independently selected from hydrogen, C 1-10  alkyl, cycloalkyl, —(CH 2 ) c (NR 3 ) 2 , C 1-6  hydroxyalkyl, —CH 2 SH, —(CH 2 ) 2 S(O) d Me, —(CH 2 ) 3 NHC(═NH)NH 2 , (1H-indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, —(CH 2 ) e COR 3″ , aryl and aryl C 1-3  alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, C 1-10  alkyl, C 1-6  alkoxy, halogen, nitro and cyano; (ii) R 3a  and R 3b  both are C 1-6  alkyl; (iii) R 3a  and R 3b  together are (CH 2 ) f  so as to form a spiro ring; (iv) R 3a  is hydrogen and R 3b  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms (v) R 3b  is hydrogen and R 3a  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R 3′  is independently hydrogen or C 1-6  alkyl and R 3″  is —OR′ or —N(R 3′ ) 2 ); (vi) R 3a  is H and R 3b  is H, CH 3 , CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CHM) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; or (viii) R 3a  is CH 3 , —CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl and R 3b  is H, where R 3′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 3″  is —OR′ or —N(R 3′ ) 2 ); 
     (d) R 4  is hydrogen, C 1-10  alkyl, C 1-10  alkyl optionally substituted with a lower alkyl, alkoxy, di(lower alkyl)-amino, or halogen, C 1-10  haloalkyl, C 3-10  cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; 
     (e) R 5  is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower alkyl, i.e., —(CH 2 ) p OH, where p is 1-6, including hydroxyl methyl (CH 2 OH), CH 2 F, N 3 , CH 2 CN, CH 2 NH 2 , CH 2 NHCH 3 , CH 2 N(CH 3 ) 2 , alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R 6  is H, R 5  cannot be N 3  and when X is OH, R 6  is CH 3  or CH 2 F and B is a purine base, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OMe, halogen, NH 2 , or N 3 ; 
     (h) Y is OH, H, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, vinyl, N 3 , CN, Cl, Br, F, I, NO 2 , OC(O)O(C 1-4  alkyl), OC(O)O(C 1-4  alkyl), OC(O)O(C 2-4  alkynyl), OC(O)O(C 2-4  alkenyl), OC 1-10  haloalkyl, O(aminoacyl), O(C 1-10  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-18  acyl) 2 , wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N 3 , CN, one to three halogen (Cl, Br, F, I), NO 2 , C(O)O(C 1-4  alkyl), C(O)O(C 1-4  alkyl), C(O)O(C 2-4  alkynyl), C(O)O(C 2-4  alkenyl), O(C 1-4  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-4  acyl) 2 ; 
     the base is a naturally occurring or modified purine or pyrimidine base represented by the following structures: 
     
       
         
         
             
             
         
       
         
         
           
             wherein 
           
         
       
    
     Z is N or CR 12 ; 
     R 7 , R 8 , R 9 , R 10 , and R 11  are independently H, F, Cl, Br, I, OH, OR′, SH, SR′, NH 2 , NHR′, NR′ 2 , lower alkyl of C 1 -C 6 , halogenated (F, Cl, Br, I) lower alkyl of C 1 -C 6 , lower alkenyl of C 2 -C 6 , halogenated (F, Cl, Br, I) lower alkenyl of C 2 -C 6 , lower alkynyl of C 2 -C 6  such as C≡CH, halogenated (F, Cl, Br, I) lower alkynyl of C 2 -C 6 , lower alkoxy of C 1 -C 6 , halogenated (F, Cl, Br, I) lower alkoxy of C 1 -C 6 , CO 2 H, CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, 
     wherein R′ is an optionally substituted alkyl, which includes, but is not limited to, an optionally substituted C 1-20  alkyl, an optionally substituted C 1-10  alkyl, an optionally substituted lower alkyl; an optionally substituted cycloalkyl; an optionally substituted alkynyl of C 2 -C 6 , an optionally substituted lower alkenyl of C 2 -C 6 , or optionally substituted acyl, which includes but is not limited to C(O) alkyl, C(O)(C 1-20  alkyl), C(O)(C 1-10  alkyl), or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     R 12  is H, halogen (including F, Cl, Br, I), OH, OR′, SH, SR′, NH 2 , NHR′, NR′ 2 , NO 2  lower alkyl of C 1 -C 6 , halogenated (F, Cl, Br, I) lower alkyl of C 1 -C 6 , lower alkenyl of C 2 -C 6 , halogenated (F, Cl, Br, I) lower alkenyl of C 2 -C 6 , lower alkynyl of C 2 -C 6 , halogenated (F, Cl, Br, I) lower alkynyl of C 2 -C 6 , lower alkoxy of C 1 -C 6 , halogenated (F, Cl, Br, I) lower alkoxy of C 1 -C 6 , CO 2 H, CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′; with the proviso that when base is represented by the structure c with R 11  being hydrogen, R 12  is not a: (i) —C≡C—H, (ii) —C═CH 2 , or (iii) —NO 2 . 
     As can be appreciated from the structure represented by formula I above, there are myriad ways to express the several embodiments and aspects of each embodiment of the present invention. As seen below, the inventors have disclosed certain embodiments directed to the compound of formula I, each having several aspects, based on the identity of the modified purine or pyrimidine base. This is not intended to be an explicit or implicit admission that the three embodiments are independent or distinct nor should it be interpreted as such. Rather, it is intended to convey information so that the full breadth of the present invention can be understood. Furthermore, the following embodiments, and aspects thereof, are not meant to be limiting on the full breadth of the invention as recited by the structure of formula I. 
     A first embodiment of the invention is directed to a compound represented by formula I-1: 
     
       
         
         
             
             
         
       
     
     wherein 
     (a) R 1  is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  alkoxy, F, Cl, Br, I, nitro, cyano, C 1-6  haloalkyl, —N(R 1′ ) 2 , C 1-6  acylamino, —NHSO 2 C 1-6  alkyl, —SO 2 N(R 1′ ) 2 , COR 1″ , and —SO 2 C 1-6  alkyl; (R 1′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 1″  is —OR′ or —N(R 1′ ) 2 ); 
     (b) R 2  is hydrogen, C 1-10  alkyl, R 3a  or R 3b  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms, C(O)CR 3a R 3b NHR 1 , where n is 2 to 4 and R 1 , R 3a , and R 3b ; 
     (c) R 3a  and R 3b  are (i) independently selected from hydrogen, C 1-10  alkyl, cycloalkyl, —(CH 2 ) c (NR 3 ) 2 , C 1-6  hydroxyalkyl, —CH 2 SH, —(CH 2 ) 2 S(O) d Me, —(CH 2 ) 3 NHC(═NH)NH 2 , (1H-indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, —(CH 2 ) e COR 3″ , aryl and aryl C 1-3  alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, C 1-10  alkyl, C 1-6  alkoxy, halogen, nitro and cyano; (ii) R 3a  and R 3b  both are C 1-6  alkyl; (iii) R 3a  and R 3b  together are (CH 2 ) f  so as to form a spiro ring; (iv) R 3a  is hydrogen and R 3b  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms (v) R 3b  is hydrogen and R 3a  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R 3′  is independently hydrogen or C 1-6  alkyl and R 3″  is —OR′ or —N(R 3′ ) 2 ); (vi) R 3a  is H and R 3b  is H, CH 3 , CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; or (viii) R 3a  is CH 3 , —CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl and R 3b  is H, where R 3′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 3  is —OR′ or —N(R 3′ ) 2 ); 
     (d) R 4  is hydrogen, C 1-10  alkyl, C 1-10  alkyl optionally substituted with a lower alkyl, alkoxy, di(lower alkyl)-amino, or halogen, C 1-10  haloalkyl, C 3-10  cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)-amino, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; 
     (e) R 5  is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower alkyl, i.e., —(CH 2 ) p OH, where p is 1-6, including hydroxyl methyl (CH 2 OH), CH 2 F, N 3 , CH 2 CN, CH 2 NH 2 , CH 2 NHCH 3 , CH 2 N(CH 3 ) 2 , alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R 6  is H, R 5  cannot be N 3  and when X is OH, R 6  is CH 3  or CH 2 F and B is a purine base, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OMe, Cl, Br, I, NH 2 , or N 3 ; 
     (h) Y is OH, H, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, vinyl, N 3 , CN, Cl, Br, F, I, NO 2 , OC(O)O(C 1-4  alkyl), OC(O)O(C 1-4  alkyl), OC(O)O(C 2-4  alkynyl), OC(O)O(C 2-4  alkenyl), OC 1-10  haloalkyl, O(aminoacyl), O(C 1-10  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-18  acyl) 2 , wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N 3 , CN, one to three halogen (Cl, Br, F, I), NO 2 , C(O)O(C 1-4  alkyl), C(O)O(C 1-4  alkyl), C(O)O(C 2-4  alkynyl), C(O)O(C 2-4  alkenyl), O(C 1-4  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-4  acyl) 2 ; 
     (i) R 7 , R 8 , R 9  are independently H, F, Cl, Br, I, OH, OR′, SH, SR′, NH 2 , NHR′, NR′ 2 , lower alkyl, halogenated (F, Cl, Br, I) lower alkyl, lower alkenyl of C 2 -C 6 , CO 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , wherein R′ is a C 1-20  alkyl; a C 1-20  cycloalkyl; a C 2 -C 6  alkenyl, a C 2 -C 6  alkynyl. 
     A first aspect of the first embodiment is directed to a compound represented by formula I-1 
     wherein 
     (a) R 1  is hydrogen, n-alkyl or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of C 1-6  alkyl, C 1-6  alkoxy, F, Cl, Br, I, nitro, cyano, C 1-6  haloalkyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  and R 3b  are independently (i) R 3a  is hydrogen and R 3b  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms (v) R 3b  is hydrogen and R 3a  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 3 to 5, n is 2 to 4, and where R 3′  is independently hydrogen or C 1-6  alkyl and R 3″  is —OR′ or —N(R 3′ ) 2 ); (vi) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; or (viii) R 3  is CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), or CH 2 SH and R 3b  is H; 
     (d) R 4  is hydrogen, C 1-10  alkyl, C 1-10  alkyl optionally substituted with a lower alkyl, alkoxy, di(lower alkyl)-amino, or halogen, C 1-10  haloalkyl, C 3-10  cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; 
     (e) R 5  is H, CN, CH 3 , vinyl, OCH 3 , OCH 2 CH 3 , CH 2 OH, CH 2 (halo), such as CH 2 F, N 3 , CH 2 CN, CH 2 N 3 , CH 2 NH 2 , CH 2 NHCH 3 , CH 2 N(CH 3 ) 2 , halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R 6  is H, R 5  cannot be N 3 ; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OMe, Cl, Br, I, NH 2 , or N 3 ; 
     (h) Y is OH, H, C 1-4  alkyl, vinyl, N 3 , CN, Cl, Br, F, I, O(C 1-6  acyl), O(C 1-4  alkyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-18  acyl) 2 , wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N 3 , CN, one to three halogen (Cl, Br, F, I), NO 2 , OC(O)O(C 1-4  alkyl), OC(O)O(C 1-4  alkyl), OC(O)O(C 2-4  alkynyl), OC(O)O(C 2-4  alkenyl), OC 1-4  haloalkyl, O(aminoacyl), O(C 1-4  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , or N(C 1-4  acyl) 2 ; 
     (i) R 7 , R 8 , R 9  are independently H, F, Cl, Br, I, OH, OR′, SH, SR′, NH 2 , NHR′, NR′ 2 , lower alkyl, halogenated (F, Cl, Br, I) lower alkyl, lower alkenyl of C 2 -C 6 , CO 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , wherein R′ is a C 1-20  alkyl; a C 1-20  cycloalkyl; a C 2 -C 6  alkenyl, a C 2 -C 6  alkynyl. 
     A second aspect of the first embodiment is directed to a compound represented by formula I-1 
     wherein 
     (a) R 1  is hydrogen, n-alkyl or a substituted or unsubstituted phenyl, where the substitutent of the substituted phenyl is at least one of a C 1-3  alkyl, a C 1-3  alkoxy, F, C 1 , Br, I, nitro, cyano, and a C 1-3  haloalkyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  and R 3b  are independently (i) R 3a  is hydrogen and R 3b  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms (v) R 3b  is hydrogen and R 3a  and R 2  together are (CH 2 ) so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 3 to 5, n is 2 to 4, and where R 3′  is independently hydrogen or C 1-6  alkyl and R 3″  is —OR′ or —N(R 3′ ) 2 ); (vi) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; or (viii) R 3a  is CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), or CH 2 SH and R 3b  is H; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, di(lower alkyl)amino-lower alkyl, or aminoacyl; 
     (e) R 5  is H, CN, CH 3 , OCH 3 , CH 2 OH, CH 2 (halo), such as CH 2 F, N 3 , CH 2 CN, CH 2 N 3 , CH 2 NH 2 , CH 2 NHCH 3 , CH 2 N(CH 3 ) 2 , halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R 6  is H, R 5  cannot be N 3 ; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OCH 3 , NH 2 , or N 3 ; 
     (h) Y is OH, H, CH 3 , vinyl, N 3 , CN, Cl, Br, F, I, OC(O)CH 3 , OCH 3 , NH 2 , NHCH 3 , NH(vinyl), NH(acetyl), NH(C(O)CH 3 ), N(CH 3 ) 2 , N(C(O)CH 3 ) 2 , or O(aminoacyl); 
     (i) R 7  and R 8  are independently H, F, Cl, Br, I, OH, OCH 3 , SH, SCH 3 , NH 2 , NHCH 3 , N(CH 3 ) 2 , CH 3 , CH 3-q X q , where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO 2 H, CO 2 CH 3 , CONH 2 , CONHCH 3 , or CON(CH 3 ) 2 ; and 
     (j) R 9  is selected from among OH, OCH 3 , SH, SCH 3 , NH 2 , NHCH 3 , N(CH 3 ) 2 , OC(O)(C1-20 alkyl), which include but are not limited to OC(O)(CH 2 ) s CH 3 , NHC(O)(C1-20 alkyl), which include but are not limited to NHC(O)(CH 2 ) s CH 3 , and N(C(O)(CH 2 ) s CH 3 ) 2 , which include but is not limited to N(C(O)(CH 2 ) s CH 3 ) 2 , where s is an integer selected from 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, and 19. 
     A third aspect of the first embodiment is directed to a compound represented by formula I-1 
     wherein 
     (a) R 1  is hydrogen, n-alkyl or a substituted or unsubstituted phenyl, where the substitutent of the substituted phenyl is at least one of a CH 3 , OCH 3 , F, Cl, Br, I, nitro, cyano, and a CH 3-q X q , where X is F, Cl, Br, or I, and q is 1-3; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl or R 3a  is CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl and R 3b  is H; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, lower haloalkyl, di(lower alkyl)amino-lower alkyl, or aminoacyl; 
     (e) R 5  is H, CN, CH 3 , OCH 3 , CH 2 OH, CH 2 (halo), such as CH 2 F, N 3 , CH 2 CN, CH 2 N 3 , CH 2 NH 2 , CH 2 NHCH 3 , CH 2 N(CH 3 ) 2 , halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R 6  is H, R 5  cannot be N 3 ; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OCH 3 , NH 2 , or N 3 ; 
     (h) Y is OH, H, CH 3 , vinyl, N 3 , CN, Cl, Br, F, I, OC(O)CH 3 , OCH 3 , NH 2 , NHCH 3 , NH(vinyl), NH(acetyl), NH(C(O)CH 3 ), N(CH 3 ) 2 , N(C(O)CH 3 ) 2 , or O(aminoacyl); 
     (i) R 7  and R 8  are independently H, F, Cl, Br, I, OH, OCH 3 , SH, SCH 3 , NH 2 , NHCH 3 , N(CH 3 ) 2 , CH 3 , CH 3-q X q , where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO 2 H, CO 2 CH 3 , CONH 2 , CONHCH 3 , or CON(CH 3 ) 2 , wherein R′ is a C 1-20  alkyl; a C 1-20  cycloalkyl; a C 2 -C 6  alkenyl, a C 2 -C 6  alkynyl′; and 
     (j) R 9  is selected from among OH, OCH 3 , SH, SCH 3 , NH 2 , NHCH 3 , N(CH 3 ) 2 , OC(O)(C1-20 alkyl), which include but are not limited to OC(O)(CH 2 ) s CH 3 , NHC(O)(C1-20 alkyl), which include but are not limited to NHC(O)(CH 2 ) s CH 3 , and N(C(O)(CH 2 ) s CH 3 ) 2 , which include but is not limited to N(C(O)(CH 2 ) s CH 3 ) 2 , where s is an integer selected from 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, and 19. 
     A fourth aspect of the first embodiment is directed to a compound represented by formula I-2 
     
       
         
         
             
             
         
       
     
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, i-propyl, i-propyl, or a substituted or unsubstituted phenyl, where the substitutent of the substituted phenyl is at least one of a CH 3 , OCH 3 , F, Cl, Br, I, nitro, cyano, and a CH 3-q X q , where X is F, Cl, Br, or I, and q is 1-3; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl or R 3a  is CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl and R 3b  is H; 
     (d) R 4  is hydrogen, C 1-10  alkyl, C 1-10  alkyl optionally substituted with a lower alkyl, alkoxy or halogen, C 1-10  haloalkyl, C 3-10  cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; 
     (e) R 5  is H, CN, CH 3 , OCH 3 , CH 2 OH, CH 2 F, N 3 , CH 2 CN, CH 2 N 3 , CH 2 NH 2 , CH 2 NHCH 3 , CH 2 N(CH 3 ) 2 , halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R 6  is H, R 5  cannot be N 3 ; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OCH 3 , Cl, Br, I, NH 2 , or N 3 ; 
     (h) Y is OH, H, CH 3 , vinyl, N 3 , CN, Cl, Br, F, I, OC(O)CH 3 , OCH 3 , NH 2 , NHCH 3 , NH(vinyl), NH(acetyl), NH(C(O)CH 3 ), N(CH 3 ) 2 , N(C(O)CH 3 ) 2 , or O(aminoacyl); 
     (i) R 7  and R 8  are independently H, F, Cl, Br, I, OH, OCH 3 , SH, SCH 3 , NH 2 , NHCH 3 , N(CH 3 ) 2 , CH 3 , CH 3-q X q , where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO 2 H, CO 2 CH 3 , CONH 2 , CONHCH 3 , or CON(CH 3 ) 2 , wherein R′ is a C 1-20  alkyl; a C 1-20  cycloalkyl; a C 2 -C 6  alkenyl, a C 2 -C 6  alkynyl; and 
     (j) R 9  is selected from among OH, OCH 3 , SH, SCH 3 , NH 2 , NHCH 3 , N(CH 3 ) 2 , OC(O)(C1-20 alkyl), which include but are not limited to OC(O)(CH 2 ) s CH 3 , NHC(O)(C1-20 alkyl), which include but are not limited to NHC(O)(CH 2 ) s CH 3 , and N(C(O)(CH 2 ) s CH 3 , which include but is not limited to N(C(O)(CH 2 ) s CH 3 ) 2 , where s is an integer selected from 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, and 19. 
     A fifth aspect of the first embodiment is directed to a compound represented by formula I-2 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, i-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, lower haloalkyl, di(lower alkyl)amino-lower alkyl, or aminoacyl; 
     (e) R 5  is H, CN, CH 3 , OCH 3 , CH 2 OH, CH 2 F, halogen, including F, Cl, Br, or I; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OCH 3 , NH 2 , or N 3 ; 
     (h) Y is OH, H, CH 3 , vinyl, N 3 , CN, Cl, Br, F, I, OC(O)CH 3 , OCH 3 , or O(aminoacyl); 
     (i) R 7  and R 8  are independently H, F, Cl, Br, I, OH, OCH 3 , SH, SCH 3 , NH 2 , NHCH 3 , N(CH 3 ) 2 , CH 3 , CH 3-q X q , where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO 2 H, CO 2 CH 3 , CONH 2 , CONHCH 3 , or CON(CH 3 ) 2 , wherein R′ is a C 1-20  alkyl; a C 1-20  cycloalkyl; a C 2 -C 6  alkenyl, a C 2 -C 6  alkynyl; and 
     (j) R 9  is selected from among OH, OCH 3 , SH, SCH 3 , NH 2 , NHCH 3 , N(CH 3 ) 2 , OC(O)(C 1-20  alkyl), which include but are not limited to OC(O)(CH 2 ) s CH 3 , NHC(O)(C 1-20  alkyl), which include but are not limited to NHC(O)(CH 2 ) s CH 3 , and N(C(O)(CH 2 ) s CH 3 ) 2 , which include but is not limited to N(C(O)(CH 2 ) s CH 3 ) 2 , where s is an integer selected from 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, and 19. 
     A sixth aspect of the first embodiment is directed to a compound represented by formula I-2 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, i-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3 , is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, C 1-10  alkyl, C 1-10  alkyl optionally substituted with a lower alkyl, alkoxy or halogen, C 1-10  haloalkyl, C 3-10  cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; 
     (e) R 5  is H, OMe, CN, CH 2 F, F, Cl, Br, or I; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, F, OCH 3 , F, Cl, Br, I, or N 3 ; 
     (h) Y is H, OH, CH 3 , F, Cl, Br, I, or N 3 , OCH 3 , OC(O)CH 3 , or O(aminoacyl); 
     (i) R 7  and R 8  are independently H, F, Br, SCH 3 , CH 3 , CH 3-q X q , where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO 2 CH 3 , CONH 2 , CONHCH 3 , or CON(CH 3 ) 2 ; and 
     (j) R 9  is selected from among OH, OCH 3 , SH, SCH 3 , NH 2 , NHCH 3 , N(CH 3 ) 2 , OC(O)(C 1-20  alkyl), which include but are not limited to OC(O)(CH 2 ) s CH 3 , NHC(O)(C 1-20  alkyl), which include but are not limited to NHC(O)(CH 2 ) s CH 3 , and N(C(O)(CH 2 ) s CH 3 ) 2 , which include but is not limited to N(C(O)(CH 2 ) s CH 3 ) 2 , where s is an integer selected from 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, and 19. 
     A seventh aspect of the first embodiment is directed to a compound represented by formula I-2 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, i-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, or N 3 ; 
     (h) Y is OH, OCH 3 , OC(O)CH 3 , or O(aminoacyl); 
     (i) R 7  and R 8  are independently H, F, Br, SCH 3 , CH 3 , CH 3-q X q , where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO 2 CH 3 , CONH 2 , CONHCH 3 , or CON(CH 3 ) 2 ; and 
     (j) R 9  is selected from among OH, OCH 3 , NH 2 , NHCH 3 , N(CH 3 ) 2 , OC(O)(C 1-20  alkyl), which include but are not limited to OC(O)(CH 2 ) s CH 3 , NHC(O)(C 1-20  alkyl), which include but are not limited to NHC(O)(CH 2 ) s CH 3 , and N(C(O)(CH 2 ) s CH 3 ) 2 , which include but is not limited to N(C(O)(CH 2 ) s CH 3 ) 2 , where s is an integer selected from among 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, and 19. 
     An eighth aspect of the first embodiment is directed to a compound represented by formula I-2 
     wherein 
     (a) R 1  is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, or N 3 ; 
     (h) Y is OH, OCH 3 , OC(O)CH 3 , or O(aminoacyl); 
     (i) R 7  and R 8  are independently H, F, Br, SCH 3 , CH 3 , CH 3-q X q , where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO 2 CH 3 , CONH 2 , CONHCH 3 , or CON(CH 3 ) 2 ; 
     (j) R 9  is selected from among OH, OCH 3 , NH 2 , NHCH 3 , N(CH 3 ) 2 , OC(O)(C 1-20  alkyl), which include but are not limited to OC(O)(CH 2 ) s CH 3 , NHC(O)(C 1-20  alkyl), which include but are not limited to NHC(O)(CH 2 )CH 3 , and N(C(O)(CH 2 ) s CH 3 ) 2 , which include but is not limited to N(C(O)(CH 2 ) s CH 3 ) 2 , where s is an integer selected from among 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, and 19. 
     A second embodiment of the invention is directed to a compound represented by formula I in which the base is a structure represented by formula b above, wherein R 1 , R 2 , R 3a , R 3b , R 4 , R 5 , R 6 , X, Y, R 7 , and R 8  are defined in the Summary of the Invention section above. 
     A first aspect of the second embodiment is directed to a compound represented by formula I-3 
     
       
         
         
             
             
         
       
     
     wherein 
     (a) R 1  is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  alkoxy, F, Cl, Br, I, nitro, cyano, C 1-6  haloalkyl, —N(R 1′ ) 2 , C 1-6  acylamino, —NHSO 2 C 1-6  alkyl, —SO 2 N(R 1′ ) 2 , COR 1″ , and —SO 2 C 1-6  alkyl; (R 1′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 1″  is —OR′ or —N(R 1′ ) 2 ); 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  and R 3b  are (i) independently selected from hydrogen, C 1-10  alkyl, cycloalkyl, —(CH 2 ) c (NR 3 ) 2 , C 1-6  hydroxyalkyl, —CH 2 SH, —(CH 2 ) 2 S(O) d Me, —(CH 2 ) 3 NHC(═NH)NH 2 , (1H-indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, —(CH 2 ) c COR 3″ , aryl and aryl C 1-3  alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, C 1-10  alkyl, C 1-6  alkoxy, halogen, nitro and cyano; (ii) R 3a  and R 3b  both are C 1-6  alkyl; (iii) R 3a  and R 3b  together are (CH 2 ) f  so as to form a spiro ring; (iv) R 3a  is hydrogen and R 3b  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms (v) R 3b  is hydrogen and R 3a  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R 3′  is independently hydrogen or C 1-6  alkyl and R 3″  is —OR′ or —N(R 3′ ) 2 ); (vi) R 3a  is H and R 3b  is H, CH 3 , CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; or (viii) R 3a  is CH 3 , —CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl and R 3b  is H, where R 3′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 3  is —OR′ or —N(R 3′ ) 2 ); 
     (d) R 4  is hydrogen, C 1-10  alkyl, C 1-10  alkyl optionally substituted with a lower alkyl, alkoxy or halogen, C 1-10  haloalkyl, C 3-10  cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; 
     (e) R 5  is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower alkyl, i.e., —(CH 2 ) p OH, where p is 1-6, including hydroxyl methyl (CH 2 OH), CH 2 F, N 3 , CH 2 CN, CH 2 NH 2 , CH 2 NHCH 3 , CH 2 N(CH 3 ) 2 , alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R 6  is H, R 5  cannot be N 3  and when X is OH, R 6  is CH 3  or CH 2 F and B is a purine base, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OMe, Cl, Br, I, NH 2 , or N 3 ; 
     (h) Y is OH, H, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, vinyl, N 3 , CN, Cl, Br, F, I, NO 2 , OC(O)O(C 1-4  alkyl), OC(O)O(C 1-4  alkyl), OC(O)O(C 2-4  alkynyl), OC(O)O(C 2-4  alkenyl), OC 1-10  haloalkyl, O(aminoacyl), O(C 1-10  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , or N(C 1-18  acyl) 2 , wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N 3 , CN, one to three halogen (Cl, Br, F, I), NO 2 , C(O)O(C 1-4  alkyl), C(O)O(C 1-4  alkyl), C(O)O(C 2-4  alkynyl), C(O)O(C 2-4  alkenyl), O(C 1-4  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , or N(C 1-4  acyl) 2 ; 
     (i) R 7  and R 8  are independently H, F, Cl, Br, I, OH, OR′, SH, SR′, NH 2 , NHR′, NR′ 2 , lower alkyl, halogenated (F, Cl, Br, I) lower alkyl, lower alkenyl of C 2 -C 6 , CO 2 H, CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , wherein R′ is a C 1-20  alkyl; a C 1-20  cycloalkyl; a C 2 -C 6  alkenyl, a C 2 -C 6  alkynyl. 
     The second aspect of the second embodiment is directed to a compound represented by formula I-3 
     wherein 
     (a) R 1  is hydrogen, n-alkyl or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of C 1-6  alkyl, C 1-6  alkoxy, F, Cl, Br, I, nitro, cyano, C 1-6  haloalkyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  and R 3b  are independently (i) R 3a  is hydrogen and R 3b  and R 2  together are (CH) n  so as to form a cyclic ring that includes the adjoining N and C atoms (v) R 3b  is hydrogen and R 3a  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 3 to 5, n is 2 to 4, and where R 3′  is independently hydrogen or C 1-6  alkyl and R 3″  is —OR′ or —N(R 3 ) 2 ); (vi) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; or (viii) R 3a  is CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), or CH 2 SH and R 3b  is H; 
     (d) R 4  is hydrogen, C 1-10  alkyl, C 1-10  alkyl optionally substituted with a lower alkyl, alkoxy or halogen, C 1-10  haloalkyl, C 3-10  cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; 
     (e) R 5  is H, CN, CH 3 , vinyl, OCH 3 , OCH 2 CH 3 , CH 2 OH, CH 2 (halo), such as CH 2 F, N 3 , CH 2 CN, CH 2 N 3 , CH 2 NH 2 , CH 2 NHCH 3 , CH 2 N(CH 3 ) 2 , halogen, including F, Cl, Br, or I; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OMe, halogen, NH 2 , or N 3 ; 
     (h) Y is OH, H, C 1-4  alkyl, vinyl, N 3 , CN, Cl, Br, F, I, O(C 1-6  acyl), O(C 1-4  alkyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-18  acyl) 2 , wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N 3 , CN, one to three halogen (Cl, Br, F, I), NO 2 , OC(O)O(C 1-4  alkyl), OC(O)O(C 1-4  alkyl), OC(O)O(C 2-4  alkynyl), OC(O)O(C 2-4  alkenyl), OC 1-10  haloalkyl, O(aminoacyl), O(C 1-4  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-4  acyl) 2 ; 
     (i) R 7  and R 8  are independently H, F, Cl, Br, I, OH, OR′, SH, SR′, NH 2 , NHR′, NR′ 2 , lower alkyl, halogenated (F, Cl, Br, I) lower alkyl, lower alkenyl of C 2 -C 6 , CO 2 H, CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , wherein R′ is a C 1-20  alkyl; a C 1-20  cycloalkyl; a C 2 -C 6  alkenyl, a C 2 -C 6  alkynyl. 
     The third aspect of the second embodiment is directed to a compound represented by formula I-3 
     wherein 
     (a) R 1  is hydrogen, n-alkyl or a substituted or unsubstituted phenyl, where the substitutent of the substituted phenyl is at least one of a C 1-3  alkyl, a C 1-3  alkoxy, F, Cl, Br, I, nitro, cyano, and a C 1-3  haloalkyl; 
     (b) R 2  is hydrogen, CH 3 , R 3a  or R 3b  and R 2  together are (CH 2 ) 3  so as to form a cyclic ring that includes the adjoining N and C atoms, C(O)CR 3a R 3b NHR 1 , where n is 2 to 4 and R 1 , R 3a , and R 3b  are as defined herein; 
     (c) R 3a  and R 3b  are independently (i) R 3a  is hydrogen and R 3b  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms (v) R 3b  is hydrogen and R 3a  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 3 to 5, n is 2 to 4, and where R 3  is independently hydrogen or C 1-6  alkyl and R 3″  is —OR′ or —N(R 3′ ) 2 ); (vi) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; or (viii) R 3a  is CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CHCH2C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl and R 3b  is H; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, CN, CH 3 , OCH 3 , CH 2 OH, CH 2 (halo), such as CH 2 F, N 3 , CH 2 CN, CH 2 N 3 , CH 2 NH 2 , CH 2 NHCH 3 , CH 2 N(CH 3 ) 2 , halogen, including F, Cl, Br, or I; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OCH 3 , halogen, NH 2 , or N 3    
     (h) Y is OH, H, CH 3 , vinyl, N 3 , CN, Cl, Br, F, I, OC(O)CH 3 , OCH 3 , NH 2 , NHCH 3 , NH(vinyl), NH(acetyl), NH(C(O)CH 3 ), N(CH 3 ) 2 , N(C(O)CH 3 ) 2 ; 
     (i) R 7  and R 8  are independently H, F, Cl, Br, I, OH, OCH 3 , SH, SCH 3 , NH 2 , NHCH 3 , N(CH 3 ) 2 , CH 3 , CH 3-q X q , where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO 2 H, CO 2 CH 3 , CONH 2 , CONHCH 3 , or CON(CH 3 ) 2 . 
     The fourth aspect of the second embodiment is directed to a compound represented by formula I-3 
     wherein 
     (a) R 1  is hydrogen, n-alkyl or a substituted or unsubstituted phenyl, where the substitutent of the substituted phenyl is at least one of a CH 3 , OCH 3 , F, Cl, Br, I, nitro, cyano, and a CH 3-q X q  where X is F, Cl, Br, or I, and q is 1-3; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl or R 3a  is CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl and R 3b  is H; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, CN, CH 3 , OCH 3 , CH 2 OH, CH 2 (halo), such as CH 2 F, N 3 , CH 2 CN, CH 2 N 3 , CH 2 NH 2 , CH 2 NHCH 3 , CH 2 N(CH 3 ) 2 , halogen, including F, Cl, Br, or I; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OCH 3 , NH 2 , or N 3 ; 
     (h) Y is OH, H, CH 3 , vinyl, N 3 , CN, Cl, Br, F, I, OC(O)CH 3 , OCH 3 , NH 2 , NHCH 3 , NH(vinyl), NH(acetyl), NH(C(O)CH 3 ), N(CH 3 ) 2 , N(C(O)CH 3 ) 2 ; 
     (i) R 7  and R 8  are independently H, F, Cl, Br, I, OH, OCH 3 , SH, SCH 3 , NH 2 , NHCH 3 , N(CH 3 ) 2 , CH 3 , CH 3-q X q , where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO 2 H, CO 2 CH 3 , CONH 2 , CONHCH 3 , or CON(CH 3 ) 2 , wherein R′ is a C 1-20  alkyl; a C 1-20  cycloalkyl; a C 2 -C 6  alkenyl, a C 2 -C 6  alkynyl. 
     The fifth aspect of the second embodiment is directed to a compound represented by formula I-4 
     
       
         
         
             
             
         
       
     
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, i-propyl, i-propyl, or a substituted or unsubstituted phenyl, where the substitutent of the substituted phenyl is at least one of a CH 3 , OCH 3 , F, Cl, Br, I, nitro, cyano, and a CH 3-q X q , where X is F, Cl, Br, or I, and q is 1-3; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl or R 3a  is CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl and R 3b  is H; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl: 
     (e) R 5  is H, CN, CH 3 , OCH 3 , CH 2 OH, CH 2 F, N 3 , CH 2 CN, CH 2 N 3 , CH 2 NH 2 , CH 2 NHCH 3 , CH 2 N(CH 3 ) 2 , halogen, including F, Cl, Br, or I; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OCH 3 , Cl, Br, I, NH 2 , or N 3 ; 
     (h) Y is OH, H, CH 3 , vinyl, N 3 , CN, Cl, Br, F, I, OC(O)CH 3 , OCH 3 , NH 2 , NHCH 3 , NH(vinyl), NH(acetyl), NH(C(O)CH 3 ), N(CH 3 ) 2 , N(C(O)CH 3 ) 2 ; 
     (i) R 7  and R 8  are independently H, F, Cl, Br, I, OH, OCH 3 , SH, SCH 3 , NH 2 , NHCH 3 , N(CH 3 ) 2 , CH 3 , CH 3-q X q , where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO 2 H, CO 2 CH 3 , CONH 2 , CONHCH 3 , or CON(CH 3 ) 2 , wherein R′ is a C 1-20  alkyl; a C 1-20  cycloalkyl; a C 2 -C 6  alkenyl, a C 2 -C 6  alkynyl, 
     The sixth aspect of the second embodiment is directed to a compound represented by formula I-4 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CHM)CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, CN, CH 3 , OCH 3 , CH 2 OH, CH 2 F, halogen, including F, Cl, Br, or I; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OCH 3 , NH 2 , or N 3 ; 
     (h) Y is OH, H, CH 3 , vinyl, NH 2 , N 3 , CN, Cl, Br, F, I, OC(O)CH 3 , OCH 3 ; 
     (i) R 7  and R 8  are independently H, F, Cl, Br, I, OH, OCH 3 , SH, SCH 3 , NH 2 , NHCH 3 , N(CH 3 ) 2 , CH 3 , CH 3-q X q , where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO 2 H, CO 2 CH 3 , CONH 2 , CONHCH 3 , or CON(CH 3 ) 2 , wherein R′ is a C 1-20  alkyl; a C 1-20  cycloalkyl; a C 2 -C 6  alkenyl, a C 2 -C 6  alkynyl. 
     The seventh aspect of the second embodiment is directed to a compound represented by formula I-4 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, OMe, CN, CH 2 F, F, Cl, Br, or I; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, F, OCH 3 , F, Cl, Br, I, NH 2  or N 3 ; 
     (h) Y is H, OH, CH 3 , F, Cl, Br, I, NH 2  or N 3 , OCH 3 , or OC(O)CH 3 , 
     (i) R 7  and R 8  are independently H, F, Br, SCH 3 , CH 3 , CH 3-q X q , where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO 2 CH 3 , CONH 2 , CONHCH 3 , or CON(CH 3 ) 2 ; 
     The eighth aspect of the second embodiment is directed to a compound represented by formula I-4 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, NH 2  or N 3 ; 
     (h) Y is OH, NH 2 , OCH 3 , or OC(O)CH 3 ; 
     (i) R 7  and R 8  are independently H, F, Br, SCH 3 , CH 3 , CH 3-q X q , where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO 2 CH 3 , CONH 2 , CONHCH 3 , or CON(CH 3 ) 2 . 
     The ninth aspect of the second embodiment is directed to a compound represented by formula I-4 
     wherein 
     (a) R 1  is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, or N 3 ; 
     (h) Y is OH, OCH 3 , or OC(O)CH 3 ; 
     (i) R 7  and R 8  are independently H, F, Br, SCH 3 , CH 3 , CH 3-q X q , where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO 2 CH 3 , CONH 2 , CONHCH 3 , or CON(CH 3 ) 2 . 
     A third embodiment of the invention is directed to a compound represented by formula I in which the base is a structure represented by formula c above, wherein R 1 , R 2 , R 3a , R 3b , R 4 , R 5 , R 6 , X, Y, Z, R 10 , R 11 , and R 12  are defined in the Summary of the Invention section above; with the proviso that R 11  is not H. 
     A first aspect of the third embodiment is directed to a compound represented by formula I-5 
     
       
         
         
             
             
         
       
     
     wherein 
     (a) R 1  is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  alkoxy, F, Cl, Br, I, nitro, cyano, C 1-6  haloalkyl, —N(R 1′ ) 2 , C 1-6  acylamino, —NHSO 2 C 1-6  alkyl, —SO 2 N(R 1′ ) 2 , COR 1″ , and —SO 2 C 1-6  alkyl; (R 1′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 1″  is —OR′ or —N(R 1′ ) 2 ); 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  and R 3b  are (i) independently selected from hydrogen, C 1-10  alkyl, cycloalkyl, —(CH 2 ) c (NR 3′ ) 2 , C 1-6  hydroxyalkyl, —CH 2 SH, —(CH 2 ) 2 S(O) d Me, —(CH 2 ) 3 NHC(═NH)NH 2 , (1H-indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, —(CH 2 ) e COR 3″ , aryl and aryl C 1-3  alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, C 1-10  alkyl, C 1-6  alkoxy, halogen, nitro and cyano; (ii) R 3a  and R 3b  both are C 1-6  alkyl; (iii) R 3a  and R 3b  together are (CH 2 ) f  so as to form a spiro ring; (iv) R 3a  is hydrogen and R 3b  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms (v) R 3b  is hydrogen and R 3a  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R 3′  is independently hydrogen or C 1-6  alkyl and R 3  is —OR′ or —N(R 3 ) 2 ); (vi) R 3a  is H and R 3b  is from H, CH 3 , CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; or (viii) R 3a  is CH 3 , —CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl and R 3b  is H, where R 3′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 3″  is —OR′ or —N(R 3′ ) 2 ); 
     (d) R 4  is hydrogen, C 1-10  alkyl, C 1-10  alkyl optionally substituted with a lower alkyl, alkoxy or halogen, C 1-10  haloalkyl, C 3-10  cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; 
     (e) R 5  is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower alkyl, i.e., —(CH 2 ) p OH, where p is 1-6, including hydroxyl methyl (CH 2 OH), CH 2 F, N 3 , CH 2 CN, CH 2 NH 2 , CH 2 NHCH 3 , CH 2 N(CH 3 ) 2 , alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R 6  is H, R 5  cannot be N 3  and when X is OH, R 6  is CH 3  or CH 2 F and B is a purine base, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OMe, halogen, NH 2 , or N 3 , 
     (h) Y is OH, H, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, vinyl, N 3 , CN, Cl, Br, F, I, NO 2 , OC(O)O(C 1-4  alkyl), OC(O)O(C 1-4  alkyl), OC(O)O(C 2-4  alkynyl), OC(O)O(C 2-4  alkenyl), OC 1-10  haloalkyl, O(aminoacyl), O(C 1-10  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-18  acyl) 2 , wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N 3 , CN, one to three halogen (Cl, Br, F, I), NO 2 , C(O)O(C 1-4  alkyl), C(O)O(C 1-4  alkyl), C(O)O(C 2-4  alkynyl), C(O)O(C 2-4  alkenyl), O(C 1-4  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-4  acyl) 2 ; 
     (i) R 10  and R 11  are independently H, F, Cl, Br, I, OH, OR′, SH, SR′, NH 2 , NHR′, NR′ 2 , lower alkyl of C 1 -C 6 , halogenated (F, Cl, Br, I) lower alkyl of C 1 -C 6 , lower alkenyl of C 2 -C 6 , halogenated (F, Cl, Br, I) lower alkenyl of C 2 -C 6 , lower alkynyl of C 2 -C 6  such as C≡CH, halogenated (F, Cl, Br, I) lower alkynyl of C 2 -C 6 , lower alkoxy of C 1 -C 6 , halogenated (F, Cl, Br, I) lower alkoxy of C 2 -C 6 , CO 2 H, COR′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, with the proviso that when R 10  is OH and R 11  is not NH 2 ; 
     wherein R′ is an optionally substituted alkyl, which includes, but is not limited to, an optionally substituted C 1-20  alkyl, an optionally substituted C 1-10  alkyl, an optionally substituted lower alkyl; an optionally substituted cycloalkyl; an optionally substituted alkynyl of C 2 -C 6 , an optionally substituted lower alkenyl of C 2 -C 6 , or optionally substituted acyl, which includes but is not limited to C(O) alkyl, C(O)(C 1-2  alkyl), C(O)(C 1-10  alkyl), or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 12 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OH, OR′, SH, SR′, NH 2 , NHR′, NR′ 2 , NO 2  lower alkyl of C 1 -C 6 , halogenated (F, Cl, Br, I) lower alkyl of C 1 -C 6 , lower alkenyl of C 2 -C 6 , halogenated (F, Cl, Br, I) lower alkenyl of C 2 -C 6 , lower alkynyl of C 2 -C 6 , halogenated (F, Cl, Br, I) lower alkynyl of C 2 -C 6 , lower alkoxy of C 1 -C 6 , halogenated (F, Cl, Br, I) lower alkoxy of C 1 -C 6 , CO 2 H, CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H or CH═CHCO 2 R′. 
     A second aspect of the third embodiment is directed to a compound represented by formula I-5 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, CN, CH 3 , OCH 3 , CH 2 OH, CH 2 F, halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H. 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OCH 3 , Cl, Br, I, NH 2 , or N 3 ; 
     (h) Y is OH, H, CH 3 , vinyl, NH 2 . N 3 , CN, Cl, Br, F, I, OC(O)CH 3 , OCH 3 ; 
     (i) R 10  and R 11  are independently H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, with the proviso that when R 10  is OH and R 11  is not NH 2 ; 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 2 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′. 
     A third aspect of the third embodiment is directed to a compound represented by formula I-5 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, CN, CH 2 F, F, Cl, Br, or I; with the proviso that X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H: 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, F, OCH 3 , F, Cl, Br, I, NH 2  or N 3 ; 
     (h) Y is H, OH, CH 3 , F, Cl, Br, I, NH 2  or N 3 , OCH 3 , or OC(O)CH 3 ; 
     (i) R 10  and R 11  are independently H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, with the proviso that when R 10  is OH and R 11  is not NH 2 ; 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 12 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′. 
     A fourth aspect of the third embodiment is directed to a compound represented by formula I-5 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, i-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, NH 2  or N 3 ; 
     (h) Y is OH, NH 2 , OCH 3 , or OC(O)CH 3 ; 
     (i) R 10  and R 11  are independently H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, with the proviso that when R 10  is OH and R 11  is not NH 2 ;
         wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and       

     (j) Z is N or CR 12 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′. 
     A fifth aspect of the third embodiment is directed to a compound represented by formula I-5 
     wherein 
     (a) R 1  is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, NH 2  or N 3 ; 
     (h) Y is OH, NH 2 , OCH 3 , or OC(O)CH 3 ; 
     (i) R 10  and R 11  are independently H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, with the proviso that when R 10  is OH and R 11  is not NH 2 ; 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is Nor CR 12 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′. 
     A sixth aspect of the third embodiment is directed to a compound represented by formula I-5 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, CN, CH 3 , OCH 3 , CH 2 OH, CH 2 F, halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H. 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OCH 3 , Cl, Br, I, NH 2 , or N 3 ; 
     (h) Y is OH, H, CH 3 , vinyl, NH 2 , N 3 , CN, Cl, Br, F, I, OC(O)CH 3 , OCH 3 ; 
     (i) R 10  is NH 2  and R 11  is H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′; 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 12 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′. 
     A seventh aspect of the third embodiment is directed to a compound represented by formula I-5 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, CN, CH 2 F, F, Cl, Br, or I; with the proviso that X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, F, OCH 3 , F, Cl, Br, I, NH 2  or N 3 ; 
     (h) Y is H, OH, CH 3 , F, Cl, Br, I, NH 2  or N 3 , OCH 3 , or OC(O)CH 3 ; 
     (i) R 10  is NH 2  and R 11  is H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′, CH═CHCO 2 H, or CH═CHCO 2 R′; 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 2 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′. 
     An eighth aspect of the third embodiment is directed to a compound represented by formula I-5 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl; 
     (e) R 5  is H, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, NH 2  or N 3 ; 
     (h) Y is OH, NH 2 , OCH 3 , or OC(O)CH 3 ; 
     (i) R 10  is NH 2  and R 11  is H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′; 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 2 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′. 
     A ninth aspect of the third embodiment is directed to a compound represented by formula I-5 
     wherein 
     (a) R 1  is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, or N-methyl-pyrrolidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, NH 2  or N 3 ; 
     (h) Y is OH, NH 2 , OCH 3 , or OC(O)CH 3 ; 
     (i) R 10  is NH 2  and R 11  is H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′; 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 2 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′. 
     A tenth aspect of the third embodiment is directed to a compound represented by formula I-6 
     
       
         
         
             
             
         
       
     
     wherein 
     (a) R 1  is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  alkoxy, F, Cl, Br, I, nitro, cyano, C 1-6  haloalkyl, —N(R 1′ ) 2 , C 1-6  acylamino, —NHSO 2 C 1-6  alkyl, —SO 2 N(R 1′ ) 2 , COR 1″ , and —SO 2 C 1-6  alkyl; (R 1′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 1″  is —OR′ or —N(R 1′ ) 2 ); 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  and R 3b  are (i) independently selected from hydrogen, C 1-10  alkyl, cycloalkyl, —(CH 2 ) c (NR 3 ) 2 , C 1-6  hydroxyalkyl, —CH 2 SH, —(CH 2 ) 2 S(O) d Me, —(CH 2 ) 3 NHC(═NH)NH 2 , (1H-indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, —(CH 2 ) e COR 3″ , aryl and aryl C 1-3  alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, C 1-10  alkyl, C 1-6  alkoxy, halogen, nitro and cyano; (ii) R 3a  and R 3b  both are C 1-6  alkyl; (iii) R 3a  and R 3b  together are (CH 2 ) f  so as to form a spiro ring; (iv) R 3a  is hydrogen and R 3b  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms (v) R 3b  is hydrogen and R 3a  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R 3′  is independently hydrogen or C 1-6  alkyl and R 3″  is —OR′ or —N(R 3′ ) 2 ); (vi) R 3a  is H and R 3b  is H, CH 3 , CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; or (viii) R 3a  is CH 3 , —CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl and R 3b  is H, where R 3′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 3″  is —OR′ or —N(R 3′ ) 2 ); 
     (d) R 4  is hydrogen, C 1-10  alkyl, C 1-10  alkyl optionally substituted with a lower alkyl, alkoxy or halogen, C 1-10  haloalkyl, C 3-10  cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; 
     (e) R 5  is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower alkyl, i.e., —(CH 2 ) p OH, where p is 1-6, including hydroxyl methyl (CH 2 OH), CH 2 F, N 3 , CH 2 CN, CH 2 NH 2 , CH 2 NHCH 3 , CH 2 N(CH 3 ) 2 , alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R 6  is H, R 5  cannot be N 3  and when X is OH, R 6  is CH 3  or CH 2 F and B is a purine base, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OMe, Cl, Br, I, NH 2 , or N 3 ; 
     (h) Y is OH, H, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, vinyl, N 3 , CN, Cl, Br, F, I, NO 2 , OC(O)O(C 1-4  alkyl), OC(O)O(C 1-4  alkyl), OC(O)O(C 2-4  alkynyl), OC(O)O(C 2-4  alkenyl), OC 1-10  haloalkyl, O(aminoacyl), O(C 1-10  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-18  acyl) 2 , wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N 3 , CN, one to three halogen (Cl, Br, F, I), NO 2 , C(O)O(C 1-4  alkyl), C(O)O(C 1-4  alkyl), C(O)O(C 2-4  alkynyl), C(O)O(C 2-4  alkenyl), O(C 1-4  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-4  acyl) 2 ; 
     (i) R 10  and R 11  are independently H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, with the proviso that when R 10  is OH and R 11  is not NH 2 ; 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 2 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′. 
     An eleventh aspect of the third embodiment is directed to a compound represented by formula I-6 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, CN, CH 3 , OCH 3 , CH 2 OH, CH 2 F, halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OCH 3 , Cl, Br, I, NH 2 , or N 3 ; 
     (h) Y is OH, H, CH 3 , vinyl, NH 2 , N 3 , CN, Cl, Br, F, I, OC(O)CH 3 , OCH 3 ; 
     (i) R 10  and R 11  are independently H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, with the proviso that when R 10  is OH and R 11  is not NH 2 ; 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 12 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′. 
     A twelfth aspect of the third embodiment is directed to a compound represented by formula I-6 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, i-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, CN, CH 2 F, F, Cl, Br, or I, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H: 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, F, OCH 3 , F, Cl, Br, I, NH 2  or N 3 ; 
     (h) Y is H, OH, CH 3 , F, Cl, Br, I, NH 2  or N 3 , OCH 3 , or OC(O)CH 3 ; 
     (i) R 10  and R 11  are independently H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, with the proviso that when R 10  is OH and R 11  is not NH 2 ; 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is Nor CR 1 ; and 
     R 12  is a H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′. 
     A thirteenth aspect of the third embodiment is directed to a compound represented by formula I-6 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, i-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3 , is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R′ is H, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, NH 2  or N 3 ; 
     (h) Y is OH, NH 2 , OCH 3 , or OC(O)CH 3 ; 
     (i) R 10  and R 11  are independently H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, with the proviso that when R 10  is OH and R 11  is not NH 2 ; 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is Nor CR 12 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′. 
     A fourteenth aspect of the third embodiment is directed to a compound represented by formula I-6 
     wherein 
     (a) R 1  is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, NH 2  or N 3 ; 
     (h) Y is OH, NH 2 , OCH 3 , or OC(O)CH 3 ; 
     (i) R 10  and R 11  are independently H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, with the proviso that when R 10  is OH and R 11  is not NH 2 ; 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 12 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′. 
     A fifteenth aspect of the third embodiment is directed to a compound represented by formula I-6 
     wherein 
     (a) R 1  is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  alkoxy, F, Cl, Br, I, nitro, cyano, C 1-6  haloalkyl, —N(R 1′ ) 2 , C 1-6  acylamino, —NHSO 2 C 1-6  alkyl, —SO 2 N(R 1′ ) 2 , COR 1″ , and —SO 2 C 1-6  alkyl; (R 1′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 1″  is —OR′ or —N(R 1′ ) 2 ); 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  and R 3b  are (i) independently selected from hydrogen, C 1-10  alkyl, cycloalkyl, —(CH 2 ) c (NR 3 ) 2 , C 1-6  hydroxyalkyl, —CH 2 SH, —(CH 2 ) 2 S(O) d Me, —(CH 2 ) 3 NHC(═NH)NH 2 , (1H-indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, —(CH 2 ) e COR 3″ , aryl and aryl C 1-3  alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, C 1-10  alkyl, C 1-6  alkoxy, halogen, nitro and cyano; (ii) R 3a  and R 3b  both are C 1-6  alkyl; (iii) R 3a  and R 3b  together are (CH 2 ) f  so as to form a spiro ring; (iv) R 3a  is hydrogen and R 3b  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms (v) R 3b  is hydrogen and R 3a  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R 3′  is independently hydrogen or C 1-6  alkyl and R 3  is —OR′ or —N(R 3′ ) 2 ); (vi) R 3a  is H and R 3b  is H, CH 3 , CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; or (viii) R 3a  is CH 3 , —CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl and R 3b  is H, where R 3′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 3″  is —OR′ or —N(R 3′ ) 2 ); 
     (d) R 4  is hydrogen, C 1-10  alkyl, C 1-10  alkyl optionally substituted with a lower alkyl, alkoxy or halogen, C 1-10  haloalkyl, C 3-10  cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; 
     (e) R 5  is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower alkyl, i.e., —(CH 2 ) p OH, where p is 1-6, including hydroxyl methyl (CH 2 OH), CH 2 F, N 3 , CH 2 CN, CH 2 NH 2 , CH 2 NHCH 3 , CH 2 N(CH 3 ) 2 , alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R 6  is H, R 5  cannot be N 3  and when X is OH, R is CH 3  or CH 2 F and B is a purine base, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OMe, halogen, NH 2 , or N 3 , 
     (h) Y is OH, H, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, vinyl, N 3 , CN, Cl, Br, F, I, NO 2 , OC(O)O(C 1-4  alkyl), OC(O)O(C 1-4  alkyl), OC(O)O(C 2-4  alkynyl), OC(O)O(C 2-4  alkenyl), OC 1-10  haloalkyl, O(aminoacyl), O(C 1-10  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-18  acyl) 2 , wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N 3 , CN, one to three halogen (Cl, Br, F, I), NO 2 , C(O)O(C 1-4  alkyl), C(O)O(C 1-4  alkyl), C(O)O(C 2-4  alkynyl), C(O)O(C 2-4  alkenyl), O(C 1-4  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-4  acyl) 2 ; 
     (i) R 10  is NH 2  and R 11  is H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′; 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 12 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′. 
     An sixteenth aspect of the third embodiment is directed to a compound represented by formula I-6 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, CN, CH 3 , OCH 3 , CH 2 OH, CH 2 F, halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OCH 3 , Cl, Br, I, NH 2 , or N 3 ; 
     (h) Y is OH, H, CH 3 , vinyl, NH 2 , N 3 , CN, Cl, Br, F, I, OC(O)CH 3 , OCH 3 ; 
     (i) R 10  is NH 2  and R 11  is H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , COR′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′; 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 12 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO, lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′. 
     A seventeenth aspect of the third embodiment is directed to a compound represented by formula I-6 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, CN, CH 2 F, F, Cl, Br, or I, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, F, OCH 3 , F, Cl, Br, I, NH 2  or N 3 ; 
     (h) Y is H, OH, CH 3 , F, Cl, Br, I, NH 2  or N 3 , OCH 3 , or OC(O)CH 3 ; 
     (i) R 10  is NH 2  and R 11  is H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′; 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 12 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO, lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′. 
     An eighteenth aspect of the third embodiment is directed to a compound represented by formula I-6 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, i-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3 , is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, NH 2  or N 3 ; 
     (h) Y is OH, NH 2 , OCH 3 , or OC(O)CH 3 ; 
     (i) R 10  is NH 2  and R 11  is H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′; 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 12 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′. 
     A nineteenth aspect of the third embodiment is directed to a compound represented by formula I-6 
     wherein 
     (a) R 1  is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, NH 2  or N 3 ; 
     (h) Y is OH, NH 2 , OCH 3 , or OC(O)CH 3 ; 
     (i) R 10  is NH 2  and R 11  are independently H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′; 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 12 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′. 
     A fourth embodiment of the invention is directed to a compound represented by formula I in which the base is a structure represented by formula c above, where R 11  is H and R 2 , R 3a , R 3b , R 4 , R 5 , R 6 , X, and Y are defined in the Summary of the Invention section above. 
     A first aspect of the fourth embodiment is directed to a compound represented by formula I-7 
     
       
         
         
             
             
         
       
     
     wherein 
     (a) R 1  is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  alkoxy, F, Cl, Br, I, nitro, cyano, C 1-6  haloalkyl, —N(R 1′ ) 2 , C 1-6  acylamino, —NHSO 2 C 1-6  alkyl, —SO 2 N(R 1′ ) 2 , COR 1″ , and —SO 2 C 1-6  alkyl; (R 1′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 1″  is —OR′ or —N(R 1′ ) 2 ); 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  and R 3b  are (i) independently selected from hydrogen, C 1-10  alkyl, cycloalkyl, —(CH 2 ) c (NR 3′ ) 2 , C 1-6  hydroxyalkyl, —CH 2 SH, —(CH 2 ) 2 S(O) d Me, —(CH 2 ) 3 NHC(═NH)NH 2 , (1H-indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, —(CH 2 ) e COR 3 , aryl and aryl C 1-3  alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, C 1-10  alkyl, C 1-6  alkoxy, halogen, nitro and cyano; (ii) R 3a  and R 3b  both are C 1-6  alkyl; (iii) R 3a  and R 3b  together are (CH 2 ) f  so as to form a spiro ring; (iv) R 3a  is hydrogen and R 3b  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms (v) R 3b  is hydrogen and R 3a  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R 3′  is independently hydrogen or C 1-6  alkyl and R 3″  is —OR′ or —N(R 3′ ) 2 ); (vi) R 3a  is H and R 3b  is H, CH 3 , CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; or (viii) R 3a  is CH 3 , —CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl and R 3b  is H, where R 3′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 3″  is —OR′ or —N(R 3′ ) 2 ); 
     (d) R 4  is hydrogen, C 1-10  alkyl, C 1-10  alkyl optionally substituted with a lower alkyl, alkoxy or halogen, C 1-10  haloalkyl, C 3-10  cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; 
     (e) R 5  is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower alkyl, i.e., —(CH 2 ) p OH, where p is 1-6, including hydroxyl methyl (CH 2 OH), CH 2 F, N 3 , CH 2 CN, CH 2 NH 2 , CH 2 NHCH 3 , CH 2 N(CH 3 ) 2 , alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R 6  is H, R 5  cannot be N 3  and when X is OH, R 6  is CH 3  or CH 2 F and B is a purine base, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OMe, halogen, NH 2 , or N 3 ; 
     (h) Y is OH, H, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, vinyl, N 3 , CN, Cl, Br, F, I, NO 2 , OC(O)O(C 1-4  alkyl), OC(O)O(C 1-4  alkyl), OC(O)O(C 2-4  alkynyl), OC(O)O(C 2-4  alkenyl), OC 1-10  haloalkyl, O(aminoacyl), O(C 1-10  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-18  acyl) 2 , wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N 3 , CN, one to three halogen (Cl, Br, F, I), NO 2 , C(O)O(C 1-4  alkyl), C(O)O(C 1-4  alkyl), C(O)O(C 2-4  alkynyl), C(O)O(C 2-4  alkenyl), O(C 1-4  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-4  acyl) 2 ; 
     (i) R 10  is H, F, Cl, Br, I, OH, OR′, SH, SR′, NH 2 , NHR′, NR′ 2 , lower alkyl of C 1 -C 6 , halogenated (F, Cl, Br, I) lower alkyl of C 1 -C 6 , lower alkenyl of C 2 -C 6 , halogenated (F, Cl, Br, I) lower alkenyl of C 2 -C 6 , lower alkynyl of C 2 -C 6  such as C≡CH, halogenated (F, Cl, Br, I) lower alkynyl of C 2 -C 6 , lower alkoxy of C 1 -C 6 , halogenated (F, Cl, Br, I) lower alkoxy of C 1 -C 6 , CO 2 H, CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H or CH═CHCO 2 R′, 
     wherein R′ is an optionally substituted alkyl, which includes, but is not limited to, an optionally substituted C 1-20  alkyl, an optionally substituted C 1-10  alkyl, an optionally substituted lower alkyl; an optionally substituted cycloalkyl; an optionally substituted alkynyl of C 2 -C 6 , an optionally substituted lower alkenyl of C 2 -C 6 , or optionally substituted acyl, which includes but is not limited to C(O) alkyl, C(O)(C 1-20  alkyl), C(O)(C 1-10  alkyl), or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 12 ; and 
     R 12  is H, halogen (including F, Cl, Br, I), OH, OR′, SH, SR′, NH 2 , NHR′, NR′ 2 , NO 2  lower alkyl of C 1 -C 6 , halogenated (F, Cl, Br, I) lower alkyl of C 2 -C 6 , lower alkenyl of C 2 -C 6 , halogenated (F, Cl, Br, I) lower alkenyl of C 2 -C 6 , lower alkynyl of C 2 -C 6 , halogenated (F, Cl, Br, I) lower alkynyl of C 2 -C 6 , lower alkoxy of C 1 -C 6 , halogenated (F, Cl, Br, I) lower alkoxy of C 1 -C 6 , CO 2 H, CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′; with the proviso that R 1  is not a: (i) —C≡C—H, (ii) —C═CH 2 , or (iii) —NO 2 . 
     A second aspect of the fourth embodiment is directed to a compound represented by formula I-7 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, CN, CH 3 , OCH 3 , CH 2 OH, CH 2 F, halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H. 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OCH 3 , halogen, NH 2 , or N 3 ; 
     (h) Y is OH, H, CH 3 , vinyl, NH 2 . N 3 , CN, Cl, Br, F, I, OC(O)CH 3 , OCH 3 ; 
     (i) R 10  is H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 12 ; and 
     R 12  is H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO, lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′; with the proviso that R′ is not a: (i) —C≡C—H, (ii) —C═CH 2 , or (iii) —NO 2 . 
     A third aspect of the third embodiment is directed to a compound represented by formula I-7 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, CN, CH 2 F, F, Cl, Br, or I; with the proviso that X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, F, OCH 3 , F, Cl, Br, I, NH 2  or N 3 ; 
     (h) Y is H, OH, CH 3 , F, Cl, Br, I, NH 2  or N 3 , OCH 3 , or OC(O)CH 3 ; 
     (i) R 10  is H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 12 ; and 
     R 12  is H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′; with the proviso that R 1  is not a: (i) —C≡C—H, (ii) —C═CH 2 , or (iii) —NO 2 . 
     A fourth aspect of the fourth embodiment is directed to a compound represented by formula I-7 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, NH 2  or N 3 ; 
     (h) Y is OH, NH 2 , OCH 3 , or OC(O)CH 3 ; 
     (i) R 10  and R 11  H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is Nor CR 12 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′; with the proviso that R 12  is not a: (i) —C≡C—H, (ii) —C═CH 2 , or (iii) —NO 2 . 
     A fifth aspect of the fourth embodiment is directed to a compound represented by formula I-7 
     wherein 
     (a) R 1  is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H, 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, NH 2  or N 3 ; 
     (h) Y is OH, NH 2 , OCH 3 , or OC(O)CH 3 ; 
     (i) R 10  is H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 2 ; and 
     R 12  is H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′. 
     A sixth aspect of the fourth embodiment is directed to a compound represented by formula I-8 
     
       
         
         
             
             
         
       
     
     wherein 
     (a) R 1  is hydrogen, n-alkyl: branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  alkoxy, F, Cl, Br, I, nitro, cyano, C 1-6  haloalkyl, —N(R 1′ ) 2 , C 1-6  acylamino, —NHSO 2 C 1-6  alkyl, —SO 2 N(R 1′ ) 2 , COR 1″ , and —SO 2 C 1-6  alkyl; (R 1′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 1  is —OR′ or —N(R 1′ ) 2 ); 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3  and R 3b  are (i) independently selected from hydrogen, C 1-10  alkyl, cycloalkyl, —(CH 2 ) c (NR 3′ ) 2 , C 1-6  hydroxyalkyl, —CH 2 SH, —(CH 2 ) 2 S(O) d Me, —(CH 2 ) 3 NHC(═NH)NH 2 , (1H-indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, —(CH 2 ) e COR 3 , aryl and aryl C 1-3  alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, C 1-10  alkyl, C 1-6  alkoxy, halogen, nitro and cyano; (ii) R 3a  and R 3b  both are C 1-6  alkyl; (iii) R 3a  and R 3b  together are (CH 2 ) f  so as to form a spiro ring; (iv) R 3a  is hydrogen and R 3b  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms (v) R 3b  is hydrogen and R 3a  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R 3′  is independently hydrogen or C 1-6  alkyl and R 3″  is —OR′ or —N(R 3′ ) 2 ); (vi) R 3a  is H and R 3b  is H, CH 3 , CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; or (viii) R 3a  is CH 3 , —CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl and R 3b  is H, where R 3′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 3  is —OR′ or —N(R 3 ) 2 ); 
     (d) R 4  is hydrogen, C 1-10  alkyl, C 1-10  alkyl optionally substituted with a lower alkyl, alkoxy or halogen, C 1-10  haloalkyl, C 3-10  cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; 
     (e) R 5  is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower alkyl, i.e., —(CH 2 ) p OH, where p is 1-6, including hydroxyl methyl (CH 2 OH), CH 2 F, N 3 , CH 2 CN, CH 2 NH 2 , CH 2 NHCH 3 , CH 2 N(CH 3 ) 2 , alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R 6  is H, R 5  cannot be N 3  and when X is OH, R is CH 3  or CH 2 F and B is a purine base, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OMe, halogen, NH 2 , or N 3 , 
     (h) Y is OH, H, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, vinyl, N 3 , CN, Cl, Br, F, I, NO 2 , OC(O)O(C 1-4  alkyl), OC(O)O(C 2-4  alkynyl), OC(O)O(C 2-4  alkenyl), OC 1-10  haloalkyl, O(aminoacyl), O(C 1-10  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4 alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-4  acyl) 2 , wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N 3 , CN, one to three halogen (Cl, Br, F, I), NO 2 , C(O)O(C 1-4  alkyl), C(O)O(C 1-4  alkyl), C(O)O(C 2-4  alkynyl), C(O)O(C 2-4  alkenyl), O(C 1-4  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-4  acyl) 2 ; 
     (i) R 10  is H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 2 ; and 
     R 12  is H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′; with the proviso that when base is represented by the structure c with R 11  being hydrogen, R 12  is not a: (i) —C≡C—H, (ii) —C═CH 2 , or (iii) —NO 2 . 
     A seventh aspect of the fourth embodiment is directed to a compound represented by formula I-8 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, CN, CH 3 , OCH 3 , CH 2 OH, CH 2 F, halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R′ cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OCH 3 , halogen, NH 2 , or N 3 ; 
     (h) Y is OH, H, CH 3 , vinyl, NH 2 , N 3 , CN, Cl, Br, F, I, OC(O)CH 3 , OCH 3 ; 
     (i) R 10  is H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 12 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , N 02 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′; with the proviso that R 12  is not a: (i) —C≡C—H, (ii) —C═CH 2 , or (iii) —NO 2 . 
     An eighth aspect of the fourth embodiment is directed to a compound represented by formula I-8 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, i-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n  Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, CN, CH 2 F, F, Cl, Br, or I, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, F, OCH 3 , F, Cl, Br, I, NH 2  or N 3 ; 
     (h) Y is H, OH, CH 3 , F, Cl, Br, I, NH 2  or N 3 , OCH 3 , or OC(O)CH 3 ; 
     (i) R 10  is H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 2 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , NO 2 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′; with the proviso that R′ is not a: (i) —C≡C—H, (ii) —C═CH 2 , or (iii) —NO 2 . 
     A ninth aspect of the fourth embodiment is directed to a compound represented by formula I-8 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, i-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, NH 2  or N 3 ; 
     (h) Y is OH, NH 2 , OCH 3 , or OC(O)CH 3 ; 
     (i) R 10  is H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 12 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , N 02 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′; with the proviso that R 12  is not a: (i) —C≡C—H, (ii) —C═CH 2 , or (iii) —NO 2 . 
     A tenth aspect of the fourth embodiment is directed to a compound represented by formula I-8 
     wherein 
     (a) R 1  is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl, 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, NH 2  or N 3 ; 
     (h) Y is OH, NH 2 , OCH 3 , or OC(O)CH 3 ; 
     (i) R 10  is H, F, Br, I, OH, OR′, NH 2 , NHR′, NR′ 2 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′, 
     wherein R′ is a lower alkyl, a lower cycloalkyl, or C(O)(lower alkyl) or alternatively, in the instance of NR′ 2 , each R′ comprise at least one C atom that are joined to form a heterocycle comprising at least two carbon atoms; and 
     (j) Z is N or CR 2 ; and 
     R 12  is an H, halogen (including F, Cl, Br, I), OR′, NH 2 , NHR′, NR′ 2 , N 02 , lower alkyl of C 1 -C 6 , CO 2 R′, CONH 2 , CONHR′, CONR′ 2 , CH═CHCO 2 H, or CH═CHCO 2 R′; with the proviso that R′ is not a: (i) —C≡C—H, (ii) —C═CH 2 , or (iii) —NO 2 . 
     A fifth embodiment of the invention is directed to a compound represented by formula I in which the base is a structure represented by formula d above, wherein R, R 2 , R 3a , R 3b , R 4 , R 5 , R 6 , X, and Y are defined in the Summary of the Invention section above. 
     The first aspect of the fifth embodiment is directed to a compound represented by formula I-9 
     
       
         
         
             
             
         
       
     
     wherein 
     (a) R′ is hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, which includes, but is not limited to, phenyl or naphthyl, where phenyl or naphthyl are optionally substituted with at least one of C 1-6  alkyl, C 2-6  alkenyl, C 2-6  alkynyl, C 1-6  alkoxy, F, Cl, Br, I, nitro, cyano, C 1-6  haloalkyl, —N(R 1′ ) 2 , C 1-6  acylamino, —NHSO 2 C 1-6  alkyl, —SO 2 N(R 1′ ) 2 , COR 1″ , and —SO 2 C 1-6  alkyl; (R 1′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 1″  is —OR′ or —N(R 1′ ) 2 ); 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  and R 3b  are (i) independently selected from hydrogen, C 1-10  alkyl, cycloalkyl, —(CH 2 ) c (NR 3′ ) 2 , C 1-6  hydroxyalkyl, —CH 2 SH, —(CH 2 ) 2 S(O) d Me, —(CH 2 ) 3 NHC(═NH)NH 2 , (1H-indol-3-yl)methyl, (1H-imidazol-4-yl)methyl, —(CH 2 ) e COR 3″ , aryl and aryl C 1-3  alkyl, said aryl groups optionally substituted with a group selected from hydroxyl, C 1-10  alkyl, C 1-6  alkoxy, halogen, nitro and cyano; (ii) R 3a  and R 3b  both are C 1-6  alkyl; (iii) R 3a  and R 3b  together are (CH 2 ) so as to form a spiro ring; (iv) R 3a  is hydrogen and R 3b  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms (v) R 3b  is hydrogen and R 3a  and R 2  together are (CH 2 ) n  so as to form a cyclic ring that includes the adjoining N and C atoms, where c is 1 to 6, d is 0 to 2, e is 0 to 3, f is 2 to 5, n is 2 to 4, and where R 3′  is independently hydrogen or C 1-6  alkyl and R 3″  is —OR′ or —N(R 3′ ) 2 ); (vi) R 3a  is H and R 3b  is H, CH 3 , CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; or (viii) R 3a  is CH 3 , —CH 2 CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH)CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl and R 3b  is H, where R 3′  is independently hydrogen or alkyl, which includes, but is not limited to, C 1-20  alkyl, C 1-10  alkyl, or C 1-6  alkyl, R 3″  is —OR′ or —N(R 3′ ) 2 ); 
     (d) R 4  is hydrogen. C 1-10  alkyl, C 1-10  alkyl optionally substituted with a lower alkyl, alkoxy or halogen, C 1-10  haloalkyl, C 3-10  cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, di(lower alkyl)amino-lower alkyl, aryl, such as phenyl, heteroaryl, such as, pyridinyl, substituted aryl, or substituted heteroaryl; 
     (e) R 5  is H, a lower alkyl, CN, vinyl, O-(lower alkyl), hydroxyl lower alkyl, i.e., —(CH 2 ) p OH, where p is 1-6, including hydroxyl methyl (CH 2 OH), CH 2 F, N 3 , CH 2 CN, CH 2 NH 2 , CH 2 NHCH 3 , CH 2 N(CH 3 ) 2 , alkyne (optionally substituted), or halogen, including F, Cl, Br, or I, with the provisos that when X is OH, base is cytosine and R 6  is H, R 5  cannot be N 3  and when X is OH, R 6  is CH 3  or CH 2 F and B is a purine base, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OMe, halogen, NH 2 , or N 3 ; 
     (h) Y is OH, H, C 1-4  alkyl, C 2-4  alkenyl, C 2-4  alkynyl, vinyl, N 3 , CN, Cl, Br, F, I, NO 2 , OC(O)O(C 1-4  alkyl), OC(O)O(C 1-4  alkyl), OC(O)O(C 2-4  alkynyl), OC(O)O(C 2-4  alkenyl), OC 1-10  haloalkyl, O(aminoacyl), O(C 1-10  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-18  acyl) 2 , wherein alkyl, alkynyl, alkenyl and vinyl are optionally substituted by N 3 , CN, one to three halogen (Cl, Br, F, I), NO 2 , C(O)O(C 1-4  alkyl), C(O)O(C 1-4  alkyl), C(O)O(C 2-4  alkynyl), C(O)O(C 2-4  alkenyl), O(C 1-4  acyl), O(C 1-4  alkyl), O(C 2-4  alkenyl), S(C 1-4  acyl), S(C 1-4  alkyl), S(C 2-4  alkynyl), S(C 2-4  alkenyl), SO(C 1-4  acyl), SO(C 1-4  alkyl), SO(C 2-4  alkynyl), SO(C 2-4  alkenyl), SO 2 (C 1-4  acyl), SO 2 (C 1-4  alkyl), SO 2 (C 2-4  alkynyl), SO 2 (C 2-4  alkenyl), OS(O) 2 (C 1-4  acyl), OS(O) 2 (C 1-4  alkyl), OS(O) 2 (C 2-4  alkenyl), NH 2 , NH(C 1-4  alkyl), NH(C 2-4  alkenyl), NH(C 2-4  alkynyl), NH(C 1-4  acyl), N(C 1-4  alkyl) 2 , N(C 1-4  acyl) 2 . 
     A second aspect of the fifth embodiment is directed to a compound represented by formula I-9 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, CN, CH 3 , OCH 3 , CH 2 OH, CH 2 F, halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H. 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OCH 3 , halogen, NH 2 , or N 3 , 
     (h) Y is OH, H, CH 3 , vinyl, NH 2 , N 3 , CN, Cl, Br, F, I, OC(O)CH 3 , OCH 3 ; 
     A third aspect of the fifth embodiment is directed to a compound represented by formula I-9 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, CN, CH 2 F, F, Cl, Br, or I; with the proviso that X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, F, OCH 3 , F, Cl, Br, I, NH 2  or N 3 ; 
     (h) Y is H, OH, CH 3 , F, Cl, Br, I, NH 2  N 3 , OCH 3 , or OC(O)CH 3 ; 
     A fourth aspect of the fifth embodiment is directed to a compound represented by formula I-9 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, NH 2  or N 3 ; 
     (h) Y is OH, NH 2 , OCH 3 , or OC(O)CH 3 ; 
     A fifth aspect of the fifth embodiment is directed to a compound represented by formula I-9 
     wherein 
     (a) R 1  is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3 , is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CHM)CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, with the provisos that when X is OH, R′ is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, NH 2  or N 3 ; 
     (h) Y is OH, NH 2 , OCH 3 , or OC(O)CH 3 ; 
     A sixth aspect of the fifth embodiment is directed to a compound represented by formula I-10 
     
       
         
         
             
             
         
       
     
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, i-propyl, i-propyl, or a substituted or unsubstituted phenyl, where the substitutent of the substituted phenyl is at least one of a CH 3 , OCH 3 , F, Cl, Br, I, nitro, cyano, and a CH 3-q X q , where X is F, Cl, Br, or I, and q is 1-3; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl or R 3a  is CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl and R 3b  is H; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl: 
     (e) R 5  is H, CN, CH 3 , OCH 3 , CH 2 OH, CH 2 F, N 3 , CH 2 CN, CH 2 N 3 , CH 2 NH 2 , CH 2 NHCH 3 , CH 2 N(CH 3 ) 2 , halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OCH 3 , Cl, Br, I, NH 2 , or N 3 ; 
     (h) Y is OH, H, CH 3 , vinyl, N 3 , CN, Cl, Br, F, I, OC(O)CH 3 , OCH 3 , NH 2 , NHCH 3 , NH(vinyl), NH(acetyl), NH(C(O)CH 3 ), N(CH 3 ) 2 , N(C(O)CH 3 ) 2 ; 
     A seventh aspect of the fifth embodiment is directed to a compound represented by formula I-10 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, CH 2 -indol-3-yl, —CH 2 CH 2 SCH 3 , CH 2 CO 2 H, CH 2 C(O)NH 2 , CH 2 CH 2 COOH, CH 2 CH 2 C(O)NH 2 , CH 2 CH 2 CH 2 CH 2 NH 2 , —CH 2 CH 2 CH 2 NHC(NH)NH 2 , CH 2 -imidazol-4-yl, CH 2 OH, CH(OH)CH 3 , CH 2 ((4′-OH)-Ph), CH 2 SH, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, CN, CH 3 , OCH 3 , CH 2 OH, CH 2 F, halogen, including F, Cl, Br, or I, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , F, or CN; 
     (g) X is H, OH, F, OCH 3 , Cl, Br, I, NH 2 , or N 3 ; and 
     (h) Y is OH, H, CH 3 , vinyl, NH 2 , N 3 , CN, Cl, Br, F, I, OC(O)CH 3 , OCH 3 . 
     An eighth aspect of the fifth embodiment is directed to a compound represented by formula I-10 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen or CH 3 ; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CHM)CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, CN, CH 2 F, F, Cl, Br, or I, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, F, OCH 3 , F, Cl, Br, I, NH 2  or N 3 ; 
     (h) Y is H, OH, CH 3 , F, Cl, Br, I, NH 2  or N 3 , OCH 3 , or OC(O)CH 3 ; 
     A ninth aspect of the fifth embodiment is directed to a compound represented by formula I-10 
     wherein 
     (a) R 1  is hydrogen, methyl, ethyl, i-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, NH 2  or N 3 ; 
     (h) Y is OH, NH 2 , OCH 3 , or OC(O)CH 3 ; 
     A tenth aspect of the fifth embodiment is directed to a compound represented by formula I-10 
     wherein 
     (a) R 1  is hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl; 
     (b) R 2  is hydrogen; 
     (c) R 3a  is H and R 3b  is H, CH 3 , CH(CH 3 ) 2 , CH 2 CH(CH 3 ) 2 , CH(CH 3 )CH 2 CH 3 , CH 2 Ph, or lower cycloalkyl; 
     (d) R 4  is hydrogen, CH 3 , Et,  i Pr,  n Pr,  n Bu, 2-butyl,  t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di(lower alkyl)amino-lower alkyl; 
     (e) R 5  is H, with the provisos that when X is OH, R 6  is CH 3  or CH 2 F, R 5  cannot be H; 
     (f) R 6  is H, CH 3 , CH 2 F, CHF 2 , CF 3 , or F; 
     (g) X is H, OH, OCH 3 , F, NH 2  or N 3 ; 
     (h) Y is OH, NH 2 , OCH 3 , or OC(O)CH 3 . 
     The following tables contain numeric identifiers associated with various substituent designators that should be viewed in light of the accompanying structure. These structures are contemplated species of the various aspects of the disclosed embodiments and are not intended to be limiting on full breadth of the contemplated compound represented by the structure of formula I. However, it is contemplated that any one of the exemplified nucleoside bases can be used in combination with any one of contemplated species that specify a particular combination of R 1 , R 2 , R 3a , R 3b , R 4 , R 5 , R 6 , X, and Y. In each of the presented tables, the phosphoramidate substituent containing the substituents R 3a  and R 3  are depicted without reference to stereochemical structure (cf structures I-1, I-3, I-5, I-7, and I-9 above). It is contemplated that the compounds recited below embody compounds in which R 3a  projects toward the viewer while R 3b  projects away from the viewer (cf. structures I-2, I-4, I-6, I-8, and I-10). Moreover, it is contemplated that the compounds recited below also embody compounds in which R 3a  projects away from the viewer while R 3b  projects towards the viewer. Not meant to be limiting, however, it is contemplated that preferred compounds are those in which R 3a  projects towards the viewer and R 3b  projects away from the viewer such that the natural L-amino acid (S)-configuration is presented. Additionally, the inventors recognize that the phosphorus atom of the phosphoramidate moiety is another source of chirality. Although the structures below do not specifically depict chirality at phosphorus, the inventors recognize that stereochemical configurations are possible such that in a staggered (or zig-zag) line structure the oxo-substitutent projects towards the viewer while the OR 1  substitutent projects away from the viewer, and vice versa, i.e., where the Cahn-Ingold-Prelog stereochemical designation of phosphorous is either R or S. Therefore, the structures below include all possible stereochemical configurations possible for phosphorus. 
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-24 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-25 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-26 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-27 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-28 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-29 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-30 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-31 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-32 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-33 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-34 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-35 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-36 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-39-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-42 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-43-1 
                   i Pr  
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-43-2 
                   i Pr  
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-43-3 
                   i Pr  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-43-4 
                   i Pr  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-43-5 
                   i Pr  
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-43-6 
                   i Pr  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-43-7 
                   i Pr  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-43-8 
                   i Pr  
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 II-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 II-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b    
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8    
                 R 9   
               
               
                   
               
             
            
               
                 III-17-1 
                 p-F—Ph 
                 H  
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b    
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8    
                 R 9   
               
               
                   
               
             
            
               
                 III-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b    
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8    
                 R 9   
               
               
                   
               
             
            
               
                 III-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-25-1 
                 Ph 
                 H  
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-39-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-42 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-47 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-47-1 
                 p-F-Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-47-2 
                 p-F-Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-47-3 
                 p-F-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-47-4 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-47-5 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-47-6 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-47-7 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-47-8 
                 p-F-Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-48 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-48-1 
                 p-Cl-Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-48-2 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-48-3 
                 p-Cl-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-48-4 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-48-5 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-48-6 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-48-7 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-48-8 
                 p-Cl-Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-49 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-49-1 
                 p-Br-Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-49-2 
                 p-Br-Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-49-3 
                 p-Br-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-49-4 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-49-5 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-49-6 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-49-7 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-49-8 
                 p-Br-Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE III-50 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 III-50-1 
                 p-I-Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-50-2 
                 p-I-Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-50-3 
                 p-I-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-50-4 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-50-5 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-50-6 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-50-7 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 III-50-8 
                 p-I-Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-1 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-2 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-3 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-4 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-5 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-6 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-6-1 
                 p-Me-Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-6-2 
                 p-Me-Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-6-3 
                 p-Me-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-6-4 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-6-5 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-6-6 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-6-7 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-6-8 
                 p-Me-Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-7 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-7-1 
                 p-F-Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-7-2 
                 p-F-Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-7-3 
                 p-F-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-7-4 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-7-6 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-7-7 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-7-8 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-7-20 
                 p-F-Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-8 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-8-1 
                 p-Cl-Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-8-2 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-8-3 
                 p-Cl-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-8-4 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-8-5 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-8-6 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-8-7 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-8-8 
                 p-Cl-Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-9 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-9-1 
                 p-Br-Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-9-2 
                 p-Br-Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-9-3 
                 p-Br-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-9-4 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-9-6 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-9-7 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-9-8 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-9-20 
                 p-Br-Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-10 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-10-1 
                 p-I-Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-10-2 
                 p-I-Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-10-3 
                 p-I-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-10-4 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-10-5 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-10-6 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-10-7 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-10-8 
                 p-I-Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-11 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-12 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y  
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-12-1 
                 Et  
                 H 
                 H 
                 H 
                 Et  
                 H 
                 F 
                 F 
                 OH  
                 H 
                 H 
                 NH 2   
               
               
                 IV-12-2 
                 Et  
                 H 
                 H 
                 CH 3   
                 Et  
                 H 
                 F 
                 F 
                 OH  
                 H 
                 H 
                 NH 2   
               
               
                 IV-12-3 
                 Et  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et  
                 H 
                 F 
                 F 
                 OH  
                 H 
                 H 
                 NH 2   
               
               
                 IV-12-4 
                 Et  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et  
                 H 
                 F 
                 F 
                 OH  
                 H 
                 H 
                 NH 2   
               
               
                 IV-12-5 
                 Et  
                 H 
                 H 
                 CH 2 Ph 
                 Et  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-12-6 
                 Et  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et  
                 H 
                 F 
                 F 
                 OH  
                 H 
                 H 
                 NH 2   
               
               
                 IV-12-7 
                 Et  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et  
                 H 
                 F 
                 F 
                 OH  
                 H 
                 H 
                 NH 2   
               
               
                 IV-12-8 
                 Et  
                 * 
                 H 
                 * 
                 Et  
                 H 
                 F 
                 F 
                 OH  
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-14 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a    
                 R 3b   
                 R 4    
                 R 5    
                 R 6    
                 X  
                 Y  
                 R 7   
                 R 8    
                 R 9   
               
               
                   
               
             
            
               
                 IV-14-1  
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F  
                 F  
                 OH  
                 H  
                 H  
                 NH 2   
               
               
                 IV-14-2  
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F  
                 F  
                 OH  
                 H  
                 H  
                 NH 2   
               
               
                 IV-14-3  
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F  
                 F  
                 OH  
                 H  
                 H  
                 NH 2   
               
               
                 IV-14-4  
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2    
                 Et 
                 H 
                 F  
                 F  
                 OH  
                 H  
                 H  
                 NH 2   
               
               
                 IV-14-5  
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F  
                 F  
                 OH  
                 H  
                 H  
                 NH 2   
               
               
                 IV-14-6  
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl  
                 Et 
                 H 
                 F  
                 F  
                 OH  
                 H  
                 H  
                 NH 2   
               
               
                 IV-14-7  
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3    
                 Et 
                 H 
                 F  
                 F  
                 OH  
                 H  
                 H  
                 NH 2   
               
               
                 IV-14-8  
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F  
                 F  
                 OH  
                 H  
                 H  
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7    
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-16-1 
                 p-Me—Ph 
                 H  
                 H 
                 H 
                 Et  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-16-2 
                 p-Me—Ph 
                 H  
                 H 
                 CH 3   
                 Et  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-16-3 
                 p-Me—Ph 
                 H  
                 H 
                 CH(CH 3 ) 2   
                 Et  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-16-4 
                 p-Me—Ph 
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-16-5 
                 p-Me—Ph 
                 H  
                 H 
                 CH 2 Ph 
                 Et  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-16-6 
                 p-Me—Ph 
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 Et  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-16-7 
                 p-Me—Ph 
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 Et  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-16-8 
                 p-Me—Ph 
                 *  
                 H 
                 * 
                 Et  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-18-1 
                 p-Cl—Ph  
                 H 
                 H 
                 H 
                 Et 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-18-2 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 3   
                 Et 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-18-3 
                 p-Cl—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-18-4 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2    
                 Et 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-18-5 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-18-6 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl  
                 Et 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-18-7 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-18-8 
                 p-Cl—Ph  
                 * 
                 H 
                 * 
                 Et 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-19-1 
                 p-Br—Ph 
                 H  
                 H 
                 H 
                 Et 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-19-2 
                 p-Br—Ph 
                 H  
                 H 
                 CH 3   
                 Et 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-19-3 
                 p-Br—Ph 
                 H  
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-19-4 
                 p-Br—Ph 
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-19-5 
                 p-Br—Ph 
                 H  
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-19-6 
                 p-Br—Ph 
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-19-7 
                 p-Br—Ph 
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-19-8 
                 p-Br—Ph 
                 *  
                 H 
                 * 
                 Et 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6    
                 X  
                 Y 
                 R 7    
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-20-1 
                 p-I—Ph  
                 H 
                 H 
                 H 
                 Et 
                 H  
                 F  
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H  
                 F  
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-20-4 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H  
                 F  
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-20-6 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-20-7 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H  
                 F  
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-20-8 
                 p-I—Ph  
                 *  
                 H 
                 * 
                 Et 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H  
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H  
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H  
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl  
                   i Pr 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3    
                   i Pr 
                 H  
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-22 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8    
                 R 9   
               
               
                   
               
             
            
               
                 IV-22-1 
                 Et  
                 H 
                 H 
                 H 
                   i Pr  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-22-2 
                 Et  
                 H 
                 H 
                 CH 3   
                   i Pr  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-22-3 
                 Et  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H  
                 NH 2   
               
               
                 IV-22-4 
                 Et  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H  
                 NH 2   
               
               
                 IV-22-5 
                 Et  
                 H 
                 H 
                 CH 2 Ph 
                   i Pr  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H  
                 NH 2   
               
               
                 IV-22-6 
                 Et  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H  
                 NH 2   
               
               
                 IV-22-7 
                 Et  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H  
                 NH 2   
               
               
                 IV-22-8 
                 Et  
                 * 
                 H 
                 * 
                   i Pr  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H  
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7    
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F  
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 IV-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F  
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 IV-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F  
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 IV-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2    
                   i Pr 
                 H 
                 F 
                 F  
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 IV-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F  
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 IV-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl  
                   i Pr 
                 H 
                 F 
                 F  
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 IV-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 IV-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-25 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7    
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-25-1 
                 Ph  
                 H 
                 H 
                 H 
                   i Pr  
                 H 
                 F  
                 F  
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 IV-25-2 
                 Ph  
                 H 
                 H 
                 CH 3   
                   i Pr  
                 H 
                 F  
                 F  
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 IV-25-3 
                 Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F  
                 F  
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 IV-25-4 
                 Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr  
                 H 
                 F  
                 F  
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 IV-25-5 
                 Ph  
                 H 
                 H 
                 CH 2 Ph 
                   i Pr  
                 H 
                 F  
                 F  
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 IV-25-6 
                 Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr  
                 H 
                 F  
                 F  
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 IV-25-7 
                 Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr  
                 H 
                 F  
                 F  
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 IV-25-8 
                 Ph  
                 * 
                 H 
                 * 
                   i Pr  
                 H 
                 F  
                 F  
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-26-1 
                 p-Me—Ph 
                 H  
                 H 
                 H 
                   i Pr  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-26-2 
                 p-Me—Ph 
                 H  
                 H 
                 CH 3   
                   i Pr  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-26-3 
                 p-Me—Ph 
                 H  
                 H 
                 CH(CH 3 ) 2   
                   i Pr  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-26-4 
                 p-Me—Ph 
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-26-5 
                 p-Me—Ph 
                 H  
                 H 
                 CH 2 Ph 
                   i Pr  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-26-6 
                 p-Me—Ph 
                 H  
                 H 
                 CH 2 -indol-3-yl 
                   i Pr  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-26-7 
                 p-Me—Ph 
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-26-8 
                 p-Me—Ph 
                 *  
                 H 
                 * 
                   i Pr  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7    
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-28-1 
                 p-Cl—Ph  
                 H  
                 H 
                 H 
                   i Pr  
                 H 
                 F 
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-28-2 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 3   
                   i Pr  
                 H 
                 F 
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-28-3 
                 p-Cl—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-28-4 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-28-5 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 Ph 
                   i Pr  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-28-6 
                 p-Cl—Ph  
                 H  
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-28-7 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-28-8 
                 p-Cl—Ph  
                 * 
                 H 
                 * 
                   i Pr  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-30-1 
                 p-I—Ph  
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F  
                 F 
                 OH  
                 H 
                 H 
                 NH 2   
               
               
                 IV-30-2 
                 p-I—Ph  
                 H 
                 H 
                 CH 3    
                   i Pr 
                 H  
                 F  
                 F 
                 OH  
                 H 
                 H 
                 NH 2   
               
               
                 IV-30-3 
                 p-I—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2    
                   i Pr 
                 H 
                 F  
                 F 
                 OH  
                 H 
                 H 
                 NH 2   
               
               
                 IV-30-4 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2    
                   i Pr 
                 H  
                 F  
                 F 
                 OH  
                 H 
                 H 
                 NH 2   
               
               
                 IV-30-5 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F  
                 F 
                 OH  
                 H 
                 H 
                 NH 2   
               
               
                 IV-30-6 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl  
                   i Pr 
                 H  
                 F  
                 F 
                 OH  
                 H 
                 H 
                 NH 2   
               
               
                 IV-30-7 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3    
                   i Pr 
                 H 
                 F  
                 F 
                 OH  
                 H 
                 H 
                 NH 2   
               
               
                 IV-30-8 
                 p-I—Ph  
                 * 
                 H 
                 * 
                   i Pr 
                 H  
                 F  
                 F 
                 OH  
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7    
                 R 8    
                 R 9   
               
               
                   
               
             
            
               
                 IV-32-1 
                 Et  
                 H 
                 H 
                 H 
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-32-2 
                 Et  
                 H 
                 H 
                 CH 3   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-32-3 
                 Et  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-32-4 
                 Et  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-32-5 
                 Et  
                 H 
                 H 
                 CH 2 Ph 
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-32-6 
                 Et  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-32-7 
                 Et  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-32-8 
                 Et  
                 * 
                 H 
                 * 
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-33 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-33-1 
                   i Pr  
                 H 
                 H 
                 H 
                   n Bu 
                 H  
                 F 
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-33-2 
                   i Pr  
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H  
                 F  
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-33-3 
                   i Pr  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H  
                 F  
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-33-4 
                   i Pr  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-33-5 
                   i Pr  
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-33-6 
                   i Pr  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-33-7 
                   i Pr  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-33-8 
                   i Pr  
                 * 
                 H 
                 * 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-37-1 
                 p-F—Ph 
                 H  
                 H 
                 H 
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-37-2 
                 p-F—Ph 
                 H  
                 H 
                 CH 3   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-37-3 
                 p-F—Ph 
                 H  
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-37-4 
                 p-F—Ph 
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-37-5 
                 p-F—Ph 
                 H  
                 H 
                 CH 2 Ph 
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-37-6 
                 p-F—Ph 
                 H  
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-37-7 
                 p-F—Ph 
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-37-8 
                 p-F—Ph 
                 *  
                 H 
                 * 
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-38-1 
                 p-Cl—Ph  
                 H  
                 H 
                 H 
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-38-2 
                 p-Cl—Ph  
                 H  
                 H 
                 CH 3   
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-38-3 
                 p-Cl—Ph  
                 H  
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-38-4 
                 p-Cl—Ph  
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-38-5 
                 p-Cl—Ph  
                 H  
                 H 
                 CH 2 Ph 
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-38-6 
                 p-Cl—Ph  
                 H  
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-38-7 
                 p-Cl—Ph  
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-38-8 
                 p-Cl—Ph  
                 * 
                 H 
                 * 
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-39-1 
                 p-Br—Ph 
                 H  
                 H 
                 H 
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-39-2 
                 p-Br—Ph 
                 H  
                 H 
                 CH 3   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-39-3 
                 p-Br—Ph 
                 H  
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-39-4 
                 p-Br—Ph 
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-39-5 
                 p-Br—Ph 
                 H  
                 H 
                 CH 2 Ph 
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-39-6 
                 p-Br—Ph 
                 H  
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-39-7 
                 p-Br—Ph 
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-39-8 
                 p-Br—Ph 
                 *  
                 H 
                 * 
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-40-1 
                 p-I—Ph  
                 H 
                 H 
                 H 
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-40-2 
                 p-I—Ph  
                 H 
                 H 
                 CH 3   
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-40-3 
                 p-I—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 F  
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-40-4 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-40-5 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 Ph 
                   n Bu  
                 H 
                 F  
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-40-6 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-40-7 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H 
                 F  
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-40-8 
                 p-I—Ph  
                 * 
                 H 
                 * 
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-42 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-43 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y  
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-43-1 
                   i Pr  
                 H  
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-43-2 
                   i Pr  
                 H  
                 H 
                 CH 3   
                 Bz  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-43-3 
                   i Pr  
                 H  
                 H 
                 CH(CH 3 ) 2   
                 Bz  
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-43-4 
                   i Pr  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz  
                 H 
                 F 
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-43-5 
                   i Pr  
                 H  
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-43-6 
                   i Pr  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz  
                 H 
                 F 
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-43-7 
                   i Pr  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz  
                 H 
                 F 
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-43-8 
                   i Pr  
                 * 
                 H 
                 * 
                 Bz  
                 H 
                 F 
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7    
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-45-1 
                 Ph  
                 H  
                 H 
                 H 
                 Bz  
                 H 
                 F 
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-45-2 
                 Ph  
                 H  
                 H 
                 CH 3   
                 Bz  
                 H 
                 F 
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-45-3 
                 Ph  
                 H  
                 H 
                 CH(CH 3 ) 2   
                 Bz  
                 H 
                 F 
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-45-4 
                 Ph  
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz  
                 H 
                 F 
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-45-5 
                 Ph  
                 H  
                 H 
                 CH 2 Ph 
                 Bz  
                 H 
                 F 
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-45-6 
                 Ph  
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 Bz  
                 H 
                 F 
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-45-7 
                 Ph 
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz  
                 H 
                 F 
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-45-8 
                 Ph  
                 * 
                 H 
                 * 
                 Bz  
                 H 
                 F 
                 F  
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-46-1 
                 p-Me—Ph 
                 H  
                 H 
                 H 
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-46-2 
                 p-Me—Ph 
                 H  
                 H 
                 CH 3   
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-46-3 
                 p-Me—Ph 
                 H  
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-46-4 
                 p-Me—Ph 
                 H  
                 H 
                 CH 3 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-46-5 
                 p-Me—Ph 
                 H  
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-46-6 
                 p-Me—Ph 
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-46-7 
                 p-Me—Ph 
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-46-8 
                 p-Me—Ph 
                 *  
                 H 
                 * 
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-48-1 
                 p-Cl—Ph  
                 H  
                 H 
                 H 
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-48-2 
                 p-Cl—Ph  
                 H  
                 H 
                 CH 3   
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-48-3 
                 p-Cl—Ph  
                 H  
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-48-4 
                 p-Cl—Ph  
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-48-5 
                 p-Cl—Ph  
                 H  
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-48-6 
                 p-Cl—Ph 
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-48-7 
                 p-Cl—Ph  
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-48-8 
                 p-Cl—Ph  
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IV-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 IV-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 IV-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 H  
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H  
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H  
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H  
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H  
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H  
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H  
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H  
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-2-3 
                 Et  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-2-4 
                 Et  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-2-8 
                 Et  
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7    
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-4-1 
                   t Bu  
                 H  
                 H 
                 H 
                 CH 3    
                 H 
                 H  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-4-2 
                   t Bu  
                 H  
                 H 
                 CH 3   
                 CH 3    
                 H 
                 H  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-4-3 
                   t Bu  
                 H  
                 H 
                 CH(CH 3 ) 2   
                 CH 3    
                 H 
                 H  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-4-4 
                   t Bu  
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3    
                 H 
                 H  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-4-5 
                   t Bu 
                 H  
                 H 
                 CH 2 Ph 
                 CH 3    
                 H 
                 H  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-4-6 
                   t Bu  
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 CH 3    
                 H 
                 H  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-4-7 
                   t Bu 
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3    
                 H 
                 H  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-4-8 
                   t Bu  
                 *  
                 H 
                 * 
                 CH 3    
                 H 
                 H  
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7    
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-5-1 
                 Ph  
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-5-2 
                 Ph  
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-5-3 
                 Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-5-4 
                 Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-5-5 
                 Ph  
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-5-6 
                 Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-5-7 
                 Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-5-8 
                 Ph  
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-13 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 (CH 3 ) 2   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol- 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 3-yl 
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 SCH 3   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 (CH 3 ) 2   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol- 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 3-yl 
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 SCH 3   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 (CH 3 ) 2   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol- 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 3-yl 
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 SCH 3   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 (CH 3 ) 2   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol- 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 3-yl 
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 SCH 3   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-28-1 
                 p-Cl—Ph 
                 PhH 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-29 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-31-3 
                 CH 3   
                 H 
                 H 
                 CH 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 (CH 3 ) 2   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 (CH 3 ) 2   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 - 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 indol- 
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                   
                   
                   
                   
                 3-yl 
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 SCH 3   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 (CH 3 ) 2   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol- 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 3-yl 
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 SCH 3   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 (CH 3 ) 2   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol- 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 3-yl 
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 SCH 3   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 (CH 3 ) 2   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol- 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 3-yl 
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 SCH 3   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 (CH 3 ) 2   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol- 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 3-yl 
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
                   
                   
                   
                 SCH 3   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 V-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-37 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-37-1 
                 p-F-Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-37-2 
                 p-F-Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-37-3 
                 p-F-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-37-4 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-37-5 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-37-6 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-37-7 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-37-8 
                 p-F-Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-38 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-38-1 
                 p-Cl-Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-38-2 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-38-3 
                 p-Cl-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-38-4 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-38-5 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-38-6 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-38-7 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-38-8 
                 p-Cl-Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-39 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-39-1 
                 p-Br-Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-39-2 
                 p-Br-Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-39-3 
                 p-Br-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-39-4 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-39-5 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-39-6 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-39-7 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-39-8 
                 p-Br-Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-40 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-40-1 
                 p-I-Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-40-2 
                 p-I-Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-40-3 
                 p-I-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-40-4 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-40-5 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-40-6 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-40-7 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-40-8 
                 p-I-Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-41 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-42 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-43 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-44 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-45 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-45-1 
                 Ph  
                 H 
                 H 
                 H 
                 Bz 
                 H  
                 H 
                 F 
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 V-45-2 
                 Ph  
                 H 
                 H 
                 CH 3   
                 Bz 
                 H  
                 H 
                 F 
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 V-45-3 
                 Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H  
                 H 
                 F 
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 V-45-4 
                 Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H  
                 H 
                 F 
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 V-45-5 
                 Ph  
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H  
                 H 
                 F 
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 V-45-6 
                 Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H  
                 H 
                 F 
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 V-45-7 
                 Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H  
                 H 
                 F 
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                 V-45-8 
                 Ph  
                 * 
                 H 
                 * 
                 Bz 
                 H  
                 H 
                 F 
                 OH 
                 H  
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-46 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-46-1 
                 p-Me-Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-46-2 
                 p-Me-Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-46-3 
                 p-Me-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-46-4 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-46-5 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-46-6 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-46-7 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-46-8 
                 p-Me-Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H  
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-47 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-47-1 
                 p-F-Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-47-2 
                 p-F-Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-47-3 
                 p-F-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-47-4 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-47-5 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-47-6 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-47-7 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-47-8 
                 p-F-Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-48 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-48-1 
                 p-Cl-Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-48-2 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-48-3 
                 p-Cl-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-48-4 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-48-5 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-48-6 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-48-7 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-48-8 
                 p-Cl-Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-49 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-49-1 
                 p-Br-Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-49-2 
                 p-Br-Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-49-3 
                 p-Br-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-49-4 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-49-5 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-49-6 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-49-7 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-49-8 
                 p-Br-Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE V-50 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 V-50-1 
                 p-I-Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-50-2 
                 p-I-Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-50-3 
                 p-I-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-50-4 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-50-5 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-50-6 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-50-7 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 V-50-8 
                 p-I-Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-1 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 V1-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 FI 
                 OH 
                 H 
                 H 
               
               
                 VI-6-6 
                 p-Me—Ph 
                 II 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 V1-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H H 
                 H 
               
               
                 VI-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H H 
                 H 
               
               
                 VI-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H H 
                 H 
               
               
                 VI-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H H 
                 H 
               
               
                 VI-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H H 
                 H 
               
               
                 VI-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H H 
                 H 
               
               
                 VI-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H H 
                 H 
               
               
                 VI-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-24 
               
               
                   
               
               
                 No 
                 R 1   
                 r2  
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R4  
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-26-8 
                 p-Me—Ph  
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a    
                 R 3b   
                 R 4   
                 R 5    
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-33-8 
                   i Pr 
                 *  
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-35 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-39-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-42 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 Vl-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VI-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VI-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 VI-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 FI 
                 NH 2   
               
               
                 VII-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-12 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-13 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2 and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-14 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-15 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-16 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-16-1 
                 p-Me-Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-16-2 
                 p-Me-Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-16-3 
                 p-Me-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-16-4 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-16-5 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-16-6 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-16-7 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-16-8 
                 p-Me-Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-17 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-17-1 
                 p-F-Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-17-2 
                 p-F-Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-17-3 
                 p-F-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-17-4 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-17-5 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-17-6 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-17-7 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-17-8 
                 p-F-Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-18 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-18-1 
                 p-Cl-Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-18-2 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-18-3 
                 p-Cl-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-18-4 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-18-5 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-18-6 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-18-7 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-18-8 
                 p-Cl-Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-19 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-19-1 
                 p-Br-Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-19-2 
                 p-Br-Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-19-3 
                 p-Br-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-19-4 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-19-5 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-19-6 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-19-7 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-19-8 
                 p-Br-Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-20 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-20-1 
                 p-I-Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-20-2 
                 p-I-Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-20-3 
                 p-I-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-20-4 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-20-5 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-20-6 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-20-7 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-20-8 
                 p-I-Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-21 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2 and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-22 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-23 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-24 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-25 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-26 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-26-1 
                 p-Me-Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VIl-26-2 
                 p-Me-Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-26-3 
                 p-Me-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-26-4 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-26-5 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-26-6 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-26-7 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-26-8 
                 p-Me-Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 II 
                 H 
                 NH 2   
               
               
                 VII-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 II 
                 NH 2   
               
               
                 VII-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OFI 
                 H 
                 H 
                 NH 2   
               
               
                 VII-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 FI 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 II 
                 NH 2   
               
               
                 VII-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-39-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-40-8 
                 p-I—Ph 
                 H 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-42 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R4 
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7    
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VII-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
                 R 9   
               
               
                   
               
             
            
               
                 VII-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                 VII-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
                 H 
                 H 
                 NH 2   
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-1 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-9-7 
                 p-Br—Ph 
                 II 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-18-8 
                 p-Cl—Ph  
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et  
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-19-8 
                 p-Br—Ph 
                 H 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-39-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-42 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-48-8 
                 p-Cl—Ph  
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE VIII-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 VIII-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                 VIII-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 OH 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-12-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-12-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-12-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-12-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-12-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-12-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-12-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-12-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-15-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-15-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-15-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-15-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-15-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-15-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-15-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-15-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-17 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 IX-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-18 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 IX-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-18-8 
                 p-Cl—Ph 
                 *  
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-19 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 IX-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-20 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 IX-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-21 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 IX-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr  
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr  
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr  
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr  
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr  
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr  
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr  
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr  
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-24 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-26 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 IX-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-27 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 IX-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-28 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7    
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 IX-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-29 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 IX-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-30 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 IX-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-31 
               
               
                   
               
               
                   
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 IX-31-1 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-31-2 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-31-3 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-31-7 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 IX-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-32 
               
               
                   
               
               
                 No 
                   
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-32-1 
                   
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-32-2 
                   
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-32-3 
                   
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-32-4 
                   
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-32-5 
                   
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-32-6 
                   
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-32-7 
                   
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-32-8 
                   
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-33 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-34 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-35 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-36 
               
               
                   
               
               
                 No 
                   
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-36-1 
                   
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-36-2 
                   
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-36-3 
                   
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-36-4 
                   
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-36-5 
                   
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-36-6 
                   
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-36-7 
                   
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-36-8 
                   
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-37 
               
               
                   
               
               
                 No 
                   
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-37-1 
                   
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-37-2 
                   
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-37-3 
                   
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-37-4 
                   
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-37-5 
                   
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-37-6 
                   
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-37-7 
                   
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-37-8 
                   
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-38 
               
               
                   
               
               
                 No 
                   
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-38-1 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-38-2 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-38-3 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-38-4 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-38-5 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-38-6 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-38-7 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-38-8 
                   
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-39 
               
               
                   
               
               
                 No 
                   
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-39-1 
                   
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-39-2 
                   
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-39-3 
                   
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-39-4 
                   
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-39-5 
                   
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-39-6 
                   
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-39-7 
                   
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-39-8 
                   
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-40 
               
               
                   
               
               
                 No 
                   
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-40-1 
                   
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-40-2 
                   
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-40-3 
                   
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-40-4 
                   
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-40-5 
                   
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-40-6 
                   
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-40-7 
                   
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-40-8 
                   
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-41 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX- 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 41-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 IX- 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 41-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 IX- 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 41-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 IX- 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 41-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 IX- 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 41-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 IX- 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 41-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 IX- 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 41-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 IX- 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 41-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-42 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-43 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-44 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-45 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-46 
               
               
                   
               
               
                 No 
                   
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-46-1 
                   
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-46-2 
                   
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-46-3 
                   
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-46-4 
                   
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-46-5 
                   
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-46-6 
                   
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-46-7 
                   
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-46-8 
                   
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-47-8 
                 p-F—Ph  
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F  
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-48-1 
                 p-Cl—Ph  
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-48-2 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-48-3 
                 p-Cl—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-48-4 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-48-5 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-48-6 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-48-7 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-48-8 
                 p-Cl—Ph  
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE IX-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 IX-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                 IX-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3    
                 H 
                 F  
                 F 
                 OH  
                 H 
                 H 
               
               
                 X-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3    
                 H 
                 F  
                 F  
                 OH  
                 H 
                 H 
               
               
                 X-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3    
                 H 
                 F  
                 F  
                 OH  
                 H 
                 H 
               
               
                 X-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3    
                 H 
                 F  
                 F  
                 OH  
                 H 
                 H 
               
               
                 X-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3    
                 H 
                 F  
                 F  
                 OH  
                 H 
                 H 
               
               
                 X-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3    
                 H 
                 F  
                 F  
                 OH  
                 H 
                 H 
               
               
                 X-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3    
                 H 
                 F  
                 F  
                 OH  
                 H 
                 H 
               
               
                 X-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3    
                 H 
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-2 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-2-1 
                 Et  
                 H 
                 H 
                 H 
                 CH 3   
                 H  
                 F 
                 F  
                 OH 
                 H 
                 H 
               
               
                 X-2-2 
                 Et  
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H  
                 F  
                 F  
                 OH 
                 H 
                 H 
               
               
                 X-2-3 
                 Et  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H  
                 F  
                 F  
                 OH 
                 H 
                 H 
               
               
                 X-2-4 
                 Et  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H  
                 F  
                 F  
                 OH 
                 H 
                 H 
               
               
                 X-2-5 
                 Et  
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H  
                 F  
                 F  
                 OH 
                 H 
                 H 
               
               
                 X-2-6 
                 Et  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H  
                 F  
                 F  
                 OH 
                 H 
                 H 
               
               
                 X-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H  
                 F  
                 F  
                 OH 
                 H 
                 H 
               
               
                 X-2-8 
                 Et  
                 * 
                 H 
                 * 
                 CH 3   
                 H  
                 F  
                 F  
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-4 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-4-6 
                   t Bu 
                 H 
                 H 
                 CH-indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-7-1  
                 p-F—Ph  
                 H 
                 H 
                 H 
                 CH 3   
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-7-2  
                 p-F—Ph 
                 H  
                 H 
                 CH 3   
                 CH 3   
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-7-3  
                 p-F—Ph  
                 H  
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-7-4  
                 p-F—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-7-6  
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-7-7  
                 p-F—Ph 
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-7-8  
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-7-20  
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
               
               
                   
               
             
            
               
                 X-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
               
               
                 X-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
               
               
                 X-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
               
               
                 X-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
               
               
                 X-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
               
               
                 X-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
               
               
                 X-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
               
               
                 X-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-27 
               
               
                   
               
               
                 No 
                   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-27-1 
                   
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-27-2 
                   
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-27-3 
                   
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-27-4 
                   
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-27-5 
                   
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-27-6 
                   
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-27-7 
                   
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-27-8 
                   
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-28 
               
               
                   
               
               
                 No 
                   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-28-1 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-28-2 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-28-3 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-28-4 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-28-5 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-28-6 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-28-7 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-28-8 
                   
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-29 
               
               
                   
               
               
                 No 
                   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-29-1 
                   
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-29-2 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-29-3 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-29-4 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-29-5 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-29-6 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-29-7 
                   
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-29-8 
                   
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-30 
               
               
                   
               
               
                 No 
                   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-30-1 
                   
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-30-2 
                   
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-30-3 
                   
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-30-4 
                   
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-30-5 
                   
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-30-6 
                   
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-30-7 
                   
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-30-8 
                   
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X- 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 36-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 X- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 36-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 X- 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 36-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 X- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 36-4 
                   
                   
                   
                 (CH 3 ) 2   
                   
                   
                   
                   
                   
                   
                   
               
               
                 X- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 36-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 X- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol- 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 36-6 
                   
                   
                   
                 3-yl 
                   
                   
                   
                   
                   
                   
                   
               
               
                 X- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 36-7 
                   
                   
                   
                 SCH 3   
                   
                   
                   
                   
                   
                   
                   
               
               
                 X- 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 36-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-37 
               
               
                   
               
               
                 No 
                 R 1   
                   
                 R 2   
                 R 3a   
                 R 3b   
                   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-37-1 
                 p-F—Ph 
                   
                 H 
                 H 
                 H 
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-37-2 
                 p-F—Ph 
                   
                 H 
                 H 
                 CH 3   
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-37-3 
                 p-F—Ph 
                   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-37-4 
                 p-F—Ph 
                   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-37-5 
                 p-F—Ph 
                   
                 H 
                 H 
                 CH 2 Ph 
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-37-6 
                 p-F—Ph 
                   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-37-7 
                 p-F—Ph 
                   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-37-8 
                 p-F—Ph 
                   
                 * 
                 H 
                 * 
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-38 
               
               
                   
               
               
                 No 
                 R 1   
                   
                 R 2   
                 R 3a   
                 R 3b   
                   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-38-1 
                 p-Cl—Ph 
                   
                 H 
                 H 
                 H 
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-38-2 
                 p-Cl—Ph 
                   
                 H 
                 H 
                 CH 3   
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-38-3 
                 p-Cl—Ph 
                   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-38-4 
                 p-Cl—Ph 
                   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-38-5 
                 p-Cl—Ph 
                   
                 H 
                 H 
                 CH 2 Ph 
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-38-6 
                 p-Cl—Ph 
                   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-38-7 
                 p-Cl—Ph 
                   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-38-8 
                 p-Cl—Ph 
                   
                 * 
                 H 
                 * 
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-39 
               
               
                   
               
               
                 No 
                 R 1   
                   
                 R 2   
                 R 3a   
                 R 3b   
                   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-39-1 
                 p-Br—Ph 
                   
                 H 
                 H 
                 H 
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-39-2 
                 p-Cl—Ph 
                   
                 H 
                 H 
                 CH 3   
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-39-3 
                 p-Cl—Ph 
                   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-39-4 
                 p-Cl—Ph 
                   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-39-5 
                 p-Cl—Ph 
                   
                 H 
                 H 
                 CH 2 Ph 
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-39-6 
                 p-Cl—Ph 
                   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-39-7 
                 p-Cl—Ph 
                   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-39-8 
                 p-Cl—Ph 
                   
                 * 
                 H 
                 * 
                   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X- 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 40-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 X- 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 40-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 X- 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 40-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 X- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 40-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 X- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 40-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 X- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol- 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 40-6 
                   
                   
                   
                 3-yl 
                   
                   
                   
                   
                   
                   
                   
               
               
                 X- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 40-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 X- 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 40-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-42 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7    
                 R 8   
               
               
                   
               
             
            
               
                 X-42-1 
                 Et  
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H  
                 H 
               
               
                 X-42-2 
                 Et  
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H  
                 H 
               
               
                 X-42-3 
                 Et  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H  
                 H 
               
               
                 X-42-4 
                 Et  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H  
                 H 
               
               
                 X-42-5 
                 Et  
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H  
                 H 
               
               
                 X-42-6 
                 Et  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H  
                 H 
               
               
                 X-42-7 
                 Et  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H  
                 H 
               
               
                 X-42-8 
                 Et  
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F  
                 F 
                 OH 
                 H  
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-46-8 
                 p-Me—Ph 
                 *  
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 X-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-2 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-2-1 
                 Et  
                 H 
                 H 
                 H 
                 CH 3    
                 H 
                 H 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XI-2-2 
                 Et  
                 H 
                 H 
                 CH 3   
                 CH 3    
                 H 
                 H 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XI-2-3 
                 Et  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3    
                 H 
                 H 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XI-2-4 
                 Et  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3    
                 H 
                 H 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XI-2-5 
                 Et  
                 H 
                 H 
                 CH 2 Ph 
                 CH 3    
                 H 
                 H 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XI-2-6 
                 Et  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3    
                 H 
                 H 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XI-2-7 
                 Et  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3    
                 H 
                 H 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XI-2-8 
                 Et  
                 * 
                 H 
                 * 
                 CH 3    
                 H 
                 H 
                 F 
                 OH 
                 H  
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-4-1 
                   t Bu 
                 H  
                 H 
                 H 
                 CH 3   
                 H  
                 H 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XI-4-2 
                   t Bu 
                 H  
                 H 
                 CH 3   
                 CH 3   
                 H  
                 H 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XI-4-3 
                   t Bu 
                 H  
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H  
                 H 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XI-4-4 
                   t Bu 
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H  
                 H 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XI-4-5 
                   t Bu 
                 H  
                 H 
                 CH 2 Ph 
                 CH 3   
                 H  
                 H 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XI-4-6 
                   t Bu 
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H  
                 H 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XI-4-7 
                   t Bu 
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H  
                 H 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XI-4-8 
                   t Bu 
                 *  
                 H 
                 * 
                 CH 3   
                 H  
                 H  
                 F 
                 OH  
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-5 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7    
                 R 8   
               
               
                   
               
             
            
               
                 XI-5-1  
                 Ph 
                 H 
                 H 
                 H 
                 CH 3    
                 H 
                 H 
                 F  
                 OH 
                 H  
                 H 
               
               
                 XI-5-2  
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3    
                 H 
                 H 
                 F  
                 OH 
                 H  
                 H 
               
               
                 XI-5-3  
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3    
                 H 
                 H 
                 F  
                 OH 
                 H  
                 H 
               
               
                 XI-5-4  
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3    
                 H 
                 H 
                 F  
                 OH 
                 H  
                 H 
               
               
                 XI-5-5  
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3    
                 H 
                 H 
                 F  
                 OH 
                 H  
                 H 
               
               
                 XI-5-6  
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F  
                 OH 
                 H  
                 H 
               
               
                 XI-5-7  
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3    
                 H 
                 H 
                 F  
                 OH 
                 H  
                 H 
               
               
                 XI-5-8  
                 Ph  
                 * 
                 H 
                 * 
                 CH 3    
                 H 
                 H 
                 F  
                 OH 
                 H  
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 Xl-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 )2 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F  
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 II 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XI-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XI-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XI-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XI-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XI-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XI-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XI-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
                 H  
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-25-1 
                 Ph  
                 H  
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
                 H  
                 H 
               
               
                 XI-25-2 
                 Ph  
                 H  
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
                 H  
                 H 
               
               
                 X1-25-3 
                 Ph  
                 H  
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
                 H  
                 H 
               
               
                 XI-25-4 
                 Ph  
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
                 H  
                 H 
               
               
                 XI-25-5 
                 Ph  
                 H  
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
                 H  
                 H 
               
               
                 XI-25-6 
                 Ph  
                 H  
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
                 H  
                 H 
               
               
                 XI-25-7 
                 Ph  
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
                 H  
                 H 
               
               
                 XI-25-8 
                 Ph  
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
                 H  
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-29-8 
                 p-Br—Ph 
                 *  
                 H 
                 * 
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 H  
                 H 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H  
                 H 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H  
                 H 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H  
                 H 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H  
                 H 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H  
                 H 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H  
                 H 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 H  
                 H 
                 F  
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H  
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H  
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H  
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H  
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H  
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H  
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H  
                 F  
                 OH 
                 H 
                 H 
               
               
                 XI-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H  
                 F  
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-39-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-42 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE X1-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XI-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XI-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XI-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII- 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 1-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XII- 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 1-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XII-  
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 1-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XII- 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 1-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XII- 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 1-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XII- 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 1-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XII- 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 1-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XII- 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 1-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a    
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-4-1  
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a    
                 R 3b   
                 R 4   
                 R 5   
                 R6  
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-5-3  
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-5-5  
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-5-7  
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7    
                 R 8   
               
               
                   
               
             
            
               
                 XII-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X1I-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X1I-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-11-1  
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-11-3  
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et  
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-11-5  
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-11-7  
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-11-8  
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7    
                 R 8   
               
               
                   
               
             
            
               
                 XII-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-12-5  
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-13-1 
                   i Pr  
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-13-2 
                   i Pr  
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-13-3 
                   i Pr  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-13-4  
                   i Pr  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-13-5 
                   i Pr  
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-13-6 
                   i Pr  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-13-7 
                   i Pr  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-13-8 
                   i Pr  
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-14-1 
                   t Bu  
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3  ) 2   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-14-6 
                   t Bu  
                 H 
                 H 
                 CH 2 -indol-3 -yl 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a    
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et  
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et  
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et  
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et  
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et  
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R4 
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
               
               
                   
               
             
            
               
                 XII-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
               
               
                 XII-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
               
               
                 XII-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
               
               
                 XII-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
               
               
                 XII-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
               
               
                 XII-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
               
               
                 XII-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
               
               
                 XII-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X1I-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-23-8 
                 &#39;Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X1I-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-35-1 
                 Ph  
                 H  
                 H 
                 H 
                   n Bu 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-35-2 
                 Ph  
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-35-3 
                 Ph  
                 H  
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-35-4 
                 Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-35-5 
                 Ph  
                 H  
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-35-6 
                 Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-35-7 
                 Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-35-8 
                 Ph  
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-39-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-41-1  
                 CH 3   
                 H  
                 H 
                 H 
                 Bz 
                 N 3   
                 F 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XII-41-2  
                 CH 3   
                 H  
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 F 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XII-41-3  
                 CH 3   
                 H  
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XII-41-4  
                 CH 3   
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-41-5  
                 CH 3   
                 H  
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XII-41-6  
                 CH 3   
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XII-41-7  
                 CH 3   
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XII-41-8  
                 CH 3   
                 *  
                 H 
                 * 
                 Bz 
                 N 3   
                 F 
                 F  
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-42 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-42-1 
                 Et  
                 H 
                 H 
                 H 
                 Bz  
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-42-2 
                 Et  
                 H 
                 H 
                 CH 3   
                 Bz  
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-42-3 
                 Et  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz  
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-42-4 
                 Et  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-42-5 
                 Et  
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-42-6 
                 Et  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-42-7 
                 Et  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-42-8 
                 Et  
                 * 
                 H 
                 * 
                 Bz  
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-45 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-45-1 
                 Ph  
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-45-2 
                 Ph  
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-45-3 
                 Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-45-4 
                 Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-45-5 
                 Ph  
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-45-6 
                 Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-45-7 
                 Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-45-8 
                 Ph  
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7    
                 R 8   
               
               
                   
               
             
            
               
                 XII-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XII-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XII-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XII-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XII-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XII-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H  
                 H 
               
               
                 XII-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 F  
                 F 
                 OH 
                 H  
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH, 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH,CH(CH 3 )2 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XII-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE II-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XII-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XII-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-12 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-13 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-14 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-15 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-16 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-16-1 
                 p-Me-Ph 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-16-2 
                 p-Me-Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-16-3 
                 p-Me-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-16-4 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-16-5 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-16-6 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-16-7 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-16-8 
                 p-Me-Ph 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-17 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-17-1 
                 p-F-Ph 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-17-2 
                 p-F-Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-17-3 
                 p-F-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-17-4 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-17-5 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-17-6 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-17-7 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-17-8 
                 p-F-Ph 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-18 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-18-1 
                 p-Cl-Ph 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-18-2 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-18-3 
                 p-Cl-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-18-4 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-18-5 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-18-6 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-18-7 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-18-8 
                 p-Cl-Ph 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-19 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-19-1 
                 p-Br-Ph 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-19-2 
                 p-Br-Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-19-3 
                 p-Br-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-19-4 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-19-5 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-19-6 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-19-7 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-19-8 
                 p-Br-Ph 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-20 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-20-1 
                 p-I-Ph 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-20-2 
                 p-I-Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-20-3 
                 p-I-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-20-4 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-20-5 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-20-6 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-20-7 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-20-8 
                 p-I-Ph 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-21 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-22 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-23 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-24 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-25 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-26 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-26-1 
                 p-Me-Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-26-2 
                 p-Me-Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-26-3 
                 p-Me-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-26-4 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-26-5 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-26-6 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-26-7 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-26-8 
                 p-Me-Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII- 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 31-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 31-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 31-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 31-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 31-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 31-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 31-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 31-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII- 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 32-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 32-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 32-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 32-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 32-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 32-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 32-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 32-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII- 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 33-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 33-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 33-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 33-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 33-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 33-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 33-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 33-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII- 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 34-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 34-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 34-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 34-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 34-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 34-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 34-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 34-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII- 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 35-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 35-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 35-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 35-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 35-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 35-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 35-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 35-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-39-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII- 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 41-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 41-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 41-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 41-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 41-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 41-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 41-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIII- 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 41-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-42 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-47-1 
                 p-F—Ph  
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-47-2 
                 p-F—Ph  
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-47-3 
                 p-F—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-47-4 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-47-5 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-47-6 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-47-7 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-47-8 
                 p-F—Ph  
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-48-8  
                 p-Cl—Ph  
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-49-1 
                 p-Br—Ph  
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-49-2 
                 p-Br—Ph  
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-49-3 
                 p-Br—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-49-4 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-49-5 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-49-6 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-49-7 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-49-8 
                 p-Br—Ph  
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIII-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIII-50-1 
                 p-I—Ph 
                 H  
                 H 
                 H 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-50-2 
                 p-I—Ph 
                 H  
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-50-3 
                 p-I—Ph 
                 H  
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-50-4 
                 p-I—Ph 
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-50-5 
                 p-I—Ph 
                 H  
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-50-6 
                 p-I—Ph 
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-50-7 
                 p-I—Ph 
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIII-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-6-1  
                 p-Me—Ph  
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-6-2 
                 p-Me—Ph  
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-6-3 
                 p-Me—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-6-4 
                 p-Me—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-6-5 
                 p-Me—Ph  
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-6-6 
                 p-Me—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-6-7 
                 p-Me—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-6-8 
                 p-Me—Ph  
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-36-8 
                 p-Me—Ph 
                 *  
                 H 
                 * 
                   n Bu 
                 N 3   
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-39-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-42 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-47-8  
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIV-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIV-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 II 
               
               
                 XIV-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XIV-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 N 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-17 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XV-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-18 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XV-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-19 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XV-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-20 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XV-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-21 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XV-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-22 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7    
                 R 8   
               
               
                   
               
             
            
               
                 XV-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-22-8 
                 Et  
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-26 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XV-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-27 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XV-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-28 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XV-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-29 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XV-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-30 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XV-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-31 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XV-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XV-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-32 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-33 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-34 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-35 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-36 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-36-1 
                 p-Me-Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-36-2 
                 p-Me-Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-36-3 
                 p-Me-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-36-4 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-36-5 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-36-6 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-36-7 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-36-8 
                 p-Me-Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-37 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-37-1 
                 p-Me-Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-37-2 
                 p-Me-Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-37-3 
                 p-Me-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-37-4 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-37-5 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-37-6 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-37-7 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-37-8 
                 p-Me-Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-38 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-38-1 
                 p-Cl-Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-38-2 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-38-3 
                 p-Cl-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-38-4 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-38-5 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-38-6 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-38-7 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-38-8 
                 p-Cl-Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-39 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-39-1 
                 p-Br-Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-39-2 
                 p-Br-Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-39-3 
                 p-Br-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-39-4 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-39-5 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-39-6 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-39-7 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-39-8 
                 p-Br-Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-40 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-40-1 
                 p-I-Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-40-2 
                 p-I-Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-40-3 
                 p-I-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-40-4 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-40-5 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-40-6 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-40-7 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-40-8 
                 p-I-Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-41 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-42 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-43 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-44 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-45 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-46 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-46-1 
                 p-Me-Ph 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-46-2 
                 p-Me-Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-46-3 
                 p-Me-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-46-4 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-46-5 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-46-6 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-46-7 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-46-8 
                 p-Me-Ph 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2 and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-49-6  
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-49-7  
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-49-8  
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 F  
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XV-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XV-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XV-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-5 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7    
                 R 8   
               
               
                   
               
             
            
               
                 XVI-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-10 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7    
                 R 8   
               
               
                   
               
             
            
               
                 XVI-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-12-1 
                 Et  
                 H 
                 H 
                 H 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-12-2 
                 Et  
                 H 
                 H 
                 CH 3   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-12-3 
                 Et  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-12-4 
                 Et  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-12-5 
                 Et  
                 H  
                 H 
                 CH 2 Ph 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-12-6 
                 Et  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-12-7 
                 Et  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-12-8 
                 Et  
                 * 
                 H 
                 * 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-13-1 
                   i Pr  
                 H 
                 H 
                 H 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-13-2 
                   i Pr  
                 H 
                 H 
                 CH 3   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-13-3 
                   i Pr  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-13-4 
                   i Pr  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-13-5 
                   i Pr  
                 H  
                 H 
                 CH 2 Ph 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-13-6 
                   i Pr  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-13-7 
                   i Pr  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-13-8 
                   i Pr  
                 * 
                 H 
                 * 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-14-1 
                   t Bu  
                 H 
                 H 
                 H 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-14-2 
                   t Bu  
                 H 
                 H 
                 CH 3   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-14-3 
                   t Bu  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-14-4 
                   t Bu  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-14-5 
                   t Bu  
                 H  
                 H 
                 CH 2 Ph 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-14-6 
                   t Bu  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-14-7 
                   t Bu  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-14-8 
                   t Bu  
                 * 
                 H 
                 * 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-15-1 
                 Ph  
                 H 
                 H 
                 H 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-15-2 
                 Ph  
                 H 
                 H 
                 CH 3   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-15-3 
                 Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-15-4 
                 Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-15-5 
                 Ph  
                 H  
                 H 
                 CH 2 Ph 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-15-6 
                 Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-15-7 
                 Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-15-8 
                 Ph  
                 * 
                 H 
                 * 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-16-1 
                 p-Me—Ph  
                 H 
                 H 
                 H 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-16-2 
                 p-Me—Ph  
                 H 
                 H 
                 CH 3   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-16-3 
                 p-Me—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-16-4 
                 p-Me—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-16-5 
                 p-Me—Ph  
                 H  
                 H 
                 CH 2 Ph 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-16-6 
                 p-Me—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-16-7 
                 p-Me—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-16-8 
                 p-Me—Ph  
                 * 
                 H 
                 * 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-17-1 
                 p-F—Ph  
                 H 
                 H 
                 H 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-17-2 
                 p-F—Ph  
                 H 
                 H 
                 CH 3   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-17-3 
                 p-F—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-17-4 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-17-5 
                 p-F—Ph  
                 H  
                 H 
                 CH 2 Ph 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-17-6 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-17-7 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-17-8 
                 p-F—Ph  
                 * 
                 H 
                 * 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-18-1 
                 p-Cl—Ph  
                 H 
                 H 
                 H 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-18-2 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 3   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-18-3 
                 p-Cl—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-18-4 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-18-5 
                 p-Cl—Ph  
                 H  
                 H 
                 CH 2 Ph 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-18-6 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-18-7 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-18-8 
                 p-Cl—Ph  
                 * 
                 H 
                 * 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-19-1 
                 p-Br—Ph  
                 H 
                 H 
                 H 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-19-2 
                 p-Br—Ph  
                 H 
                 H 
                 CH 3   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-19-3 
                 p-Br—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-19-4 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-19-5 
                 p-Br—Ph  
                 H  
                 H 
                 CH 2 Ph 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-19-6 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-19-7 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-19-8 
                 p-Br—Ph  
                 * 
                 H 
                 * 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-20-1 
                 p-I—Ph  
                 H 
                 H 
                 H 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-20-2 
                 p-I—Ph  
                 H 
                 H 
                 CH 3   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-20-3 
                 p-I—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-20-4 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-20-5 
                 p-I—Ph  
                 H  
                 H 
                 CH 2 Ph 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-20-6 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-20-7 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-20-8 
                 p-I—Ph  
                 * 
                 H 
                 * 
                 Et  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-21-1 
                 CH 3    
                 H 
                 H 
                 H 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-21-2 
                 CH 3    
                 H 
                 H 
                 CH 3   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-21-3 
                 CH 3    
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-21-4 
                 CH 3    
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-21-5 
                 CH 3    
                 H  
                 H 
                 CH 2 Ph 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-21-6 
                 CH 3    
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-21-7 
                 CH 3    
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-21-8 
                 CH 3    
                 * 
                 H 
                 * 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-22-1 
                 Et  
                 H 
                 H 
                 H 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-22-2 
                 Et  
                 H 
                 H 
                 CH 3   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-22-3 
                 Et  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-22-4 
                 Et  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-22-5 
                 Et  
                 H  
                 H 
                 CH 2 Ph 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-22-6 
                 Et  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-22-7 
                 Et  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-22-8 
                 Et  
                 * 
                 H 
                 * 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-23-1 
                   i Pr  
                 H 
                 H 
                 H 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-23-2 
                   i Pr  
                 H 
                 H 
                 CH 3   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-23-3 
                   i Pr  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-23-4 
                   i Pr  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-23-5 
                   i Pr  
                 H  
                 H 
                 CH 2 Ph 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-23-6 
                   i Pr  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-23-7 
                   i Pr  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-23-8 
                   i Pr  
                 * 
                 H 
                 * 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-24-1 
                   t Bu  
                 H 
                 H 
                 H 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-24-2 
                   t Bu  
                 H 
                 H 
                 CH 3   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-24-3 
                   t Bu  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-24-4 
                   t Bu  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-24-5 
                   t Bu  
                 H  
                 H 
                 CH 2 Ph 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-24-6 
                   t Bu  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-24-7 
                   t Bu  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-24-8 
                   t Bu  
                 * 
                 H 
                 * 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-25-1 
                 Ph  
                 H 
                 H 
                 H 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-25-2 
                 Ph  
                 H 
                 H 
                 CH 3   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-25-3 
                 Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-25-4 
                 Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-25-5 
                 Ph  
                 H  
                 H 
                 CH 2 Ph 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-25-6 
                 Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-25-7 
                 Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-25-8 
                 Ph  
                 * 
                 H 
                 * 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-26-1 
                 p-Me—Ph  
                 H 
                 H 
                 H 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-26-2 
                 p-Me—Ph  
                 H 
                 H 
                 CH 3   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-26-3 
                 p-Me—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-26-4 
                 p-Me—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-26-5 
                 p-Me—Ph  
                 H  
                 H 
                 CH 2 Ph 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-26-6 
                 p-Me—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-26-7 
                 p-Me—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-26-8 
                 p-Me—Ph  
                 * 
                 H 
                 * 
                   i Pr  
                 F  
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7    
                 R 8   
               
               
                   
               
             
            
               
                 XVI-28-1 
                 p-Cl—Ph  
                 H 
                 H 
                 H 
                   i Pr  
                 F 
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 F  
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-31-8 
                 CH 3   
                 H 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-34-1 
                   n Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-34-2 
                   n Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-34-3 
                   n Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-34-4 
                   n Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-34-5 
                   n Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-34-6 
                   n Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-34-7 
                   n Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-34-8 
                   n Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-35 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-35-8 
                 Ph 
                 H 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 FI 
                 H 
               
               
                 XVI-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R32 
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-39-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-41-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-41-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-41-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-41-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-41-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-41-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-41-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-41-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-42 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-43-1 
                   i Pr  
                 H 
                 H 
                 H 
                 Bz  
                 F 
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XVI-43-2 
                   i Pr  
                 H 
                 H 
                 CH 3   
                 Bz  
                 F 
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XVI-43-3 
                   i Pr  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz  
                 F 
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XVI-43-4 
                   i Pr  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz  
                 F 
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XVI-43-5 
                   i Pr  
                 H 
                 H 
                 CH 2 Ph 
                 Bz  
                 F 
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XVI-43-6 
                   i Pr  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz  
                 F 
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XVI-43-7 
                   i Pr  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz  
                 F 
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XVI-43-8 
                   i Pr  
                 *  
                 H 
                 * 
                 Bz  
                 F 
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVI-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVI-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVI-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-50-1 
                 p-I—Ph  
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-50-2 
                 p-I—Ph  
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-50-3 
                 p-I—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-50-4 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2    
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-50-5 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-50-6 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl  
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-50-7 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3    
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-50-8 
                 p-I—Ph  
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X  
                 Y 
                 R 7    
                 R 8   
               
               
                   
               
             
            
               
                 XVII-3-1 
                   i Pr  
                 H 
                 H 
                 H 
                 CH 3   
                 F  
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-3-2 
                   i Pr  
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F  
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-3-3 
                   i Pr  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F  
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-3-4 
                   i Pr  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F  
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-3-5 
                   i Pr  
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F  
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-3-6 
                   i Pr  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F  
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-3-7 
                   i Pr  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F  
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-3-8 
                   i Pr  
                 * 
                 H 
                 * 
                 CH 3   
                 F  
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII- 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 22-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 22-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 22-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 22-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 22-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 22-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 22-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 22-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII- 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 23-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 23-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 23-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 23-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 23-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 23-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 23-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 23-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII- 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 24-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 24-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 24-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 24-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 24-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 24-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 24-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 24-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII- 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 25-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 25-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 25-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 25-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 25-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 25-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 25-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 25-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII- 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 31-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 31-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 31-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 31-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 31-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 31-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 31-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 31-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII- 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 32-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 32-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 32-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 32-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 32-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 32-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 32-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 32-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII- 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 33-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 33-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 33-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 33-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 33-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 33-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 33-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 33-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII- 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 34-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 34-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 34-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 34-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 34-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 34-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 34-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 34-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII- 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 35-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 35-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 35-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 35-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 35-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 35-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 35-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XVII- 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 35-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVIl-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-39-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-42 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVII-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XVII-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 F 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVII-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-2 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-3 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-4 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-5 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-6 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-6-1 
                 p-Me-Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-6-2 
                 p-Me-Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-6-3 
                 p-Me-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-6-4 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-6-5 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-6-6 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-6-7 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-6-8 
                 p-Me-Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-7 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-7-1 
                 p-F-Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-7-2 
                 p-F-Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-7-3 
                 p-F-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-7-4 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-7-6 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-7-7 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-7-8 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-7-20 
                 p-F-Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-8 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-8-1 
                 p-Cl-Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-8-2 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 3   
                 CH 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIIl-8-3 
                 p-Cl-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-8-4 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-8-5 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-8-6 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-8-7 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-8-8 
                 p-Cl-Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-9 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-9-1 
                 p-Br-Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-9-2 
                 p-Br-Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-9-3 
                 p-Br-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-9-4 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-9-6 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-9-7 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-9-8 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-9-20 
                 p-Br-Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-10 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-10-1 
                 p-I-Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-10-2 
                 p-I-Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-10-3 
                 p-I-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-10-4 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-10-5 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-10-6 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-10-7 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-10-8 
                 p-I-Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-11 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-11-7 
                 CH 3    
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-12 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-13 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-14 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-15 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-16 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-16-1 
                 p-Me-Ph 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-16-2 
                 p-Me-Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-16-3 
                 p-Me-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-16-4 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-16-5 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-16-6 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-16-7 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-16-8 
                 p-Me-Ph 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-22-6 
                 Et 
                 H 
                 II 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 II 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-36-1 
                 p-MePh 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-36-2 
                 p-MePh 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-36-3 
                 p-MePh 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-36-4 
                 p-MePh 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-36-5 
                 p-MePh 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-36-6 
                 p-MePh 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-36-7 
                 p-MePh 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-36-8 
                 p-MePh 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-37-1 
                 p-F-Ph  
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-37-2 
                 p-F-Ph  
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-37-3 
                 p-F-Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-37-4 
                 p-F-Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-37-5 
                 p-F-Ph  
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-37-6 
                 p-F-Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-37-7 
                 p-F-Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-37-8 
                 p-F-Ph  
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-38-1 
                 p-Cl-Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-38-2 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-38-3 
                 p-Cl-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-38-4 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-38-5 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-38-6 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-38-7 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-38-8 
                 p-Cl-Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-39-1 
                 p-Br-Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-39-2 
                 p-Br-Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-39-3 
                 p-Br-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-39-4 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-39-5 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-39-6 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-39-7 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-39-8 
                 p-Br-Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-40-1 
                 p-I-Ph  
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-40-2 
                 p-I-Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-40-3 
                 p-I-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-40-4 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-40-5 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-40-6 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-40-7 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-40-8 
                 p-I-Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-42 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-46-1 
                 p-Me-Ph 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-46-2 
                 p-Me-Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-46-3 
                 p-Me-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-46-4 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-46-5 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-46-6 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-46-7 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-46-8 
                 p-Me-Ph 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-47-1  
                 p-F—Ph  
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH  
                 H 
                 H 
               
               
                 XVIII-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-48-1  
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH  
                 H 
                 H 
               
               
                 XVIII-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-49-1  
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH  
                 H 
                 H 
               
               
                 XVIII-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XVIII-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XVIII-50-1  
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH  
                 H 
                 H 
               
               
                 XVIII-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                 XVIII-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 H 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-1-1  
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-2-1  
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-3-1  
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-4-1  
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-5-1  
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-6-1  
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-7-1 
                 p-F—Ph  
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-7-20  
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-8-8  
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-9-20  
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-10-1  
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-11-1  
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-13-1 
                   i Pr  
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-13-2 
                   i Pr  
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-13-3 
                   i Pr  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-13-4 
                   i Pr  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-13-5 
                   i Pr  
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-13-6 
                   i Pr  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-13-7 
                   i Pr  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-13-8 
                   i Pr  
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
               
               
                   
               
             
            
               
                 XIX-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
               
               
                 XIX-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
               
               
                 XIX-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
               
               
                 XIX-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
               
               
                 XIX-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
               
               
                 XIX-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
               
               
                 XIX-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
               
               
                 XIX-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-29-1 
                 p-Br—Ph  
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-29-2 
                 p-Br—Ph  
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-29-3 
                 p-Br—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-29-4 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-29-5 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-29-6 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-29-7 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-29-8 
                 p-Br—Ph  
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 F 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XIX-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 F 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XIX-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XIX-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 F 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XIX-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 F 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XIX-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 F 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XIX-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH3 
                   i Pr 
                 OCH 3   
                 F 
                 F  
                 OH 
                 H 
                 H 
               
               
                 XIX-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 F 
                 F  
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-35 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH- 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
                   
                   
                   
                 (CH 3 ) 2   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIX-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol- 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
                   
                   
                   
                 3-yl 
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIX-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 - 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
                   
                   
                   
                 SCH 3   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XIX-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-39-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-40-1 
                 p-I—Ph  
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-40-2 
                 p-I—Ph  
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-40-3 
                 p-I—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-40-4 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-40-5 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-40-6 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-40-7 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-40-8 
                 p-I—Ph  
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2 and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-42 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 X1X-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XIX-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XIX-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XIX-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XIX-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 F 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XX-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XX-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XX-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XX-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XX-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH  
                 H 
                 H 
               
               
                 XX-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-16-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-16-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-16-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-16-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-16-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-16-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-16-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-16-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
               
               
                   
               
             
            
               
                 XX-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                 XX-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-37 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XX-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-38 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XX-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-39 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XX-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-39-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-40 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XX-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-41 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XX-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-42 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XX-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-43 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XX-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-44 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XX-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-45 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
               
            
           
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
            
               
                   
                 XX-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-46 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XX-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-47 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y  
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XX-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-48 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XX-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-49 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XX-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX-50 
               
               
                   
               
               
                   
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
                 R 7   
                 R 8   
                   
               
               
                   
               
             
            
               
                   
                 XX-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
                   
               
               
                   
                 XX-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 OCH 3   
                 H 
                 F 
                 OH 
                 H 
                 H 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI 3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXL-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XX1-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-32 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-33 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-34 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-35 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-36 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-37 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-38 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-39 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-39-8 
                 p-Br—Ph 
                 H 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-40 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-41 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-42 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-43 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-44 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-45 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-46 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXI-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz  
                 H  
                 CH 3   
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXI-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXI-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXI-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXII-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXII-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXII-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXII-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXII-16-1  
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXII-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXII-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXII-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXII-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXII-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXII-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXII-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXII-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXII-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXII-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-39-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-41-2  
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-42 
               
               
                   
               
               
                 No  
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXII-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6  X Y 
               
               
                   
               
             
            
               
                 XXII-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F H OH 
               
               
                 XXII-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F H OH 
               
               
                 XXII-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F H OH 
               
               
                 XXII-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F H OH 
               
               
                 XXII-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F H OH 
               
               
                 XXII-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F H OH 
               
               
                 XXII-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F H OH 
               
               
                 XXII-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F H OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXII-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-49 
               
               
                   
               
               
                 No 
                 R l   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXII-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXII-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXII-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-2 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-3 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXIII-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R4 
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXIII-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-6 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-12-8  
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-22 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-22-1  
                 Et  
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-22-2 
                 Et  
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-22-3 
                 Et  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-22-4 
                 Et  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-22-5 
                 Et  
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-22-6 
                 Et  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-22-7 
                 Et  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-22-8 
                 Et  
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-23 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-23-1 
                   i Pr 
                 H  
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-23-2 
                   i Pr 
                 H  
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-23-3 
                   i Pr 
                 H  
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-23-4 
                   i Pr 
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-23-5 
                   i Pr 
                 H  
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-23-6 
                   i Pr 
                 H  
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-23-7 
                   i Pr 
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-24 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-24-1 
                   t Bu  
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-24-2 
                   t Bu  
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-24-3 
                   t Bu  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-24-4 
                   t Bu  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-24-5 
                   t Bu  
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-24-6 
                   t Bu  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-24-7 
                   t Bu  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-24-8 
                   t Bu  
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-25 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-25-1 
                 Ph  
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-25-2 
                 Ph  
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-25-3 
                 Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-25-4 
                 Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-25-5 
                 Ph  
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-25-6 
                 Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-25-7 
                 Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-25-8 
                 Ph  
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-26 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-27 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-27-1 
                 p-F—Ph 
                 H  
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-27-2 
                 p-F—Ph 
                 H  
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-27-3 
                 p-F—Ph 
                 H  
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-27-4 
                 p-F—Ph 
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-27-5 
                 p-F—Ph 
                 H  
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-27-6 
                 p-F—Ph 
                 H  
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-27-7 
                 p-F—Ph 
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-28 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-29 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-30 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXIII-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-31 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-31-1 
                 CH 3   
                 H  
                 H 
                 H 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-31-2 
                 CH 3   
                 H  
                 H 
                 CH 3   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-31-3 
                 CH 3   
                 H  
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-31-4 
                 CH 3   
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-31-5 
                 CH 3   
                 H  
                 H 
                 CH 2 Ph 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-31-6 
                 CH 3   
                 H  
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-31-7 
                 CH 3   
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-32 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-32-1  
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-33 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-34 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-34-1  
                   t Bu 
                 H  
                 H 
                 H 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-34-2 
                   t Bu 
                 H  
                 H 
                 CH 3   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-34-3 
                   t Bu 
                 H  
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-34-4 
                   t Bu 
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-34-5 
                   t Bu 
                 H  
                 H 
                 CH 2 Ph 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-34-6 
                   t Bu 
                 H  
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-34-7 
                   t Bu 
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-35 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-36 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII-36-1 
                 p-Me—Ph  
                 H  
                 H 
                 H 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-36-2 
                 p-Me—Ph  
                 H  
                 H 
                 CH 3   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-36-3 
                 p-Me—Ph  
                 H  
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-36-4 
                 p-Me—Ph  
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-36-5 
                 p-Me—Ph  
                 H  
                 H 
                 CH 2 Ph 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-36-6 
                 p-Me—Ph  
                 H  
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-36-7 
                 p-Me—Ph  
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXIII-36-8 
                 p-Me—Ph  
                 * 
                 H 
                 * 
                   n Bu 
                 H  
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII- 
                 p-F—Ph  
                 H 
                 H 
                 H 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 37-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-F—Ph  
                 H 
                 H 
                 CH 3   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 37-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-F—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 37-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 37-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-F—Ph  
                 H  
                 H 
                 CH 2 Ph 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 37-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 37-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 37-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-F—Ph  
                 * 
                 H 
                 * 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 37-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII- 
                 p-Cl—Ph  
                 H 
                 H 
                 H 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 38-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 3   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 38-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Cl—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 38-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 38-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Cl—Ph  
                 H  
                 H 
                 CH 2 Ph 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 38-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 38-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 38-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Cl—Ph  
                 * 
                 H 
                 * 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 38-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII- 
                 p-Br—Ph  
                 H 
                 H 
                 H 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 39-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Br—Ph  
                 H 
                 H 
                 CH 3   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 39-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Br—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 39-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 39-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Br—Ph  
                 H  
                 H 
                 CH 2 Ph 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 39-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 39-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 39-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Br—Ph  
                 * 
                 H 
                 * 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 39-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII- 
                 p-I—Ph  
                 H 
                 H 
                 H 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 40-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-I—Ph  
                 H 
                 H 
                 CH 3   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 40-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-I—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 40-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 40-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-I—Ph  
                 H  
                 H 
                 CH 2 Ph 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 40-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 40-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 40-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-I—Ph  
                 * 
                 H 
                 * 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 40-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII- 
                 CH 3    
                 H 
                 H 
                 H 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 41-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 CH 3    
                 H 
                 H 
                 CH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 41-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 CH 3    
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 41-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 CH 3    
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 41-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 CH 3    
                 H  
                 H 
                 CH 2 Ph 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 41-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 CH 3    
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 41-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 CH 3    
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 41-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 CH 3    
                 * 
                 H 
                 * 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 41-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-42 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII- 
                 Et  
                 H 
                 H 
                 H 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 42-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 Et  
                 H 
                 H 
                 CH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 42-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 Et  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 42-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 Et  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 42-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 Et  
                 H  
                 H 
                 CH 2 Ph 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 42-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 Et  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 42-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 Et  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 42-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 Et  
                 * 
                 H 
                 * 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 42-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII- 
                   i Pr  
                 H 
                 H 
                 H 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 43-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                   i Pr  
                 H 
                 H 
                 CH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 43-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                   i Pr  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 43-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                   i Pr  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 43-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                   i Pr  
                 H  
                 H 
                 CH 2 Ph 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 43-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                   i Pr  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 43-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                   i Pr  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 43-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                   i Pr  
                 * 
                 H 
                 * 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 43-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII- 
                   t Bu  
                 H 
                 H 
                 H 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 44-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                   t Bu  
                 H 
                 H 
                 CH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 44-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                   t Bu  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 44-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                   t Bu  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 44-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                   t Bu  
                 H  
                 H 
                 CH 2 Ph 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 44-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                   t Bu  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 44-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                   t Bu  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 44-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                   t Bu  
                 * 
                 H 
                 * 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 44-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII- 
                 Ph  
                 H 
                 H 
                 H 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 45-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 Ph  
                 H 
                 H 
                 CH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 45-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 45-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 45-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 Ph  
                 H  
                 H 
                 CH 2 Ph 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 45-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 45-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 45-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 Ph  
                 * 
                 H 
                 * 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 45-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII- 
                 p-Me—Ph  
                 H 
                 H 
                 H 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 46-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Me—Ph  
                 H 
                 H 
                 CH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 46-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Me—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 46-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Me—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 46-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Me—Ph  
                 H  
                 H 
                 CH 2 Ph 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 46-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Me—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 46-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Me—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 46-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Me—Ph  
                 * 
                 H 
                 * 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 46-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII- 
                 p-F—Ph  
                 H 
                 H 
                 H 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 47-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-F—Ph  
                 H 
                 H 
                 CH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 47-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-F—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 47-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 47-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-F—Ph  
                 H  
                 H 
                 CH 2 Ph 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 47-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 47-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 47-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-F—Ph  
                 * 
                 H 
                 * 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 47-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII- 
                 p-Cl—Ph  
                 H 
                 H 
                 H 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 48-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 48-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Cl—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 48-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 48-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Cl—Ph  
                 H  
                 H 
                 CH 2 Ph 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 48-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 48-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 48-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Cl—Ph  
                 * 
                 H 
                 * 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 48-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII- 
                 p-Br—Ph  
                 H 
                 H 
                 H 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 49-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Br—Ph  
                 H 
                 H 
                 CH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 49-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Br—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 49-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 49-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Br—Ph  
                 H  
                 H 
                 CH 2 Ph 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 49-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 49-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 49-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-Br—Ph  
                 * 
                 H 
                 * 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 49-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIII-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIII- 
                 p-I—Ph  
                 H 
                 H 
                 H 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 50-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-I—Ph  
                 H 
                 H 
                 CH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 50-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-I—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 50-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 50-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-I—Ph  
                 H  
                 H 
                 CH 2 Ph 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 50-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 50-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 50-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIII- 
                 p-I—Ph  
                 * 
                 H 
                 * 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 50-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV- 
                 CH 3    
                 H 
                 H 
                 H 
                 CH 3    
                 H  
                 F 
                 F 
                 OH 
               
               
                 1-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIV- 
                 CH 3    
                 H 
                 H 
                 CH 3   
                 CH 3    
                 H  
                 F 
                 F 
                 OH 
               
               
                 1-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIV- 
                 CH 3    
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3    
                 H  
                 F 
                 F 
                 OH 
               
               
                 1-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIV- 
                 CH 3    
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3    
                 H  
                 F 
                 F 
                 OH 
               
               
                 1-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIV- 
                 CH 3    
                 H  
                 H 
                 CH 2 Ph 
                 CH 3    
                 H  
                 F 
                 F 
                 OH 
               
               
                 1-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIV- 
                 CH 3    
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3    
                 H  
                 F 
                 F 
                 OH 
               
               
                 1-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIV- 
                 CH 3    
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3    
                 H  
                 F 
                 F 
                 OH 
               
               
                 1-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIV- 
                 CH 3    
                 * 
                 H 
                 * 
                 CH 3    
                 H  
                 F 
                 F 
                 OH 
               
               
                 1-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-2 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-3 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-3-1 
                   i Pr  
                 H  
                 H 
                 H 
                 CH 3   
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-3-2 
                   i Pr  
                 H  
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-3-3 
                   i Pr  
                 H  
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-3-4 
                   i Pr  
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-3-5 
                   i Pr  
                 H  
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-3-6 
                   i Pr  
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-3-7 
                   i Pr  
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-3 8 
                   i Pr  
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-4 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-4-1 
                   t Bu  
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-4-2 
                   t Bu  
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-4-3 
                   t Bu  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-4-4 
                   t Bu  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-4-5 
                   t Bu  
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-4-6 
                   t Bu  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-4-7 
                   t Bu  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-4-8 
                   t Bu  
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-5 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-6 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-6-1 
                 p-Me-Ph  
                 H 
                 H 
                 H 
                 CH 3   
                 H  
                 H 
                 F 
                 OH 
               
               
                 XXIV-6-2 
                 p-Me-Ph  
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H  
                 H 
                 F 
                 OH 
               
               
                 XXIV-6-3 
                 p-Me-Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H  
                 H 
                 F 
                 OH 
               
               
                 XXIV-6-4 
                 p-Me-Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H  
                 H 
                 F 
                 OH 
               
               
                 XXIV-6-5 
                 p-Me-Ph  
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H  
                 H 
                 F 
                 OH 
               
               
                 XXIV-6-6 
                 p-Me-Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H  
                 H 
                 F 
                 OH 
               
               
                 XXIV-6-7 
                 p-Me-Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H  
                 H 
                 F 
                 OH 
               
               
                 XXIV-6-8 
                 p-Me-Ph  
                 * 
                 H 
                 * 
                 CH 3   
                 H  
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-7 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-7-1 
                 p-F-Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-7-2 
                 p-F-Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-7-3 
                 p-F-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-7-4 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-7-6 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-7-7 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-7-8 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-7-20 
                 p-F-Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-8 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-8-1 
                 p-Cl-Ph  
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-8-2 
                 p-Cl-Ph  
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-8-3 
                 p-Cl-Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-8-4 
                 p-Cl-Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-8-5 
                 p-Cl-Ph  
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-8-6 
                 p-Cl-Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-8-7 
                 p-Cl-Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-8-8 
                 p-Cl-Ph  
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-9 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-9-1 
                 p-Br-Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-9-2 
                 p-Br-Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-9-3 
                 p-Br-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-9-4 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-9-6 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-9-7 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-9-8 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-9-20 
                 p-Br-Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-10 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-10-1 
                 p-I-Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-10-2 
                 p-I-Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-10-3 
                 p-I-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-10-4 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-10-5 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-10-6 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-10-7 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-10-8 
                 p-I-Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-11 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-12 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-13 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-13-1  
                   i Pr  
                 H 
                 H 
                 H 
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-13-2 
                   i Pr  
                 H 
                 H 
                 CH 3   
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-13-3 
                   i Pr  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-13-4 
                   i Pr  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-13-5 
                   i Pr  
                 H 
                 H 
                 CH 2 Ph 
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-13-6 
                   i Pr  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-13-7 
                   i Pr  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-13-8 
                   i Pr  
                 * 
                 H 
                 * 
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-14 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-15 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-15-1 
                 Ph  
                 H 
                 H 
                 H 
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-15-2 
                 Ph  
                 H 
                 H 
                 CH 3   
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-15-3 
                 Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-15-4 
                 Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-15-5 
                 Ph  
                 H 
                 H 
                 CH 2 Ph 
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-15-6 
                 Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-15-7 
                 Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-15-8 
                 Ph  
                 * 
                 H 
                 * 
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-16 
               
               
                   
               
               
                 N o   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-16-1 
                 p-Me-Ph  
                 H 
                 H 
                 H 
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-16-2 
                 p-Me-Ph  
                 H 
                 H 
                 CH 3   
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-16-3 
                 p-Me-Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-16-4 
                 p-Me-Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-16-5 
                 p-Me-Ph  
                 H 
                 H 
                 CH 2 Ph 
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-16-6 
                 p-Me-Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-16-7 
                 p-Me-Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                 XXIV-16-8 
                 p-Me-Ph  
                 * 
                 H 
                 * 
                 Et  
                 H 
                 H  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R3 b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-38-1 
                 p-Cl—Ph 
                 H  
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-39 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-39-1 
                 p-Br—Ph  
                 H  
                 H  
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-39-2 
                 p-Br—Ph  
                 H  
                 H  
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-39-3 
                 p-Br—Ph  
                 H  
                 H  
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-39-4 
                 p-Br—Ph  
                 H  
                 H  
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-39-5 
                 p-Br—Ph  
                 H  
                 H  
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-39-6 
                 p-Br—Ph  
                 H  
                 H  
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-39-7 
                 p-Br—Ph  
                 H  
                 H  
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-39-8 
                 p-Br—Ph  
                 *  
                 H  
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXIV-40-1  
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXIV-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-42 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R3 a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXIV-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXIV-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIV-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIV-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXIV-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-14 4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-21-S 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-24-1 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-24-2 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-24-3 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-24-7 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-27 
               
               
                   
               
               
                 No 
                 R1 
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3    
                 F 
                 OH 
               
               
                 XXV-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3    
                 F 
                 OH 
               
               
                 XXV-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3    
                 F 
                 OH 
               
               
                 XXV-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3    
                 F 
                 OH 
               
               
                 XXV-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3    
                 F 
                 OH 
               
               
                 XXV-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3    
                 F 
                 OH 
               
               
                 XXV-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3    
                 F 
                 OH 
               
               
                 XXV-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3    
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3    
                 F 
                 OH 
               
               
                 XXV-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a    
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-29-1  
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr  
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr  
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr  
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr  
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr  
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr  
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr  
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr  
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXV-30-1  
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXV-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                 XXV-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-32 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-34 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-34-1  
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-34-8  
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-36 
               
               
                   
               
               
                 No 
                 R l   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-38 6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-39-1 
                 p-Br—Ph  
                 H 
                 H 
                 H 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-39-2 
                 p-Br—Ph  
                 H 
                 H 
                 CH 3   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-39-3 
                 p-Br—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-39-4 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-39-5 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 Ph 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-39-6 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-39-7 
                 p-Br—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-39-8  
                 p-Br—Ph  
                 * 
                 H 
                 * 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu  
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXV-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3    
                 F 
                 OH 
               
               
                 XXV-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3    
                 F 
                 OH 
               
               
                 XXV-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3    
                 F 
                 OH 
               
               
                 XXV-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3    
                 F 
                 OH 
               
               
                 XXV-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3    
                 F 
                 OH 
               
               
                 XXV-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3    
                 F 
                 OH 
               
               
                 XXV-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3    
                 F 
                 OH 
               
               
                 XXV-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3    
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-42 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-42-1  
                 Et  
                 H  
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-42-2 
                 Et  
                 H  
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-42-3 
                 Et  
                 H  
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-42-4 
                 Et  
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-42-5 
                 Et  
                 H  
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-42-6 
                 Et  
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-42-7 
                 Et  
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-42-8 
                 Et  
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-44 2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-46-1  
                 p-Me—Ph 
                 H  
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-46-2  
                 p-Me Ph 
                 H  
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-46-3  
                 p-Me Ph 
                 H  
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-46-4  
                 p-Me Ph 
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-46-5 
                 p-Me Ph 
                 H  
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-46-6  
                 p-Me Ph 
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-46-7  
                 p-Me Ph 
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-46-8  
                 p-Me Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-47-1 
                 p-F Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-47-2 
                 p-F Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-47-3 
                 p-F Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-47-4 
                 p-F Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-47-5 
                 p-F Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-47-6 
                 p-F Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-47-7 
                 p-F Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-47-8 
                 p-F Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-48-1 
                 p-Cl Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-48-2 
                 p-Cl Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-48-3 
                 p-Cl Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-48-4 
                 p-Cl Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-48-5 
                 p-Cl Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-48-6 
                 p-Cl Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-48-7 
                 p-Cl Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-48-8 
                 p-Cl Ph  
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-49-1 
                 p-Br Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-49-2 
                 p-Br Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-49-3 
                 p-Br Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-49-4 
                 p-Br Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-49-5 
                 p-Br Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-49-6 
                 p-Br Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-49-7 
                 p-Br Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-49-8 
                 p-Br Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXV-50-1  
                 p-I Ph 
                 H  
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-50-2 
                 p-I Ph 
                 H  
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-50-3 
                 p-I Ph 
                 H  
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-50-4 
                 p-I Ph 
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-50-5 
                 p-I Ph 
                 H  
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-50-6 
                 p-I Ph 
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-50-7 
                 p-I Ph 
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXV-50-8 
                 p-I Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-1-1 
                 CH 3   
                 H  
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-1-2 
                 CH 3   
                 H  
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-1-3 
                 CH 3   
                 H  
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-1-4 
                 CH 3   
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-1-5 
                 CH 3   
                 H  
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-1-6 
                 CH 3   
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-1-7 
                 CH 3   
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-2-1  
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-3-1 
                   i Pr  
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-3-2 
                   i Pr  
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-3-3 
                   i Pr  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-3-4 
                   i Pr  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-3-5 
                   i Pr  
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-3-6 
                   i Pr  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-3-7 
                   i Pr  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-3-8 
                   i Pr  
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-4-1 
                   t Bu  
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-4-2 
                   t Bu  
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-4-3 
                   t Bu  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-4-4 
                   t Bu  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI 4-5 
                   t Bu  
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-4-6 
                   t Bu  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-4-7 
                   t Bu  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-4-8 
                   t Bu  
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-6-1 
                 p-Me Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-6-2 
                 p-Me Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-6-3 
                 p-Me Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-6-4 
                 p-Me Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-6-5 
                 p-Me Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-6-6 
                 p-Me Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-6-7 
                 p-Me Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-6-8 
                 p-Me Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-7 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-7-1  
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-7-2  
                 p-F—Ph  
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-7-3  
                 p-F—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-7-4  
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-7-6  
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-7-7  
                 p-F—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-7-8  
                 p-F—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-7-20  
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-9-1  
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-9-2  
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-9-3  
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-9-4  
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-9-6  
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-9-7  
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-9-8  
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-9- 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 20 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXVI-10-1  
                 p-I—Ph 
                 H  
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-10-2  
                 p-I—Ph 
                 H  
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-10-3  
                 p-I—Ph 
                 H  
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-10-4  
                 p-I—Ph 
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-10-5  
                 p-I—Ph 
                 H  
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-10-6  
                 p-I—Ph 
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-10-7  
                 p-I—Ph 
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-10-8  
                 p-I—Ph 
                 *  
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-18 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXVI-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI 25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-28 
               
               
                   
               
               
                 Ns 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXVI-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b    
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-32 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5    
                 R 6    
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXVI-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-33 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-34 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-37-8 
                 p-F—Ph  
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-39-8 
                 p-Br—Ph  
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-42 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXV1-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXV1-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-42-8  
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXV1-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVI-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVI-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVI-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXVI-50-7 
                 p-I—Ph 
                 II 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 FI 
                 OH 
               
               
                 XXVI-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-7-1  
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-7-2  
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-7-3  
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-7-4  
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-7-6  
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-7-7  
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-7-8  
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-9-1  
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-9-2  
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-9-3  
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-9-4  
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-9-6  
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-9-7  
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-9-8  
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol- 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
                   
                   
                   
                 3-yl 
                   
                   
                   
                   
                   
               
               
                 XXVII-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-l 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
                   
                   
                   
                 3-y 
                   
                   
                   
                   
                   
               
               
                 XXVII-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-28-8 
                 p-Cl—Ph  
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-32 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-33 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-33-1 
                   i Pr  
                 H 
                 H 
                 H 
                   n Bu 
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXVII-33-2 
                   i Pr  
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXVII-33-3 
                   i Pr  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXVII-33-4 
                   i Pr  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXVII-33-5 
                   i Pr  
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXVII-33-6 
                   i Pr  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXVII-33-7 
                   i Pr  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXVII-33-8 
                   i Pr  
                 * 
                 H 
                 * 
                   n Bu 
                 H  
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-34 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-34-1 
                   t Bu  
                 H 
                 H 
                 H 
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-34-2 
                   t Bu  
                 H 
                 H 
                 CH 3   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-34-3 
                   t Bu  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-34-4 
                   t Bu  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-34-5 
                   t Bu  
                 H 
                 H 
                 CH 2 Ph 
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-34-6 
                   t Bu  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-34-7 
                   t Bu  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-34-8 
                   t Bu  
                 * 
                 H 
                 * 
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-35 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-35-1 
                 Ph 
                 H  
                 H 
                 H 
                   n Bu  
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXVII-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-35-8 
                 Ph 
                 *  
                 H 
                 * 
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-36 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-37 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-37-1 
                 p-F—Ph  
                 H 
                 H 
                 H 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-37-2 
                 p-F—Ph  
                 H 
                 H 
                 CH 3   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-37-3 
                 p-F—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-37-4 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-37-5 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 Ph 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-37-6 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-37-7 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-37-8 
                 p-F—Ph  
                 * 
                 H 
                 * 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-38 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-38-1 
                 p-Cl—Ph 
                 H  
                 H 
                 H 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-38-2 
                 p-Cl—Ph 
                 H  
                 H 
                 CH 3   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-38-3 
                 p-Cl—Ph 
                 H  
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-38-4 
                 p-Cl—Ph 
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-38-5 
                 p-Cl—Ph 
                 H  
                 H 
                 CH 2 Ph 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-38-6 
                 p-Cl—Ph 
                 H  
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-38-7 
                 p-Cl—Ph 
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-38-8 
                 p-Cl—Ph 
                 *  
                 H 
                 * 
                   n Bu  
                 H  
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-39 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-39-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu  
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-40 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-40-1 
                 p-I—Ph  
                 H 
                 H 
                 H 
                   n Bu  
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXVII-40-2 
                 p-I—Ph  
                 H 
                 H 
                 CH 3   
                   n Bu  
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXVII-40-3 
                 p-I—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu  
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXVII-40-4 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu  
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXVII-40-5 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 Ph 
                   n Bu  
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXVII-40-6 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu  
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXVII-40-7 
                 p-I—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu  
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXVII-40-8 
                 p-I—Ph  
                 * 
                 H 
                 * 
                   n Bu  
                 H  
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-41 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-42 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-42-1 
                 Et  
                 H  
                 H 
                 H 
                 Bz  
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXVII-42-2 
                 Et  
                 H  
                 H 
                 CH 3   
                 Bz  
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXVII-42-3 
                 Et  
                 H  
                 H 
                 CH(CH 3 ) 2   
                 Bz  
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXVII-42-4 
                 Et  
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz  
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXVII-42-5 
                 Et  
                 H  
                 H 
                 CH 2 Ph 
                 Bz  
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXVII-42-6 
                 Et  
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 Bz  
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXVII-42-7 
                 Et  
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz  
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXVII-42-8 
                 Et  
                 * 
                 H 
                 * 
                 Bz  
                 H 
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-43 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXVII-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXVII-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXVII-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXVII-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXVII-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXVII-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXVII-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F  
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-45 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXVII-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXVII-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                 XXVII-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz  
                 H  
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVII-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVII-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXVII-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-2-1 
                 Et  
                 H 
                 H 
                 H 
                 CH 3   
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-2-8 
                 Et  
                 * 
                 H 
                 * 
                 CH 3   
                 H  
                 H  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-8-1 
                 p-Cl—Ph  
                 H 
                 H 
                 H 
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-8-2 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 3   
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-8-3 
                 p-Cl—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-8-4 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-8-5 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 Ph 
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-8-6 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-8-7 
                 p-Cl—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                 XXVIII-8-8 
                 p-Cl—Ph  
                 * 
                 H 
                 * 
                 CH 3    
                 H  
                 H  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-13 
               
               
                   
               
               
                   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X Y 
               
               
                   
               
             
            
               
                   
               
            
           
           
               
               
               
               
               
               
               
               
               
               
            
               
                 XXVIII-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVHI-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-17 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a    
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-18-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-21 
               
               
                   
               
               
                   
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-21 -8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-27 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-27-1 
                 p-F—Ph  
                 H 
                 H 
                 H 
                   i Pr  
                 H  
                 H  
                 F  
                 OH 
               
               
                 XXVIII-27-2 
                 p-F—Ph  
                 H 
                 H 
                 CH 3   
                   i Pr  
                 H  
                 H  
                 F  
                 OH 
               
               
                 XXVIII-27-3 
                 p-F—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr  
                 H  
                 H  
                 F  
                 OH 
               
               
                 XXVIII-27-4 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr  
                 H  
                 H  
                 F  
                 OH 
               
               
                 XXVIII-27-5 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 Ph 
                   i Pr  
                 H  
                 H  
                 F  
                 OH 
               
               
                 XXVIII-27-6 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr  
                 H  
                 H  
                 F  
                 OH 
               
               
                 XXVIII-27-7 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr  
                 H  
                 H  
                 F  
                 OH 
               
               
                 XXVIII-27-8 
                 p-F—Ph  
                 * 
                 H 
                 * 
                   i Pr  
                 H  
                 H  
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-30 
               
               
                   
               
               
                 No 
                 R l   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr  
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-32 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-33-1 
                   i Pr  
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-33-2 
                   i Pr  
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-33-3 
                   i Pr  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-33-4 
                   i Pr  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-33-5 
                   i Pr  
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-33-6 
                   i Pr  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-33-7 
                   i Pr  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-33-8 
                   i Pr  
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-39-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-41-5 
                 CH 3   
                 II 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-42 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-45 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXVIII-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXVIII-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXVIII-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX 1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH . 
               
               
                 XXIX-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-5-8  
                 Ph  
                 *  
                 H  
                 * 
                 CH 3   
                 H  
                 CH 3   
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-6-1  
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-6-8 
                 p-Me—Ph 
                 *  
                 H  
                 * 
                 CH 3   
                 H  
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-8-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-8-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-8-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-8-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-8-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-8-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-8-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-8-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-9-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-9-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-9-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-9-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-9-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-9-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-9-8 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-9-20 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 10-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 10-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 10-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 10-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 10-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 10-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 10-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 10-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH3 
                 F 
                 OH 
               
               
                 XXIX-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX 12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 16-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 16-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 16-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 16-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 16-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 16-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 16-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 16-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 18-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 18-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 18-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 18-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 18-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 18-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 18-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 18-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 19-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 19-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 19-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 19-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 19-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 19-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 19-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 19-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX 21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 26-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 26-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 26-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 26-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 26-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 26-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 26-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 26-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 28-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 28-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 28-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 28-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 28-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 28-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 28-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 28-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 29-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 29-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 29-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 29-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 29-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 29-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 29-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 29-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 36-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 36-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 36-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 36-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 36-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 36-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 36-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 36-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX- 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 37-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 37-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 37-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 37-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 37-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 37-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 37-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 37-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 38-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 38-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 38-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 38-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 38-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 38-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 38-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 38-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 39-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 39-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 39-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 39-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 39-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 39-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 39-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 39-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 40-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 40-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 40-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 40-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 40-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 40-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 40-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 40-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-42 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 XXIX-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 46-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 46-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 46-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 46-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 46-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 46-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 46-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 46-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX- 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 47-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 47-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 47-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 47-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 47-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 47-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 47-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 47-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 48-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 48-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 48-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 48-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 48-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 48-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 48-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 48-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 49-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 49-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 49-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 49-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 49-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 49-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 49-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 49-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXIX-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 50-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 50-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 50-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 50-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 50-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 50-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 50-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXIX- 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 CH 3   
                 F 
                 OH 
               
               
                 50-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-1 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-2 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-3 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-4 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-5 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-6 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX- 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 6-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 6-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 6-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 6-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 6-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 6-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 6-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 6-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-7-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-7-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-7-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-7-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-7-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-7-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-7-8 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-7-20 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX- 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 8-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 8-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 8-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 8-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 8-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 8-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 8-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 8-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX- 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 9-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 9-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 9-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 9-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 9-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 9-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 9-8 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXX- 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 9-20 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-10-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-10-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-10-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-10-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-10-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-10-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-10-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-10-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-16-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-16-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-16-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-16-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-16-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-16-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-16-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-16-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-17-8 
                 p-F—Ph 
                 *  
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-18-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-18-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-18-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-18-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-18-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-18-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-18-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-18-8 
                 p-Cl—Ph 
                 *  
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-19-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-19-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-19-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-19-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-19-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-19-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-19-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-19-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-39-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-42 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-44 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-45 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-47 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-47-1  
                 p-F-Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H  
                 F 
                 H 
                 OH 
               
               
                 XXX-47-2 
                 p-F-Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H  
                 F 
                 H 
                 OH 
               
               
                 XXX-47-3 
                 p-F-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H  
                 F 
                 H 
                 OH 
               
               
                 XXX-47-4 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H  
                 F 
                 H 
                 OH 
               
               
                 XXX-47-5 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H  
                 F 
                 H 
                 OH 
               
               
                 XXX-47-6 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H  
                 F 
                 H 
                 OH 
               
               
                 XXX-47-7 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H  
                 F 
                 H 
                 OH 
               
               
                 XXX-47-8 
                 p-F-Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H  
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-48 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-48-1 
                 p-Cl-Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-48-2 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-48-3 
                 p-Cl-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-48 4 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-48-5 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-48-6 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-48-7 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-48-8 
                 p-Cl-Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-49 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-49-1  
                 p-Br-Ph  
                 H  
                 H 
                 H 
                 Bz 
                 H  
                 F  
                 H 
                 OH 
               
               
                 XXX-49-2 
                 p-Br-Ph  
                 H  
                 H 
                 CH 3   
                 Bz 
                 H  
                 F  
                 H 
                 OH 
               
               
                 XXX-49-3 
                 p-Br-Ph  
                 H  
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H  
                 F  
                 H 
                 OH 
               
               
                 XXX-49-4 
                 p-Br-Ph  
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H  
                 F  
                 H 
                 OH 
               
               
                 XXX-49-5 
                 p-Br-Ph  
                 H  
                 H 
                 CH 2 Ph 
                 Bz 
                 H  
                 F  
                 H 
                 OH 
               
               
                 XXX-49-6 
                 p-Br-Ph  
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H  
                 F  
                 H 
                 OH 
               
               
                 XXX-49-7 
                 p-Br-Ph  
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H  
                 F  
                 H 
                 OH 
               
               
                 XXX-49-8 
                 p-Br-Ph  
                 * 
                 H 
                 * 
                 Bz 
                 H  
                 F  
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXX-50 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXX-50-1 
                 p-I-Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-50-2 
                 p-I-Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-50-3 
                 p-I-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-50-4 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-50-5 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-50-6 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-50-7 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                 XXX-50-8 
                 p-I-Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 H 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-1 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-1-1 
                 CH 3   
                 H  
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-1-2 
                 CH 3   
                 H  
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-1-3 
                 CH 3   
                 H  
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-1-4 
                 CH 3   
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-1-5 
                 CH 3   
                 H  
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-1-6 
                 CH 3   
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-1-7 
                 CH 3   
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-2 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXXI-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXXI-2-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXXI-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXXI-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXXI-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXXI-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXXI-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F  
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-3 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-3-1 
                   i Pr  
                 H  
                 H 
                 H 
                 CH 3   
                 H  
                 F 
                 F  
                 OH 
               
               
                 XXXI-3-2 
                   i Pr  
                 H  
                 H 
                 CH 3   
                 CH 3   
                 H  
                 F 
                 F  
                 OH 
               
               
                 XXXI-3-3 
                   i Pr  
                 H  
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H  
                 F 
                 F  
                 OH 
               
               
                 XXXI-3-4 
                   i Pr  
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H  
                 F 
                 F  
                 OH 
               
               
                 XXXI-3-5 
                   i Pr  
                 H  
                 H 
                 CH 2 Ph 
                 CH 3   
                 H  
                 F 
                 F  
                 OH 
               
               
                 XXXI-3-6 
                   i Pr  
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H  
                 F 
                 F  
                 OH 
               
               
                 XXXI-3-7 
                   i Pr  
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H  
                 F 
                 F  
                 OH 
               
               
                 XXXI-3-8 
                   i Pr  
                 * 
                 H 
                 * 
                 CH 3   
                 H  
                 F 
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-4 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-4-1 
                   t Bu 
                 H  
                 H 
                 H 
                 CH 3   
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-4-2 
                   t Bu 
                 H  
                 H 
                 CH 3   
                 CH 3   
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-4-3 
                   t Bu 
                 H  
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-4 4 
                   t Bu 
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-4-5 
                   t Bu 
                 H  
                 H 
                 CH 2 Ph 
                 CH 3   
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-4-6 
                   t Bu 
                 H  
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-4-7 
                   t Bu 
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 H  
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-5 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-5-1  
                 Ph 
                 H 
                 H 
                 H 
                 CH 3    
                 H  
                 F 
                 F  
                 OH 
               
               
                 XXXI-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3    
                 H  
                 F 
                 F  
                 OH 
               
               
                 XXXI-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3    
                 H  
                 F 
                 F  
                 OH 
               
               
                 XXXI-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3    
                 H  
                 F 
                 F  
                 OH 
               
               
                 XXXI-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3    
                 H  
                 F 
                 F  
                 OH 
               
               
                 XXXI-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3    
                 H  
                 F 
                 F  
                 OH 
               
               
                 XXXI-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3    
                 H  
                 F 
                 F  
                 OH 
               
               
                 XXXI-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3    
                 H  
                 F 
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-6 
               
               
                   
               
               
                 N   o     
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-6-1 
                 p-Me-Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-6-2 
                 p-Me-Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-6-3 
                 p-Me-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-6-4 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-6-5 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-6-6 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-6-7 
                 p-Me-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-6-8 
                 p-Me-Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-7 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-7-1 
                 p-F-Ph 
                 H 
                 H 
                 H 
                 CH 3    
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-7-2 
                 p-F-Ph 
                 H 
                 H 
                 CH 3   
                 CH 3    
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-7-3 
                 p-F-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3    
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-7-4 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3    
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-7-6 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3    
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-7-7 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3    
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-7-8 
                 p-F-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3    
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-7-20 
                 p-F-Ph 
                 * 
                 H 
                 * 
                 CH 3    
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-8 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-8-1 
                 p-Cl-Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-8-2 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-8-3 
                 p-Cl-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-8-4 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-8-5 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-8-6 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-8-7 
                 p-Cl-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-8-8 
                 p-Cl-Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-9 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-9-1  
                 p-Br-Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-9-2 
                 p-Br-Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-9-3 
                 p-Br-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-9-4 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-9-6 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-9-7 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-9-8 
                 p-Br-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-9-20 
                 p-Br-Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H  
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-10 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-10-1 
                 p-I-Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXXI-10-2 
                 p-I-Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXXI-10-3 
                 p-I-Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXXI-10-4 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXXI-10-5 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXXI-10-6 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXXI-10-7 
                 p-I-Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 F  
                 F  
                 OH 
               
               
                 XXXI-10-8 
                 p-I-Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 F  
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-11 
               
               
                   
               
               
                 
                   N 
                   
                     o 
                   
                 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI- 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 16-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 16-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 16-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 16-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 16-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 F 
                 F 
                 H 
                 OH 
               
               
                 16-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 16-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 16-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI- 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 18-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 18-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 18-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 18-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 18-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 18-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 18-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 18-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI- 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 19-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 19-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 19-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 19-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 19-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 19-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 19-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 19-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-20 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-20-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-20-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-20-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-20-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-20-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-20-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-20-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-20-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-22 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-22-1 
                 Et 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-22-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-22-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-22-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-22-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-22-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-22-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-22-8 
                 Et 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI- 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 26-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 26-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 26-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 26-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 26-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 26-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 26-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXI- 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F 
                 F 
                 OH 
               
               
                 26-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXI-27-1 
                 p-F—Ph  
                 H 
                 H 
                 H 
                   i Pr  
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-27-2 
                 p-F—Ph  
                 H 
                 H 
                 CH 3   
                   i Pr  
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-27-3 
                 p-F—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr  
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-27-4 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr  
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-27-5 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 Ph 
                   i Pr  
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-27-6 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr  
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-27-7 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr  
                 H  
                 F  
                 F 
                 OH 
               
               
                 XXXI-27-8 
                 p-F—Ph  
                 * 
                 H 
                 * 
                   i Pr  
                 H  
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXI-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXI-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXI-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXI-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-32 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXI-32-1 
                 Et  
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-32-2 
                 Et  
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-32-3 
                 Et  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-32-4 
                 Et  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-32-5 
                 Et  
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-32-6 
                 Et  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-32-7 
                 Et  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-32-8 
                 Et  
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-33 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXI-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-34 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXI-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-35 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXI-35-1 
                 Ph  
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-35-2 
                 Ph  
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-35-3 
                 Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-35-4 
                 Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-35-5 
                 Ph  
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-35-6 
                 Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-35-7 
                 Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-35-8 
                 Ph  
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXI-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-37 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXI-37-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-37-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-37-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-37-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-37-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-37-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-37-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-37-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXI-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXI-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-39-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-40 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXI-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                 XXXI-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 F  
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXI-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-42 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-43 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-44 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-45 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-46 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-46-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-47 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-47-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-48 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-49 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXI-50 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXI-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                 XXXI-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 F 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-1 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-1-1 
                 CH 3   
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-1-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-1-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-1-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-1-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-1-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-1-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-1-8 
                 CH 3   
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-2 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-2-1 
                 Et 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-2-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-2 3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-2-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-2-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-2-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-2-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-2-8 
                 Et 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-3 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-3-1 
                   i Pr 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-3-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-3-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-3-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-3-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-3-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-3-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-3-8 
                   i Pr 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-4 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-4-1 
                   t Bu 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-4-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-4-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-4-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-4-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-4-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-4-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-4-8 
                   t Bu 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-5 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-5-1 
                 Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-5-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-5-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-5-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-5-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-5-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-5-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-5-8 
                 Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-6 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-6-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-6-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-6-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-6-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-6-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-6-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-6-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-6-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-7 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII- 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 7-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 7-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 7-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 7-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 7-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 7-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 7-8 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 7-20 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-8 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII- 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 8-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 8-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 8-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 8-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 8-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 8-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 8-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 8-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-9 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 9-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 9-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 9-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 9-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 9-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 9-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 9-8 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 9-20 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-10 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII- 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 10-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 10-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 10-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 10-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 10-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 10-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 10-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 CH 3   
                 H 
                 H 
                 F 
                 OH 
               
               
                 10-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-11 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-11-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-11-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-11-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-11-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-11-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-11-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-11-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-11-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-12 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-12-1 
                 Et 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-12-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-12-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-12-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-12-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-12-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-12-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-12-8 
                 Et 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-13 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-13-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-13-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-13-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-13-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-13-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-13-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-13-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-13-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-14 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-14-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-14-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-14-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-14-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-14-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-14-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-14-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-14-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-15 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-15-1 
                 Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-15-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-15-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-15-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-15-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-15-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-15-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-15-8 
                 Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-16 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII- 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 16-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 16-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 16-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 16-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 16-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 16-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 16-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 16-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-17 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-17-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-17-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-17-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-17-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-17-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-17-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-17-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-17-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-18 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII- 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 18-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 18-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 18-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 18-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 18-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 H 
                 Et 
                 H 
                 F 
                 OH 
               
               
                 18-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 18-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 18-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 19-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 19-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 19-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 19-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 19-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 19-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 19-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 19-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-19 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 19-1 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 19-2 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 19-3 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 19-4 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 19-5 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 19-6 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 19-7 
                   
                   
                   
                   
                   
                   
                   
                   
                   
               
               
                 XXXII- 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Et 
                 H 
                 H 
                 F 
                 OH 
               
               
                 19-8 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-21 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-21-1 
                 CH 3   
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-21-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-21-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-21-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-21-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-21-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-21-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-21-8 
                 CH 3   
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-22 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXII-22-1 
                 Et  
                 H  
                 H 
                 H 
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
               
               
                 XXXII-22-2 
                 Et  
                 H  
                 H 
                 CH 3   
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
               
               
                 XXXII-22-3 
                 Et  
                 H  
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
               
               
                 XXXII-22-4 
                 Et  
                 H  
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
               
               
                 XXXII-22-5 
                 Et  
                 H  
                 H 
                 CH 2 Ph 
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
               
               
                 XXXII-22-6 
                 Et  
                 H  
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
               
               
                 XXXII-22-7 
                 Et  
                 H  
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
               
               
                 XXXII-22-8 
                 Et  
                 * 
                 H 
                 * 
                   i Pr 
                 H  
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-23 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-23-1 
                   i Pr 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-23-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-23-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-23-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-23-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-23-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-23-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-23-8 
                   i Pr 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-24 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-24-1 
                   t Bu 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-24-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-24-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-24-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-24-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-24-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-24-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-24-8 
                   t Bu 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-25 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXII-25-1 
                 Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H  
                 H 
                 F  
                 OH 
               
               
                 XXXII-25-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H  
                 H 
                 F  
                 OH 
               
               
                 XXXII-25-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H  
                 H 
                 F  
                 OH 
               
               
                 XXXII-25-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H  
                 H 
                 F  
                 OH 
               
               
                 XXXII-25-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H  
                 H 
                 F  
                 OH 
               
               
                 XXXII-25-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H  
                 H 
                 F  
                 OH 
               
               
                 XXXII-25-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H  
                 H 
                 F  
                 OH 
               
               
                 XXXII-25-8 
                 Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H  
                 H 
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-26 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXII-26-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXXII-26-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXXII-26-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXXII-26-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXXII-26-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXXII-26-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXXII-26-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXXII-26-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-27 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXII-27-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXXII-27-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXXII-27-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXXII-27-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXXII-27-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXXII-27-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXXII-27-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
               
               
                 XXXII-27-8 
                 p-F—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-28 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-28-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-28-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-28-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-28-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-28-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-28-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-28-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-28-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-29 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-29-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-29-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-29-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-29-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-29-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-29-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-29-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-29-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and Rejoined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-30 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a    
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-30-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-30-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-30-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-30-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-30-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-30-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-30-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-30-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   i Pr 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-31 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-31-1 
                 CH 3   
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-31-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-31-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-31-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-31-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-31-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-31-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-31-8 
                 CH 3   
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-32 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-32-1 
                 Et 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-32-2 
                 Et 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-32-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-32-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-32-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-32-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-32-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-32-8 
                 Et 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-33 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-33-1 
                   i Pr 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-33-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-33-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-33-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-33-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-33-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-33-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-33-8 
                   i Pr 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-34 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-34-1 
                   t Bu 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-34-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-34-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-34-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-34-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-34-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-34-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-34-8 
                   t Bu 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-35 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-35-1 
                 Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-35-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-35-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-35-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-35-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-35-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-35-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-35-8 
                 Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-36 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-36-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-36-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-36-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-36-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-36-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-36-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-36-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-36-8 
                 p-Me—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-37 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R3 
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-37-1 
                 p-F—Ph  
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-37-2 
                 p-F—Ph  
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-37-3 
                 p-F—Ph  
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-37-4 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-37-5 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-37-6 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-37-7 
                 p-F—Ph  
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-37-8 
                 p-F—Ph  
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-38 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-38-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-38-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-38-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-38-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-38-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-38-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-38-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXH-38-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-39 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-39-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-39-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-39-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-39-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-39-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-39-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-39-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-39-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-40 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4    
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-40-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-40-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-40-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-40-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-40-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-40-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-40-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-40-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                   n Bu 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-41 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-41-1 
                 CH 3   
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-41-2 
                 CH 3   
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-41-3 
                 CH 3   
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-41-4 
                 CH 3   
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-41-5 
                 CH 3   
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-41-6 
                 CH 3   
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-41-7 
                 CH 3   
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-41-8 
                 CH 3   
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-42 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-42-1 
                 Et 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-42-2 
                 Et 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-42-3 
                 Et 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-42-4 
                 Et 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-42-5 
                 Et 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-42-6 
                 Et 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-42-7 
                 Et 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-42-8 
                 Et 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-43 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-43-1 
                   i Pr 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-43-2 
                   i Pr 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-43-3 
                   i Pr 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-43-4 
                   i Pr 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-43-5 
                   i Pr 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-43-6 
                   i Pr 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-43-7 
                   i Pr 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-43-8 
                   i Pr 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-44 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2    
                 R 3a    
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-44-1 
                   t Bu 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-44-2 
                   t Bu 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-44-3 
                   t Bu 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-44-4 
                   t Bu 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-44-5 
                   t Bu 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-44-6 
                   t Bu 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-44-7 
                   t Bu 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-44-8 
                   t Bu 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-45 
               
               
                   
               
               
                 No 
                 R 1    
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5    
                 R 6   
                 X  
                 Y 
               
               
                   
               
             
            
               
                 XXXII-45-1 
                 Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-45-2 
                 Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-45-3 
                 Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-45-4 
                 Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-45-5 
                 Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-45-6 
                 Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-45-7 
                 Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-45-8 
                 Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-46 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-46-1 
                 p-Me—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-46-2 
                 p-Me—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-46-3 
                 p-Me—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-46-4 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-46-5 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-46-6 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-46-7 
                 p-Me—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-46-8 
                 p-Me—Ph  
                 * 
                 H  
                 * 
                 Bz  
                 H  
                 H  
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-47 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2    
                 R 3a    
                 R 3b   
                 R 4    
                 R 5   
                 R 6    
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-47-1 
                 p-F—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-47-2 
                 p-F—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-47-3 
                 p-F—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-47-4 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-47-5 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-47-6 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-47-7 
                 p-F—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-47-8 
                 p-F—Ph 
                 * 
                 H  
                 * 
                 Bz  
                 H  
                 H  
                 F  
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-48 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-48-1 
                 p-Cl—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-48-2 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-48-3 
                 p-Cl—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-48-4 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-48-5 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-48-6 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-48-7 
                 p-Cl—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-48-8 
                 p-Cl—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-49 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-49-1 
                 p-Br—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-49-2 
                 p-Br—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-49-3 
                 p-Br—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-49-4 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-49-5 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-49-6 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-49-7 
                 p-Br—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-49-8 
                 p-Br—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     
       
         
           
               
               
               
               
               
               
               
               
               
               
             
               
                 TABLE XXXII-50 
               
               
                   
               
               
                 No 
                 R 1   
                 R 2   
                 R 3a   
                 R 3b   
                 R 4   
                 R 5   
                 R 6   
                 X 
                 Y 
               
               
                   
               
             
            
               
                 XXXII-50-1 
                 p-I—Ph 
                 H 
                 H 
                 H 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-50-2 
                 p-I—Ph 
                 H 
                 H 
                 CH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-50-3 
                 p-I—Ph 
                 H 
                 H 
                 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-50-4 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH(CH 3 ) 2   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-50-5 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 Ph 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-50-6 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 -indol-3-yl 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-50-7 
                 p-I—Ph 
                 H 
                 H 
                 CH 2 CH 2 SCH 3   
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                 XXXII-50-8 
                 p-I—Ph 
                 * 
                 H 
                 * 
                 Bz 
                 H 
                 H 
                 F 
                 OH 
               
               
                   
               
               
                 *R 2  and R 3b  joined together by (CH 2 ) 3  to form five-membered ring. 
               
            
           
         
       
     
     Dosage, Administration, and Use 
     A sixth embodiment of the present invention is directed to a composition for the treatment of any of the viral agents disclosed herein said composition comprising a pharmaceutically acceptable medium selected from among an excipient, carrier, diluent, and equivalent medium and a compound, that is intended to include its salts (acid or basic addition salts), hydrates, solvates, and crystalline forms can be obtained, represented by formula I. 
     It is contemplated that the formulation of the sixth embodiment can contain any of the compounds contemplated in any of the aspects of the first, second, third, fourth, and fifth embodiments or those specifically recited in the tables above or exemplified herein, either alone or in combination with another compound of the present invention. 
     The compounds of the present invention may be formulated in a wide variety of oral administration dosage forms and carriers. Oral administration can be in the form of tablets, coated tablets, hard and soft gelatin capsules, solutions, emulsions, syrups, or suspensions. Compounds of the present invention are efficacious when administered by suppository administration, among other routes of administration. The most convenient manner of administration is generally oral using a convenient daily dosing regimen which can be adjusted according to the severity of the disease and the patient&#39;s response to the antiviral medication. 
     A compound or compounds of the present invention, as well as their pharmaceutically acceptable salts, together with one or more conventional excipients, carriers, or diluents, may be placed into the form of pharmaceutical compositions and unit dosages. The pharmaceutical compositions and unit dosage forms may be comprised of conventional ingredients in conventional proportions, with or without additional active compounds and the unit dosage forms may contain any suitable effective amount of the active ingredient commensurate with the intended daily dosage range to be employed. The pharmaceutical compositions may be employed as solids, such as tablets or filled capsules, semisolids, powders, sustained release formulations, or liquids such as suspensions, emulsions, or filled capsules for oral use; or in the form of suppositories for rectal or vaginal administration. A typical preparation will contain from about 5% to about 95% active compound or compounds (w/w). The term “preparation” or “dosage form” is intended to include both solid and liquid formulations of the active compound and one skilled in the art will appreciate that an active ingredient can exist in different preparations depending on the desired dose and pharmacokinetic parameters. 
     The term “excipient” as used herein refers to a compound that is used to prepare a pharmaceutical composition, and is generally safe, non-toxic and neither biologically nor otherwise undesirable, and includes excipients that are acceptable for veterinary use as well as human pharmaceutical use. The compounds of this invention can be administered alone but will generally be administered in admixture with one or more suitable pharmaceutical excipients, diluents or carriers selected with regard to the intended route of administration and standard pharmaceutical practice. 
     A “pharmaceutically acceptable salt” form of an active ingredient may also initially confer a desirable pharmacokinetic property on the active ingredient which were absent in the non-salt form, and may even positively affect the pharmacodynamics of the active ingredient with respect to its therapeutic activity in the body. The phrase “pharmaceutically acceptable salt” of a compound as used herein means a salt that is pharmaceutically acceptable and that possesses the desired pharmacological activity of the parent compound. Such salts include: (1) acid addition salts, formed with inorganic acids such as hydrochloric acid, hydrobromic acid, sulfuric acid, nitric acid, phosphoric acid, and the like; or formed with organic acids such as glycolic acid, pyruvic acid, lactic acid, malonic acid, malic acid, maleic acid, fumaric acid, tartaric acid, citric acid, 3-(4-hydroxybenzoyl)benzoic acid, cinnamic acid, mandelic acid, methanesulfonic acid, ethanesulfonic acid, 1,2-ethane-disulfonic acid, 2-hydroxyethanesulfonic acid, benzenesulfonic acid, 4-chlorobenzenesulfonic acid, 2-naphthalenesulfonic acid, 4-toluenesulfonic acid, camphorsulfonic acid, lauryl sulfuric acid, gluconic acid, glutamic acid, salicylic acid, muconic acid, and the like or (2) basic addition salts formed with the conjugate bases of any of the inorganic acids listed above, wherein the conjugate bases comprise a cationic component selected from among Na + , K + , Mg 2+ , Ca 2+ , and NH g R′″ 4-g   + , in which R′″ is a C 1-3  alkyl and g is a number selected from among 0, 1, 2, 3, or 4. It should be understood that all references to pharmaceutically acceptable salts include solvent addition forms (solvates) or crystal forms (polymorphs) as defined herein, of the same acid addition salt. 
     Solid form preparations include powders, tablets, pills, capsules, suppositories, and dispersible granules. A solid carrier may be one or more substances which may also act as diluents, flavoring agents, solubilizers, lubricants, suspending agents, binders, preservatives, tablet disintegrating agents, or an encapsulating material. In powders, the carrier generally is a finely divided solid which is a mixture with the finely divided active component. In tablets, the active component generally is mixed with the carrier having the necessary binding capacity in suitable proportions and compacted in the shape and size desired. Suitable carriers include but are not limited to magnesium carbonate, magnesium stearate, talc, sugar, lactose, pectin, dextrin, starch, gelatin, tragacanth, methylcellulose, sodium carboxymethylcellulose, a low melting wax, cocoa butter, and the like. Solid form preparations may contain, in addition to the active component, colorants, flavors, stabilizers, buffers, artificial and natural sweeteners, dispersants, thickeners, solubilizing agents, and the like. 
     Liquid formulations also are suitable for oral administration include liquid formulation including emulsions, syrups, elixirs and aqueous suspensions. These include solid form preparations which are intended to be converted to liquid form preparations shortly before use. Emulsions may be prepared in solutions, for example, in aqueous propylene glycol solutions or may contain emulsifying agents such as lecithin, sorbitan monooleate, or acacia. Aqueous suspensions can be prepared by dispersing the finely divided active component in water with viscous material, such as natural or synthetic gums, resins, methylcellulose, sodium carboxymethylcellulose, and other well known suspending agents. 
     The compounds of the present invention may be formulated for administration as suppositories. A low melting wax, such as a mixture of fatty acid glycerides or cocoa butter is first melted and the active component is dispersed homogeneously, for example, by stirring. The molten homogeneous mixture is then poured into convenient sized molds, allowed to cool, and to solidify. 
     The compounds of the present invention may be formulated for vaginal administration. Pessaries, tampons, creams, gels, pastes, foams or sprays containing in addition to the active ingredient such carriers as are known in the art to be appropriate. 
     Suitable formulations along with pharmaceutical carriers, diluents and excipients are described in  Remington: The Science and Practice of Pharmacy  1995, edited by E. W. Martin, Mack Publishing Company, 19th edition, Easton, Pa., which is hereby incorporated by reference. The compounds of the present invention can also be encapsulated in liposomes, such as those disclosed in U.S. Pat. Nos. 6,180,134, 5,192,549, 5,376,380, 6,060,080, 6,132,763, each of which is incorporated by reference. A skilled formulation scientist may modify the formulations within the teachings of the specification to provide numerous formulations for a particular route of administration without rendering the compositions of the present invention unstable or compromising their therapeutic activity. 
     The modification of the present compounds to render them more soluble in water or other vehicle, for example, may be easily accomplished by minor modifications (e.g., salt formulation), which are well within the ordinary skill in the art. It is also well within the ordinary skill of the art to modify the route of administration and dosage regimen of a particular compound in order to manage the pharmacokinetics of the present compounds for maximum beneficial effect in patients. 
     A seventh embodiment of the present invention is directed to a use of the compound represented by formula I in the manufacture of a medicament for the treatment of any condition the result of an infection by any one of the following viral agents: hepatitis C virus, West Nile virus, yellow fever virus, dengue virus, rhinovirus, polio virus, hepatitis A virus, bovine viral diarrhea virus and Japanese encephalitis virus. 
     The term “medicament” means a substance used in a method of treatment and/or prophylaxis of a subject in need thereof, wherein the substance includes, but is not limited to, a composition, a formulation, a dosage form, and the like, comprising the compound of formula I. It is contemplated that the compound of the use of the compound represented by formula I in the manufacture of a medicament for the treatment of any of the antiviral conditions disclosed herein of the seventh embodiment can be any of the compounds contemplated in any of the aspects of the first, second, third, fourth, fifth embodiments or those specifically recited in the tables above or exemplified herein, either alone or in combination with another compound of the present invention. A medicament includes, but is not limited to, any one of the compositions contemplated by the sixth embodiment of the present invention. 
     A eighth embodiment of the present invention is directed to a method of treatment and/or prophylaxis in a subject in need thereof said method comprises administering a therapeutically effective amount of the compound represented by formula I to the subject. 
     A first aspect of the eighth embodiment is directed to a method of treatment and/or prophylaxis in a subject in need thereof said method comprises administering a therapeutically effective of at least two or more different compounds falling within the scope of the compound represented by formula I to the subject. 
     A second aspect of the eighth embodiment is directed to a method of treatment and/or prophylaxis in a subject in need thereof said method comprises alternatively or concurrently administering a therapeutically effective of at least two compounds falling within the scope of the compound represented by formula I to the subject. 
     It is intended that a subject in need thereof is one that has any condition the result of an infection by any of the viral agents disclosed herein, which includes, but is not limited to, hepatitis C virus, West Nile virus, yellow fever virus, dengue virus, rhinovirus, polio virus, hepatitis A virus, bovine viral diarrhea virus or Japanese encephalitis virus, flaviviridae viruses or pestiviruses or hepaciviruses or a viral agent causing symptoms equivalent or comparable to any of the above-listed viruses. 
     The term “subject” means a mammal, which includes, but is not limited to, cattle, pigs, sheep, chicken, turkey, buffalo, llama, ostrich, dogs, cats, and humans, preferably the subject is a human. It is contemplated that in the method of treating a subject thereof of the sixth embodiment can be any of the compounds contemplated in any of the aspects of the first, second, and third embodiments or those specifically recited in the tables above, either alone or in combination with another compound of the present invention. 
     The term “therapeutically effective amount” as used herein means an amount required to reduce symptoms of the disease in an individual. The dose will be adjusted to the individual requirements in each particular case. That dosage can vary within wide limits depending upon numerous factors such as the severity of the disease to be treated, the age and general health condition of the patient, other medicaments with which the patient is being treated, the route and form of administration and the preferences and experience of the medical practitioner involved. For oral administration, a daily dosage of between about 0.1 and about 10 g, including all values in between, such as 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5, 5.5, 6, 6.5, 7, 7.5, 8, 8.5, 9, and 9.5, per day should be appropriate in monotherapy and/or in combination therapy. A preferred daily dosage is between about 0.5 and about 7.5 g per day, more preferred 1.5 and about 6.0 g per day. Generally, treatment is initiated with a large initial “loading dose” to rapidly reduce or eliminate the virus following by a decreasing the dose to a level sufficient to prevent resurgence of the infection. One of ordinary skill in treating diseases described herein will be able, without undue experimentation and in reliance on personal knowledge, experience and the disclosures of this application, to ascertain a therapeutically effective amount of the compounds of the present invention for a given disease and patient. 
     Therapeutic efficacy can be ascertained from tests of liver function including, but not limited to protein levels such as serum proteins (e.g., albumin, clotting factors, alkaline phosphatase, aminotransferases (e.g., alanine transaminase, aspartate transaminase), 5′-nucleosidase, γ-glutaminyltranspeptidase, etc.), synthesis of bilirubin, synthesis of cholesterol, and synthesis of bile acids; a liver metabolic function, including, but not limited to, carbohydrate metabolism, amino acid and ammonia metabolism. Alternatively the therapeutic effectiveness may be monitored by measuring HCV-RNA. The results of these tests will allow the dose to be optimized. 
     A third aspect of the eighth embodiment, is directed to a method of treatment and/or prophylaxis in a subject in need thereof said method comprises administering to the subject a therapeutically effective of a compound represented by formula I and a therapeutically effective amount of another antiviral agent; wherein the administration is concurrent or alternative. It is understood that the time between alternative administration can range between 1-24 hours, which includes any sub-range in between including, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, and 23 hours. Examples of “another antiviral agents” include, but are not limited to: HCV NS3 protease inhibitors (see WO 2008010921, WO 2008010921, EP 1881001, WO 2007015824, WO 2007014925, WO 2007014926, WO 2007014921, WO 2007014920, WO 2007014922, US 2005267018, WO 2005095403, WO 2005037214, WO 2004094452, US 2003187018, WO 200364456, WO 2005028502, and WO 2003006490); HCV NS5B Inhibitors (see US 2007275947, US20072759300, WO2007095269, WO 2007092000, WO 2007076034, WO 200702602, US 2005-98125, WO 2006093801, US 2006166964, WO 2006065590, WO 2006065335, US 2006040927, US 2006040890, WO 2006020082, WO 2006012078, WO 2005123087, US 2005154056, US 2004229840, WO 2004065367, WO 2004003138, WO 2004002977, WO 2004002944, WO 2004002940, WO 2004000858, WO 2003105770, WO 2003010141, WO 2002057425, WO 2002057287, WO 2005021568, WO 2004041201, US 20060293306, US 20060194749, US 20060241064, U.S. Pat. No. 6,784,166, WO 2007088148, WO 2007039142, WO 2005103045, WO 2007039145, WO 2004096210, and WO 2003037895); HCV NS4 Inhibitors (see WO 2007070556 and WO 2005067900); HCV NS5a Inhibitors (see US 2006276511, WO 2006120252, WO 2006120251, WO 2006100310, WO 2006035061); Toll-like receptor agonists (see WO 2007093901); and other inhibitors (see WO 2004035571, WO 2004014852, WO 2004014313, WO 2004009020, WO 2003101993, WO 2000006529). 
     A fourth aspect of the eighth embodiment, is directed to a method of treatment in a subject in need thereof said method comprises alternatively or concurrently administering a therapeutically effective of a compound represented by formula I and another antiviral agent to the subject. It is understood that the time between alternative administration can range between 1-24 hours, which includes any sub-range in between including, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, and 23 hours. 
     A fifth aspect of the eighth embodiment, is directed to a method of treatment and/or prophylaxis in a subject in need thereof said method comprises administering to the subject a therapeutically effective of at least one compound represented by formula I and a therapeutically effective amount of another antiviral agent; wherein the administration is concurrent or alternative. It is understood that the time between alternative administration can range between 1-24 hours, which includes any sub-range in between including, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, and 23 hours. 
     A sixth aspect of the eighth embodiment, is directed to a method of treatment in a subject in need thereof said method comprises alternatively or concurrently administering a therapeutically effective of at least one compound represented by formula I and another antiviral agent to the subject. It is understood that the time between alternative administration can range between 1-24 hours, which includes any sub-range in between including, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, and 23 hours. 
     It is contemplated that the another antiviral agent includes, but is not limited to interferon-α, interferon-β, pegylated interferon-α, ribavirin, levovirin, viramidine, another nucleoside HCV polymerase inhibitor, a HCV non-nucleoside polymerase inhibitor, a HCV protease inhibitor, a HCV helicase inhibitor or a HCV fusion inhibitor. When the active compound or its derivative or salt are administered in combination with another antiviral agent the activity may be increased over the parent compound. When the treatment is combination therapy, such administration may be concurrent or sequential with respect to that of the nucleoside derivatives. “Concurrent administration” as used herein thus includes administration of the agents at the same time or at different times. Administration of two or more agents at the same time can be achieved by a single formulation containing two or more active ingredients or by substantially simultaneous administration of two or more dosage forms with a single active agent. 
     It will be understood that references herein to treatment extend to prophylaxis as well as to the treatment of existing conditions. Furthermore, the term “treatment” of a HCV infection, as used herein, also includes treatment or prophylaxis of a disease or a condition associated with or mediated by HCV infection, or the clinical symptoms thereof. 
     Process for Preparation 
     An ninth embodiment of the present invention is directed to a process for preparing the compound of formula I, which comprises reacting a suitably substituted phosphochloridate compound 4 with a nucleoside analog 5 
     
       
         
         
             
             
         
       
     
     wherein the substituents R 1 , R 2 , R 3a , R 3b , R 4 , R 5 , X, Y, R 6 , and base have their meanings as disclosed in the Detailed Description of the Invention and X′ is a leaving group, such as Cl, Br, I, tosylate, mesylate, trifluoroacetate, trifluorosulfonate, pentafluorophenoxide, p-NO 2 -phenoxide, or other commonly used leaving groups as disclosed in  Advanced Organic Chemistry  by March, Fourth Edition. Leaving groups and methods that can be used to effect the formation of a phosphoramidate nucleoside conjugate are found in US 20060142238 and WO 2007095269. Preferably, the leaving group is C 1 . 
     This reaction is performed in an anhydrous aprotic solvent such tetrahydrofuran, dioxane, or both tetrahydrofuran and dioxane, or any functional equivalent thereof, with tetrahydrofuran being the preferred solvent. The reaction is typically initiated at a temperature range from −78° C. to 40° C. with the preferred reaction temperature being between 0° C. and room temperature. The nucleoside is first stirred with a base (5 to 12 equivalents) such as N-methylimidazole, collidine, pyridine, 2,6-lutidine, 2, 6- t Bu-pyridine, etc. a tertiary amine base, such as triethylamine, diisopropylethylamine, etc., or an alkyl Grignard reagent, such as tBuMgCl, tBuMgBr, MeMgCl, MeMgBr, etc. The phosphorochloridate (3-10 equivalents) is dissolved in the reaction solvent and added to the mixture of the nucleoside and base. The reaction is then allowed to stir over a period of time at a temperature between room temperature and 40° C. for a period of 30 min to 24 hr. with the preferred reaction temperature being room temperature and time being 24 hr. The solvent is removed from the reaction mixture and the product is purified by chromatography on silica gel. 
     A tenth embodiment of the present invention is directed to a product obtained by a process which comprises reacting a suitably substituted phosphochloridate compound 4 with a nucleoside analog 5 
     
       
         
         
             
             
         
       
     
     wherein the substituents R 1 , R 2 , R 3a , R 3b , R 4 , R 5 , X, Y, R 6 , X′, and base have their meanings as disclosed in the Detailed Description of the Invention. 
     This reaction can be performed in an anhydrous aprotic solvent or other suitable solvent, such as tetrahydrofuran, dioxane, or a mixture of tetrahydrofuran and dioxane, with tetrahydrofuran being the preferred solvent. The reaction is typically initiated at a temperature range from −78° C. to 40° C. with the preferred reaction temperature being between 0° C. and room temperature. The nucleoside is first stirred with a base (5 to 12 equivalents) such as N-methylimidazole, a tertiary amine base or tButyl Magnesium Chloride. A phosphorochloridate (3-10 equivalents (or suitable “phosphoro-(leaving group)-date”)) is dissolved in the reaction solvent and added to the mixture of the nucleoside and base. The reaction is then allowed to stir over a period of time at a temperature between room temperature and 40° C. for a period of 30 min to 24 hr. with the preferred reaction temperature being room temperature and time being 24 hr. The solvent is removed from the reaction mixture and the product is purified by chromatography on silica gel. 
     Compounds and Preparation 
     Phosphoramidate compounds of the present invention can be prepared by condensation of a nucleoside analog 5 with a suitably substituted phosphochloridate compound 4 (Scheme 1). The nucleoside analog is made by conventional procedures disclosed in any one of U.S. Published Application Nos. 2005/0009737, 2006/0199783, 2006/0122146, and 2007/0197463, each of which is incorporated by reference in its entirety. 
     Disclosed 1H-NMR values were recorded on a Varian AS-400 instrument. Mass spectral data were obtain using either a Micromass-Quattromicro API or a Waters Acquity. 
     Thus, by way of example only, a suitably substituted phenol can be reacted with phosphorus oxychloride (1) to afford an aryloxy phosphorodichloridate 2 (see Example 1) which is subsequently treated with a acid addition salt of an α-amino acid ester in the presence of TEA to afford an aryloxy phosphorochloridate 4. This arylalkoxy-amino acid phosphoramidate is reacted with the nucleoside analog to provide the product I (for procedure see, e.g., C. McGuigan et al. Antiviral Res. 1992 17:311-321; D. Curley et al. Antiviral Res. 1990 14:345-356; McGuigan et al. Antiviral Chem. Chemother 1990 1(2):107-113). 
     
       
         
         
             
             
         
       
     
     The preparation of nucleoside phosphoramidates requires reacting an appropriately substituted phosphochloridate with a nucleoside containing a free 5′-hydroxyl moiety. In cases where only one hydroxyl group is present, preparation of the phosphoramidate usually proceeds smoothly when the phosphochloridate is reacted with the desired nucleoside. In cases where the nucleoside contains more than one free hydroxyl group, preparation of the appropriately protected nucleoside might be required. Silyl, acetonide or other alcohol protecting groups known in the art might be warranted for protection of the sugar moiety. For protection of the nucleoside base, protecting a free amino group may require amidine protection strategy. 
     Condensation of the phosphochloridate can be carried out on the unprotected nucleoside. Since the 5′-OH group of a nucleoside is much less hindered than the 3′-OH group, selective phosphoramidation is possible under carefully controlled conditions. After condensation to form a protected phosphoramidate nucleoside, deprotection to obtain the free phosphoramidate nucleoside can be carried out using standard protocols for nucleic acid chemistry. In many cases, the desired product is readily separated from the starting material using column chromatography on silica gel. The synthetic scheme is summarized in Scheme 1. 
     A further understanding of the disclosed embodiments will be appreciated by consideration of the following examples, which are only meant to be illustrative, and not limit the disclosed invention. 
     Example 1 
     General Procedure for Preparation of Phosphorodichloridates 
     
       
         
         
             
             
         
       
     
     A solution of the appropriate phenol R 1 —OH (1 eq) and triethylamine (1 eq.) in anhydrous ether was added dropwise to a stirred solution of phosphoryl trichloride 1 (1 eq) at 0° C. over a period of 3 hours under nitrogen. Then the temperature was warmed to room temperature, and the reaction was stirred overnight. The triethylamine salt was quickly removed with suction filtration and the filtrate concentrated in vacuo to dryness to afford 2 as an oil which was used without further purification. 
     Example 2 
     General Procedure for Preparation of Phosphorochloridates 
     
       
         
         
             
             
         
       
     
     A solution of triethylamine (2 eq) in anhydrous dichloromethane was added dropwise to a solution of aryloxy-phosphodichloridate 2 (1 eq) and the appropriate amino ester 3 (1 eq) in anhydrous dichloromethane with vigorous stirring at −78° C. over a period of 30 to 120 minutes. Then the reaction temperature was allowed to warm to room temperature and stirred over night. Solvent was removed. The residue was washed with ethyl ether and filtered, the filtrate was dried over reduced pressure to give 4. 
     Example 3 
     General Procedures for Nucleoside Phosphoramidate Derivatives 
     
       
         
         
             
             
         
       
     
     A solution of the appropriate phosphorochloridate 4 (6.5 equivalents) in anhydrous tetrahydrofuran (THF) was added to a mixture of nucleoside 5 (1 equivalent) and N-methylimidazole (8 equivalents) in anhydrous THF with vigorous stirring at room temperature and the reaction mixture was stirred overnight. The solvent was removed in vacuo and the crude was purified by column chromatography and/or preparative thin layer chromatography to give I. 
     Example 4 
     Preparation of 2′-deoxy-2′-fluoro-2′-C-methyluridine 
     
       
         
         
             
             
         
       
     
     2′-Deoxy-2′-fluoro-2′-C-methylcytidine (1.0 g, 1 eq) (Clark, J., et al., J. Med. Chem., 2005, 48, 5504-5508) was dissolved in 10 ml of anhydrous pyridine and concentrated to dryness in vacuo. The resulting syrup was dissolved in 20 ml of anhydrous pyridine under nitrogen and cooled to 0° C. with stirring. The brown solution was treated with benzoyl chloride (1.63 g, 3 eq) dropwise over 10 min. The ice bath was removed and stirring continued for 1.5 h whereby thin-layer chromatography (TLC) showed no remaining starting material. The mixture was quenched by addition of water (0.5 ml) and concentrated to dryness. The residue was dissolved in 50 mL of dichloromethane (DCM) and washed with saturated NaHCO 3  aqueous solution and H 2 O. The organic phase was dried over NaSO 4  and filtered, concentrated to dryness to give N 4 ,3′,5′-tribenzoyl-2′-Deoxy-2′-fluoro-2′-C-methylcytidine (2.0 g, Yield: 91%). 
     N 4 ,3′,5′-tribenzoyl-2′-Deoxy-2′-fluoro-2′-C-methylcytidine (2.0 g, 1 eq) was refluxed in 80% aqueous AcOH overnight. After cooling and standing at room temperature (15° C.), most of the product precipitated and then was filtered through a sintered funnel. White precipitate was washed with water and co-evaporated with toluene to give a white solid. The filtrate was concentrated and co-evaporated with toluene to give additional product which was washed with water to give a white solid. Combining the two batches of white solid gave 1.50 g of 3′,5′-dibenzoyl-2′-Deoxy-2′-fluoro-2′-C-methyluridine (Yield: 91%). 
     To a solution of 3′,5′-dibenzoyl-2′-Deoxy-2′-fluoro-2′-C-methyluridine (1.5 g, 1 eq) in MeOH (10 mL) was added a solution of saturated ammonia in MeOH (20 mL). The reaction mixture was stirred at 0° C. for 30 min, and then warmed to room temperature slowly. After the reaction mixture was stirred for another 18 hours, the reaction mixture was evaporated under reduced pressure to give the residue, which was purified by column chromatography to afford pure compound 2′-deoxy-2′-fluoro-2′-C-methyluridine (500 mg, Yield: 60%). 
     Example 5 
     Preparation of 2′-Deoxy-2′-fluoro-2′-C-methyluridine 5′-(phenyl methoxy-alanyl Phosphate) 
     
       
         
         
             
             
         
       
     
     Phenyl methoxyalaninyl phosphorochloridate (1 g, 6.5 eq) dissolved in 3 mL of THF was added to a mixture of 2′-Deoxy-2′-fluoro-2′-C-methyluridine (0.15 g, 1 eq) and N-methylimidazole (0.3 g, 8 eq) in 3 mL THF with vigorous stirring at room temperature, then the reaction was stirred overnight. Solvent was removed by reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25×30×2 mm column using a water/acetonitrile gradient elution mobile phase. The acetonitrile and water were removed under reduced pressure to give the desired product (50.1 mg, 15.6%).  1 H NMR (DMSO-d 6 ) δ 1.20-1.27 (m, 6H), 3.58 (d, J=16.0 Hz, 3H), 3.75-3.92 (m, 2H), 4.015-4.379 (m, 2H), 5.54 (t, J=10.2 Hz, 1H), 5.83-5.91 (m, 1H), 6.00-6.16 (m, 1H), 7.18 (d, J=8.0 Hz, 2H), 7.22 (s, 1H), 7.35 (t, J=4.4 Hz, 2H), 7.55 (s, 1H), 11.52 (s, 1H); MS, m/e 502 (M+1) + . 
     Example 6 
     Preparation of 2′-Deoxy-2′-fluoro-2′-C-methyluridine 5′-(phenyl methoxy-valyl Phosphate) 
     
       
         
         
             
             
         
       
     
     Phenyl methoxy-valyl phosphorochloridate (0.6 g, 3.6 eq) dissolved in 3 mL of THF was added to a mixture of 2′-Deoxy-2′-fluoro-2′-C-methyluridine (0.15 g, 1 eq) and N-methylimidazole (0.44 g, 9 eq) in 3 mL THF with vigorous stirring at room temperature, then the reaction was stirred overnight. Solvent was removed by reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25×30×2 mm column using a water/acetonitrile gradient elution mobile phase. The acetonitrile and water were removed under reduced pressure to give the desired product (60 mg, 20%).  1 H NMR (DMSO-d 6 ) δ 0.74-0.847 (m, 6H), 1.20-1.28 (m, 3H), 1.89-1.92 (m, 1H), 3.50-3.54 (m, 1H), 3.58 (d, J=10.4 Hz, 3H), 3.72-3.95 (m, 1H), 4.03-4.05 (m, 1H), 4.23-4.43 (m, 2H), 5.56 (t, J=16.0 Hz, 1H), 5.85-5.92 (m, 1H), 6.01-6.07 (m, 1H), 7.16-7.21 (m, 3H), 7.37 (t, J=8 Hz, 2H), 7.55-7.60 (m, 1H), 11.52 (s, 1H); MS, m/e 530 (M+1) + . 
     Example 7 
     Preparation of 2′-Deoxy-2′-fluoro-2′-C-methyluridine 5′-(4-bromophenyl methoxy-valyl Phosphate) 
     
       
         
         
             
             
         
       
     
     4-Bromophenyl methoxy-valyl phosphorochloridate (1 g, 3.4 eq) dissolved in 3 mL of THF was added to a mixture of 2′-deoxy-2′-fluoro-2′-C-methyluridine (0.2 g, 1 eq) and N-methylimidazole (0.35 g, 6 eq) in 3 mL THF with vigorous stirring at room temperature, then the reaction was stirred overnight. Solvent was removed by reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25×30×2 mm column using a water/acetonitrile gradient elution mobile phase. The acetonitrile and water were removed reduced pressure to give the desired product (120 mg, 26%).  1 H NMR (DMSO-d 6 ) δ 0.72-0.82 (m, 6H), 1.19-1.26 (m, 3H), 1.86-1.92 (m, 1H), 3.48-3.50 (m, 1H), 3.56 (d, J=12.0 Hz, 3H), 3.72-3.89 (m, 1H), 3.96-4.03 (m, 1H), 4.22-4.37 (m, 2H), 5.54-5.60 (m, 1H), 5.85-5.91 (m, 1H), 5.98-6.13 (m, 1H), 7.15 (d, J=8.0 Hz, 2H), 7.49-7.56 (m, 3H), 11.53 (s, 1H); MS, m/e 608 (M+1) + . 
     Example 8 
     Preparation of 2′-Deoxy-2′-fluoro-2′-C-methyluridine 5′-(4-bromophenyl methoxy-alanyl Phosphate) 
     
       
         
         
             
             
         
       
     
     4-Bromophenyl methoxy-alanyl phosphorochloridate (0.6 g, 5 eq) dissolved in 3 mL of THF was added to a mixture of 2′-deoxy-2′-fluoro-2′-C-methyluridine (0.15 g, 1 eq) and N-methylimidazole (0.3 g, 7.8 eq) in 3 mL THF with vigorous stirring at room temperature, then the reaction was stirred overnight. Solvent was removed by reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25×30×2 mm column using a water/acetonitrile gradient elution mobile phase. The acetonitrile and water were removed under reduced pressure to give the desired product (40 mg, 12%);  1 H NMR (DMSO-d 6 ) δ 1.20-1.26 (m, 6H), 3.57 (d, J=2.8 Hz, 3H), 3.84 (s, 1H), 3.97-4.03 (m, 1H), 4.21-4.25 (m, 1H), 4.33-4.37 (m, 2H), 5.54-5.60 (m, 1H), 5.83-5.89 (m, 1H), 5.98-6.19 (m, 1H), 7.16 (t, J=10.2 Hz, 2H), 7.52-7.57 (m, 3H), 11.52 (s, 1H); MS, m/e 580 (M+1) + . 
     Example 9 
     Preparation of N 4 —(N,N-dimethylformamidinyl)-2′-deoxy-2′-fluoro-2′-C-methylcytidine 
     
       
         
         
             
             
         
       
     
     2′-Deoxy-2′-fluoro-2′-C-methylcytidine (500 mg, 1.9 mmol) was stirred with dimethylformamide dimethyl acetal in DMF (10 mL). The resulting mixture was stirred at room temperature overnight. After solvent removal the crude product was used for next step without further purification. 
     Example 10 
     Preparation of 2′-Deoxy-2′-fluoro-2′-C-methylcytidine 5′-(phenyl methoxy-alanyl Phosphate) 
     
       
         
         
             
             
         
       
     
     Phenyl methoxyalaninyl phosphorochloridate (0.6 g, 6 eq) dissolved in 3 mL of THF was added to a mixture of N 4 —(N,N-dimethylformamidinyl)-2′-deoxy-2′-fluoro-2′-C-methylcytidine (0.15 g, 1 eq) and N-methylimidazole (0.3 g, 7.8 eq) in 3 mL THF with vigorous stirring at room temperature, then the reaction was stirred overnight. Solvent was removed by reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25×30×2 mm column using a water/acetonitrile gradient elution mobile phase. The acetonitrile and water were removed under reduced pressure to give the desired product (62 mg, 20.6%).  1 H NMR (DMSO-d 6 ) δ 1.16 (d, J=23.2 Hz, 3H), 1.22 (d, J=7.2 Hz, 3H), 3.56 (S, 3H), 3.69-3.75 (d, J=25.6 Hz, 1H), 3.82-3.86 (m, 1H), 3.96-3.98 (m, 1H), 4.21-4.34 (m, 2H), 5.68 (d, J=7.2 Hz, 1H), 5.75-5.77 (m, 1H), 6.07-6.16 (m, 1H), 7.15-7.19 (m, 3H), 7.2 (d, J=9.2 Hz, 2H), 7.39 (t, J=7.8 Hz, 2H), 7.48 (d, J=9.2 Hz, 1H); MS, m/e 501 (M+1) + . 
     Example 11 
     Preparation of 2′-Deoxy-2′-fluoro-2′-C-methylcytidine 5′-(4-bromophenyl methoxy-valyl Phosphate) 
     
       
         
         
             
             
         
       
     
     4-Bromophenyl methoxy-valyl phosphorochloridate (1.0 g, 3.4 eq.) dissolved in 3 mL of THF was added to a mixture of N 4 —(N,N-dimethylformamidinyl)-2′-deoxy-2′-fluoro-2′-C-methylcytidine (0.2 g, 1 eq.) and N-methylimidazole (0.35 g, 6 eq.) in 3 mL THF with vigorous stirring at room temperature, then the reaction was stirred overnight. Solvent was removed by reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25×30×2 mm column using a water/acetonitrile gradient elution mobile phase. The acetonitrile and water were removed under reduced pressure to give the desired product as a white solid (59 mg, 13%);  1 H NMR (DMSO-d 6 ) δ 0.74-0.83 (m, 6H), 1.12-1.20 (m, 3H), 1.89-1.92 (m, 1H), 3.49-3.51 (m, 1H), 3.55 (s, 3H), 3.59-3.68 (m, 1H), 3.72-0.383 (m, 1H), 4.21-4.39 (m, 2H), 5.70-5.72 (m, 1H), 5.76-5.83 (m, 1H), 6.04-6.16 (m, 1H), 7.15 (d, J 13.0 Hz, 2H), 7.26 (s, 1H), 7.33 (s, 1H), 7.46-7.55 (m, 1H), 7.56 (d, J=4.4 Hz, 2H); MS, m/e 607 (M+1) + . 
     Example 12 
     Preparation of 2′-deoxy-2′-fluoro-2′-C-methylcytidine 5′-(phenyl methoxy-valyl Phosphate) 
     
       
         
         
             
             
         
       
     
     Phenyl methoxy-valyl phosphorochloridate (0.6 g, 6 eq) dissolved in 3 mL of THF was added to a mixture of N 4 —(N,N-dimethylformamidinyl)-2′-deoxy-2′-fluoro-2′-C-methylcytidine (0.15 g, 1 eq) and N-methylimidazole (0.3 g, 7.8 eq) in 3 mL THF with vigorous stirring at room temperature, then the reaction was stirred overnight. Solvent was removed by reduced pressure The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25×30×2 mm column using a water/acetonitrile gradient elution mobile phase. The acetonitrile and water were removed under reduced pressure to give the desired product as a white solid (86 mg, 42.9%).  1 H NMR (DMSO-d 6 ) δ 0.72-0.80 (m, 6H), 1.09-1.18 (m, 3H), 1.87-1.92 (m, 1H), 3.47-3.51 (m, 1H), 3.58 (s, 3H), 3.71-3.75 (m, 1H), 3.97 (t, J=11.2 Hz, 1H), 4.22-4.37 (m, 2H), 5.70 (d, J=8.0 Hz, 1H), 5.76-5.84 (m, 1H), 6.01-6.15 (m, 1H), 7.13-7.18 (m, 3H), 7.27 (s, 2H), 7.34 (d, J=4.0 Hz, 2H), 7.46-7.50 (m, 1H): MS, m/e 529 (M+1) + . 
     Examples 
     Example numbers 13-54 and 56-66 are prepared using similar procedures described for examples 5-8. The example number, compound identification, and NMR/MS details are shown below: 
     
       
         
         
             
             
         
       
     
                                                     Ex.   R 1     R 2     R 3a     R 3b     R 4     NMR/MS                  13   Ph   H   H   Me   Et   1H NMR (DMSO-d 6 ) δ 1.12-1.16 (m, 3H), 1.20-1.28(m, 6H), 3.70-                               3.90 (m, 2H), 4.00-4.08 (m, 3H), 4.18-4.45 (m, 2H), 5.52-5.58 (m, 1H),                               5.85-5.98 (m, 1H), 6.00-6.20 (m, 2H), 7.16-7.23 (m, 3H), 7.37-7.40                               (m, 2H), 7.54-7.60 (m, 1H), 11.54 (s, 1H); MS, m/e 516.1 (M + 1) +       14   1-Napth   H   H   Me   Bn   1H NMR (DMSO-d 6 ) δ 1.18-1.30 (m, 6H), 3.78-4.10 (m, 3H), 4.38-                               4.49 (m, 2H), 4.99-5.11 (m, 2H), 5.28-5.40 (m, 1H), 5.85-6.10 (m,                               2H), 6.30-6.41 (m, 1H), 7.28-7.32 (m, 5H), 7.41-7.60 (m, 5H), 7.73-                               7.76(m, 1H), 7.94-8.1l(m, 1H), 8.13-8.15(m, 1H), 11.50 (s, 1H);                               MS, m/e 628.4 (M + 1) +       15   Ph   H   H   H   Me   1H NMR (DMSO-d 6 ) δ 1.22 (d, J = 22.4 Hz, 3H), 3.59(s, 3H), 3.63-                               3.69 (m, 2H), 3.74-3.8(m, 1H), 4.02(d, J = 11.2 Hz, 1H), 4.23-4.28(m,                                1H), 4.40-4.43 (m, 1H), 5.57-5.60 (m, 1H), 5.89(d, J = 6.8 Hz, 1H),                                6.00-6.06(m, 2H), 7.15-7.23 (m, 3H), 7.35-7.39 (m, 2H), 7.52(d, J = 8                                Hz, 1H), 11.52(s, 1H); MS, m/e 487.97 (M + 1) +       16   2,4-   H   H   Me   Me   1H NMR (DMSO-d 6 ) δ 1.22-1.28 (m, 6H), 3.57-3.60 (m, 3H), 3.84-           Cl—Ph                   3.92 (m, 2H), 4.00-4.04 (m, 1H), 4.31-4.44 (m, 2H), 5.54-5.61 (m,                               1H), 5.85-6.10 (m, 2H), 6.32-6.43 (m, 1H), 7.44-7.54 (m, 3H), 7.72-                               7.75 (m, 1H), 11.54 (s, 1H); MS, m/e 570.2 (M + 1) +       17   1-Napth   H   H   Me   Me   1H NMR (DMSO-d 6 ) δ 1.15-1.27 (m, 6H), 3.51-3.55 (d, 3H), 3.85-                               3.96 (m, 2H), 4.00-4.10(m, 1H), 4.30-4.46 (m, 2H), 5.31-5.39 (m, 1H),                               5.89-6.05 (m, 2H), 6.22-6.34 (m, 1H), 7.44-7.60 (m, 5H), 7.73-7.77                               (m, 1H), 7.93-7.96 (m, 1H), 8.12-8.14 (m, 1H), 11.50(s, 1H); MS, m/e                               552.1 (M + 1) +       18   Ph   *   H   *   Me   1H NMR (DMSO-d 6 ) δ 1.19 (d, J = 22.8 Hz, 3H), 1.69-1.84 (m, 3H),                               1.99-2.04 (m, 1H), 3.16-3.21 (m, 2H), 3.58 (s, 3H), 3.68-3.8 (m, 1H),                               4.00 (m, 1H), 4.01-4.13 (m, 1H), 4.22-4.25 (m, 1 H), 4.5 (d, J = 11.2                               Hz, 1H), 5.54 (d, J = 8.0 Hz, 1H), 5.86 (s, 1H), 5.6 (d, J = 19.6 Hz,                               1H), 7.15-7.2 (m, 3H), 7.34 (t, J = 8.0 Hz, 2H), 7.51 (d, J = 8.0 Hz,                               1H), 11.38 (s, 1H); MS, m/e 527.93(M + 1) +       19   Ph   H   H   Me   n-Bu   1H NMR (DMSO-d 6 ) δ 0.80-0.90 (m, 3H), 1.20-1.35 (m, 8H), 1.48-                               1.55 (m, 2H), 3.78-3.88 (m, 2H), 3.95-4.08 (m, 3H), 4.22-4.45 (m,                               2H), 5.55-5.57(t, 1H), 5.85-6.18 (m, 3H), 7.14-7.23 (m, 3H), 7.35-7.40                               (m, 2H), 7.51-7.60 (d, 1H), 11.50 (s, 1H); MS, m/e 544.2 (M + 1) +       20   Ph   H   H   Me   Bn   1H NMR (DMSO-d 6 ) δ 1.20-1.30 (m, 6H), 3.72-4.05 (m, 3H), 4.23-                               4.27 (m, 1H), 4.32-4.45 (m, 1H), 5.07-5.10(t, 2H), 5.52-5.56(t, 1H),                               5.86-6.10 (m, 2H), 6.13-6.21(m, 1H), 7.15-7.21 (m, 3H), 7.29-7.40 (m,                               7H), 7.51-7.56 (d, 1H), 11.50 (s, 1H); MS, m/e 578.2 (M + 1) +       21   4-F—Ph   H   H   Me   Me   1H NMR (DMSO-d 6 ) δ 1.28-1.34 (m, 6H), 3.65(d, J = 4 Hz, 3H), 3.85-                               3.96 (m, 2H), 4.06-4.12 (m, 1H), 4.30-4.34 (m, 1H), 4.40-4.47 (m, 1H),                               5.62-5.67 (m, 1H), 5.94-6.01(m, 1H), 6.09 (d, J = 18.8 Hz, 1H), 6.17-                               6.26 (m, 1H), 7.27-7.33(m, 4H), 7.62 (d, J = 7.6 Hz, 1H), 11.61 (s, 1H);                               MS, m/e 519.94(M + 1) +       22   4-Cl—Ph   H   H   Me   Me   1H NMR (DMSO-d 6 ) δ 1.22-1.28 (m, 6H), 3.58 (d, 2H), 3.70-                               3.95(m, 2H), 3.95-4.08 (m, 1H), 4.23-4.45 (m, 2H), 5.55-5.61(t, 1H),                               5.85-6.10 (m, 2H), 6.15-6.23(m, 1H), 7.20-7.26 (m, 2H), 7.43-7.46 (m,                               2H), 7.54-7.57 (d, 1H), 11.50 (s, 1H); MS, m/e 536.1 (M + 1) +       23   3,4-   H   H   Me   Me   1H NMR (DMSO-d 6 ) δ 1.13 (m, 6H), 3.49 (s, 3H), 3.61-3.85 (m, 2H),           Cl—Ph                   3.90-3.93 (m, 1H), 4.16-4.22 (m, 1H), 4.27-4.31 (m, 1H), 5.47-5.52                               (m, 1H), 5.82 (d, J = 11.6 Hz, 1H), 5.93(d, J = 19.2 Hz, 1H), 6.15-6.25                               (m, 1H), 7.13 (t, J = 9.6 Hz, 1H), 7.43 (d, J = 12 Hz, 2H), 7.57 (d, J =                               6.0 Hz, 1H), 11.43(s, 1H); MS, m/e 569.85 (M + 1) +       24   Ph   H   H   Me   2-Bu   1H NMR (DMSO-d 6 ) δ 0.83 (d, J = 6.8 Hz, 6H), 1.20-1.26 (m, 6H),                               1.79-1.86 (m, 1H), 3.73-3.90 (m, 4H), 4.01 (t, J = 11.2 Hz, 1H),4.21-                               4.28 (m, 1H), 4.33-4.42 (m, 1H), 5.54 (t, J = 7.6 Hz, 1H), 5.85-5.92                               (m, 1H), 5.99-6.13 (m, 2H), 7.19 (t, J = 8 Hz, 3H), 7.36 (t, J = 7.6 Hz,                               2H), 7.53 (d, J = 7.6 Hz, 1H), 11.52 (s, 1H); MS, m/e 544.00 (M + 1) +       25   Ph   H   H   Me   i-Pr   1H NMR (DMSO-d 6 ) δ 1.13-1.28 (m, 12H), 3.74-3.81 (m, 2H), 3.95-                               4.08 (m, 1H), 4.20-4.45 (m, 2H), 4.83-4.87 (m, 1H), 5.52-5.58 (m, 1H),                               5.84-6.15 (m, 3H), 7.17-7.23 (m, 3H), 7.35-7.39 (m, 2H), 7.54-7.57                               (m, 1H), 11.50 (s, 1H); MS, m/e 530.2 (M + 1) +       26   4-   H   H   Me   n-Bu   1HNMR (400 MHz, DMSO-d 6 ): δ = 0.78-0.82 (m, 3H), 1.29-1.47 (m,           MeO—Ph                   8H), 1.49-1.54 (m, 2H), 3.66-3.87 (m, 5H), 3.96-4.02 (m, 3H), 4.21-                               4.39 (m, 2H), 5.57 (t, J = 12.0 Hz, 1H), 5.84-6.05 (m, 3H), 6.90 (dd,                                J1 = 8.0 Hz, J2 = 4.0 Hz, 2H), 7.09-7.14 (dd, J1 = 16.0 Hz, J2 = 4.0                                Hz, 2H), 7.55 (d, J = 8.0 Hz, 1H), 11.48-11.62 (s, 1H)       27   4-F—Ph   H   H   Me   Et   1H NMR (DMSO-d 6 ) δ 1.12-1.28 (m, 9H), 3.72-3.94(m, 2H), 3.98-                               4.10 (m, 3H), 4.21-4.42(m, 2H), 5.55-5.61 (t, 1H), 5.85-6.20 (m, 3H),                                7.18-7.25 (m, 4H), 7.55-7.58 (d, 1H), 11.50 (s, 1H); MS, m/e 533.90                                (M + 1) +       28   4-F—Ph   H   H   Me   i-Pr   1H NMR (DMSO-d 6 ) δ 1.13-1.30 (m, 12H), 3.74-3.85(m, 2H), 3.98-                               4.06 (m, 1H), 4.23-4.41(m, 2H), 4.83-4.87 (m, 1H), 5.55-5.61 (t, 1H),                               5.85-6.12 (m, 3H), 7.18-7.24 (m, 4H), 7.55-7.58 (d, 1H), 11.50 (s, 1H);                               MS, m/e 547.91 (M + 1) +       29   4-F—Ph   H   H   Me   Bn   1H NMR (DMSO-d 6 ) δ 1.10-1.23 (m, 6H), 3.65-3.89(m, 3H), 4.10-4.30                               (m, 2H), 4.96-5.00(m, 2H), 5.46-5.50 (t, 1H), 5.75-5.96 (m, 2H), 6.04-                               6.12(m, 1H), 7.05-7.11 (m, 4H), 7.20-7.24 (d, 5H), 7.42-7.45(d, 1H),                               11.50 (s, 1H); MS, m/e 595.94 (M + 1) +       30   4-   H   H   Me   i-Pr   1HNMR (400 MHz, DMSO-d 6 ): δ = 1.15-1.27 (m, 12H), 3.71-3.89 (m,           MeO—Ph                   5H), 3.98-4.02 (m, 1H), 4.22-4.25 (m, 1H), 4.33-4.39 (m, 1H), 4.84-                               4.87 (m, 1H), 5.57 (t, J = 12.0 Hz, 1H), 5.91-6.03 (m, 3H), 6.90 (d, J =                               8.0 Hz, 2H), 7.09-7.14 (m, 2H), 7.55 (d, J = 8.0 Hz, 1H), 11.51 (s, 1H)       31   2-Cl—Ph   H   H   Me   Bn   1H NMR (DMSO-d 6 ) δ 1.23 (m, 6 H), 3.93-4.00 (m, 3 H), 4.27-4.40                               (m, 2H), 5.0(t, J = 7.2 Hz, 2 H), 5.53 (m, 1 H), 5.80-6.0(m, 2 H),                               6.30(m, 1H), 7.15 (d, J = 2.4 Hz, 1 H), 7.27 (m, 6 H), 7.51 (m, 3 H),                               11.5 (s, 1 H); MS, m/e 579.87(M + 1)+/596.78 (M + 18) +       32   2,4-   H   H   Me   n-Bu   1H NMR (DMSO-d 6 ) δ = 0.82 (m, 3 H),1.23 (m, 8 H), 1.47 (m, 2 H),           Cl—Ph                   3.86 (m, 2 H), 3.84 (m, 3 H), 4.27-4.43 (m, 2H), 5.5 (m, 1 H), 6.02 (m,                               2 H), 6.35(m, 1H), 7.44 (m, 3 H), 7.77 (m, 1 H), 11.5 (s, 1 H); MS,                               m/e 611.87(M + 1) +       33   4-   H   H   Me   i-Pr   1H NMR (DMSO-d 6 ) δ 1.14-1.27 (m, 12H), 2.17-2.26 (m, 3H), 3.73-           Me—Ph                   3.82 (m, 1H), 3.99-4.02 (m, 1H), 4.23-4.26 (m, 1H), 4.37-4.40 (m,                               1H), 4.82-4.88 (m, 1H), 5.52-5.58 (m, 1H), 5.85-6.07 (m, 3H), 7.01-                               7.20 (m, 4H), 7.55 (d, J = 16 Hz, 1H), 11.51 (s, 1H); MS, m/e 543.98                               (M + 1) +; 1108.86 (2M + 23) +       34   4-F—Ph   H   H   Me   n-Bu   1H NMR (DMSO-d 6 ) δ 0.82-0.89 (m, 3H), 1.20-1.31 (m, 8H), 1.48-                               1.53 (m, 2H), 3.77-3.90 (m, 2H), 3.95-4.10 (m, 3H), 4.21-4.45(m, 2H),                               5.56-5.61 (t, 1H), 5.83-6.20 (m, 3H), 7.18-7.25 (m, 4H), 7.55-7.58 (d,                               1H), 11.50 (s, 1H); MS, m/e 584.1 (M + 23) +       35   3,4-   H   H   Me   Et   1H NMR (DMSO-d 6 ) δ1.12-1.31 (m, 9H), 3.77-3.92 (m, 2H), 3.95-           diCl—Ph                   4.08 (m, 3H), 4.21-4.45(m, 2H), 5.56-5.62 (t, 1H), 5.80-6.11 (m, 2H),                                6.18-6.33(m, 1H), 7.18-7.25 (m, 1H), 7.49-7.56 (d, 2H), 7.62-7.67(m,                                1H), 11.50 (s, 1H); MS, m/e 606.1 (M + 23)+       36   2-Cl—Ph   H   H   Me   i-Pr   1HNMR (400 MHz, DMSO-d 6 ): δ =1.12-1.16 (m, 6H), 1.21-1.27 (m,                               6H), 3.79-3.85 (m, 2H), 4.00-4.07 (m, 1H), 4.28-4.32 (m, 1H), 4.38-                               4.43 (m, 1H), 4.83-4.87 (m, 1H), 5.56 (dd, J1 = 16.0 Hz, J2 = 8.0 Hz,                                1H), 5.85-6.12 (m, 2H), 6.20-6.33 (m, 1H), 7.19-7.22 (m, 1H), 7.33 (t,                                J = 16.0 Hz, 1H), 7.48-7.55 (m, 3H), 11.55 (s, 1H)       37   4-   H   H   Me   Bn   1HNMR(400 MHz, DMSO-d 6 ): δ = 1.19-1.26 (m, 6H), 3.69-3.70 (s,           MeO—Ph                   3H), 3.87 (m, 2H), 3.99 (m, 1H), 4.20-4.21 (m, 1H), 4.35 (m, 1H),                               5.07-5.09 (m, 2H), 5.54 (t, J = 16.0 Hz, 1H), 5.85-5.92 (m, 1H), 6.04-                               6.10 (m, 2H), 6.86 (d, J = 8.0 Hz, 2H), 7.09 (dd, J1 = 16.0 Hz, J2 = 4.0                                Hz, 2H), 7.30-7.34 (m, 5H), 7.53 (s, 1H), 11.52 (s, 1H)       38   Ph   H   H   Me   n-Pen   1H NMR (DMSO-d 6 ) δ 0.79-0.81 (m, 3H), 1.17-1.23 (m, 10H), 3.74-                               3.81 (m, 2H), 3.94-3.96 (m, 3H), 4.19-4.36 (m, 2H), 5.49-5.54 (m,                               1H), 5.87-6.08 (m, 3H), 7.14-7.33 (m, 3H), 7.31-7.35 (m, 2H), 7.51 (d,                               J = 8 Hz, 1H), 11.51 (s, 1H) ; MS, m/e 557.9 (M + 1)+; 1136.88                               (2M + 23) +       39   4-Cl—Ph   H   H   Me   i-Pr   1H NMR (DMSO-d 6 ) δ 1.04-1.19 (m, 12H), 3.76-3.80 (m, 2H), 3.98-                               4.08 (m, 1H), 4.42-4.42 (m, 2H), 4.82-4.85 (m, 1H), 5.55-5.60 (m,                               1H), 5.80-6.20 (m, 3H), 7.20-7.25(m, 2H), 7.43 (d, J = 8.8Hz, 1H),                                7.54 (d, J = 8 Hz, 1H), 11.51 (s, 1H); MS, m/e 563.88 (M + 1) +;                                1148.73 (2M + 23) +       40   4-Cl—Ph   H   H   Me   n-Bu   1H NMR (DMSO-d 6 ) δ 0.85 (t, J = 7.2 Hz, 3H), 1.22-1.33 (m,                               8H), 1.45-1.53 (m, 2H), 3.80-3.87 (m, 2H), 3.96-4.04 (m, 3H), 4.24-                               4.27 (m, 1H), 4.35-4.39 (m, 1H), 5.56-5.61 (m, 1H), 5.82-6.11 (m,                               2H), 6.15-6.18 (m, 1H), 7.20-7.56 (m, 4H), 7.51-7.57 (m, 1H), 11.54                               (s, 1H); MS, m/e577.95(M + 1) +       41   4-Cl—Ph   H   H   Me   Et   1H NMR (DMSO-d 6 ) δ 1.14 (t, J = 7.0 Hz, 3H), 1.20-1.28 (m,                               6H), 3.77-3.88 (m, 2H), 3.99-4.07 (m, 3H), 4.24-4.28 (m, 1H), 4.34-                               4.43 (m, 1H), 5.56-5.61 (m, 1H), 5.86-6.13 (m, 2H), 6.15-6.24 (m,                               1H), 7.20-7.26 (m, 2H), 7.44 (d, J = 7.6 Hz, 2H), 7.55 (d, J = 7.6 Hz,                               1H), 11.55 (s, 1H); MS, m/e549.11(M + 1) +       42    4-   H    H    Me    n-Bu   1H NMR (DMSO-d 6 ) δ 0.79-0.83 (m, 3H), 1.17-1.28 (m, 8H), 1.45-           Me—Ph                   1.47 (m, 2H), 2.22 (d, J = 2.8 Hz, 1H), 3.70-3.90 (m, 2H), 3.95-3.98                               (m, 3H), 4.10-4.40 (m, 2H), 5.51 (t, 1H), 5.80-5.90 (m, 1H), 5.95-6.05                               (m, 2H), 7.02-7.06 (m, 2H), 7.51 (t, J = 4.2 Hz , 4H), 7.51 (d, 1H),                               11.51 (s, 1H); MS, m/e 557.99 (M + 1) +; 1136.84 (2M + 23) +       43   4-   H    H    Me    Bn   1H NMR (DMSO-d 6 ) δ 1.16-1.24 (m, 6H), 2.22 (s, 3H), 3.65-4.03           Me—Phe                   (m, 3H), 4.11-4.38 (m, 2H), 5.04-5.05 (m, 2H), 5.48-5.50 (m, 1H),                               5.77-5.87 (m, 1H), 5.90-6.11 (m, 2H), 6.98-7.10 (m, 4H), 7.28-7.32 (m,                               5H), 7.50 (t, 1H), 11.48 (s, 1H); MS, m/e 592.00 (M + 1) +.       44    Ph    H   H    Et    Me   1H NMR (DMSO-d 6 ) δ 0.70-0.80 (m, 3H), 1.11-1.26 (m, 3H), 1.42-                               1.61 (m, 2H), 3.50-3.54 (m, 3H), 3.58-3.80 (m, 2H), 3.91-4.02 (m,                               1H), 4.12-4.38 (m, 2H), 5.47-5.52 (m, 1H),5.90-6.03 (m, 2H), 7.08-                               7.16 (m, 3H), 7.26-7.35 (m, 2H),7.48 (t, 1H), 11.45 (s, 1H); MS, m/e                               515.95 (M + 1)+; 1052.82 (2M + 23) +       45    Ph    H   H    Me    4-F—Bn     1 HNMR (400 MHz, DMSO-d 6 ): δ 1.20-1.26 (m, 6H), 3.80-3.93 (m,                               2H), 3.98 (s, 1H), 4.25-4.26 (m, 1H), 4.36-4.37 (m, 1H), 5.07 (s, 2H),                               5.52-5.55 (m, 1H), 5.86-5.87(m, 1H), 5.98-6.04 (m, 1H), 6.14-6.17 (m,                               1H), 7.15-7.20 (m, 5H), 7.36 (dd, J = 20.0, 8.0 Hz, 4H), 7.54 (s, 1H),                               11.55 (s, 1H)       46    4-Cl—Ph    H    H    Me    n-Bu     1 HNMR (400 MHz, DMSO-d 6 ): δ 1.21-1.28 (m, 6H), 3.71-3.88 (m,                               1H), 3.91-3.98 (m, 1H), 4.00-4.01 (m, 1H), 4.23-4.27 (m, 1H),4.35-                               4.38 (m, 1H), 5.08 (d, J = 4.0 Hz, 2H), 5.57 (dd, J = 12.0, 8.0 Hz, 1H),                               5.91 (d, J = 8.0 Hz, 1H), 6.01 (d, J = 8.0 Hz, 1H), 6.22-6.24 (m, 1H),                               7.17-7.23 (m, 2H), 7.31-7.40 (m, 7H), 7.53 (s, 1H), 11.50 (s, 1H)       47    Ph    H   H    Me    3-Me-1-Bu     1 H NMR (DMSO-d 6 ) δ 0.80-0.82 (m, 6H), 1.18-1.40 (m, 8H), 1.50-                               1.58 (m, 1H), 3.71-3.82 (m, 3H), 3.97-3.4.01 (m, 3H), 4.21-4.40 (m,                               2H), 5.30(t, J = 8.6 Hz, 1H), 5.81-6.10 (m, 3H), 7.15-7.20 (m, 3H),                               7.32-7.36 (m, 2H), 7.48 (d, J = 8.4 Hz, 1H), 11.38 (s, 1H); MS, m/e                               557.98 (M + 1)*; 1136.88 (2M + 23) +         48    3,4-   H   H    Me    Bn     1 H NMR (DMSO-d 6 ) δ 1.05-1.37 (m, 6H), 3.71-3.82 (m, 1H), 3.87-           diCl—Ph                   4.02 (m, 2H), 4.28-4.29 (m, 1H), 4.36-4.38 (m, 1H), 5.04 (d, J = 5.2 Hz,                               2H), 5.55-5.64 (m, 1H), 5.85-5.94 (m, 1H), 6.00-6.05 (m, 1H), 6.29-                               6.40 (m, 1 H),7.17-7.24 (m, 1H), 7.30-7.41 (m, 5H), 7.45-7.58 (m, 2H),                               7.61 (d, 7 = 4.0 Hz, 1H), 11.53 (s, 1H); MS, m/e545.80(M + 1) + ;       49    Ph    H   H    Me    c-Hex     1 H NMR (DMSO-d 6 ) δ 1.18-1.41 (m, 12H), 1.59-1.67 (m, 4H), 3.74-                               13.80 (m, 1H), 3.96-4.02 (m, 1H), 4.19-4.26 (m, 1H), 4.31-4.39 (m,                               1H), 4.60 (s, 1H), 5.52 (t, J = 7.8 Hz, 1H), 5.80-6.09 (m, 3H), 7.15-                               7.20 (m, 3H), 7.32-7.36 (m, 2H), 7.52 (d, J = 8 Hz, 1H), 11.50 (s, 1H);                               MS, m/e 569.98 (M + 1)*; 592.14 (M + 23)*       50    Ph    H   Me    H    n-Bu   1H NMR (DMSO-d 6 ) δ 0.76 (t, J = 7.2 Hz, 3H), 1.10-1.22 (m, 8H),                               1.38-1.43 (m, 2H), 3.72-3.75 (m, 2H), 3.87-3.93 (m, 3H), 4.14-4.21                               (m, 1H), 4.23-4.33 (m, 1H), 5.46-5.54 (m, 1H), 5.84-6.11 (m, 3H),                               7.09-7.14(m, 2H), 7.27-7.32 (m, 2H), 7.34-7.51 (m, 1H), 11.47 (s,                               1H); MS, m/e543.98(M + 1) +       51    Ph    H   Me    H    i-Pr   1H NMR (DMSO-d 6 ) δ 1.39 (d, J = 7.2 Hz, 6H), 1.19-1.29 (m, 6H),                               3.65-3.75 (m, 2H), 3.95-4.05 (m, 1H), 4.20-4.22 (m, 1H), 4.31-4.33                               (m, 1H), 4.79-4.82 (m, 1H), 5.48-5.57 (m, 1H), 5.84-5.91 (m, 1H),                               5.96-6.07 (m, 2H), 7.12-7.35 (m, 5H), 7.44-7.54 (m, 1H), 11.49(s, 1H);                               MS, m/e529.96 (M + 1) +       52   Ph   H   Me   H   Bn     1 H NMR (DMSO-d 6 ) δ 1.18-1.28 (m, 6H), 3.70-3.83 (m, 1H), 3.87-                               3.94 (m, 1H), 3.99-4.01 (m, 1H), 4.23-4.26 (m, 1H), 4.33-4.37 (m,                               1H), 5.03-5.12 (m, 2H), 5.51-5.59 (m, 1H), 5.87-5.90 (m, 1H), 5.95-                               6.07 (m, 1H), 6.10-6.27 (m, 1H), 7.15-7.23 (m, 3H), 7.31-7.38 (m,                               7H), 7.47-7.56 (m, 1H), 11.50 (s, 1H); MS, m/e577.99 (M + 1) +       53   2-Cl—Ph   H   H   Me   n-Bu     1 HNMR (400 MHz, DMSO-d 6 ): δ 0.81-0.86 (m, 3H), 1.21-1.31 (m,                               8H), 1.46-1.52 (m, 2H), 3.84-3.90 (m, 2H), 3.97-4.04 (m, 3H),4.27-                               4.41 (m, 2H), 5.53-5.58 (m, 1H), 5.82-5.95 (m, 1H), 5.96-6.10 (m,                               1H), 6.27-6.31 (m, 1H), 7.19-7.22 (m, 1H), 7.34 (dd, J = 8.0, 4.0 Hz,                               1H), 7.47-7.55 (m, 3H), 11.55 (s, 1H)       54   4-Br—Ph   H   H   Me   i-Pr     1 HNMR (400 MHz, DMSO-d 6 ): δ 1.10-1.14 (m, 6H), 1.20-1.27 (m,                               6H), 3.74-3.81 (m, 2H), 3.99-4.01 (m, 1H), 4.21-4.25 (m, 1H), 4.37-                               4.38 (m, 1H), 4.81-4.85 (m, 1H), 5.58 (dd, J = 8.0, 4.0 Hz, 1H), 5.82-                               5.95 (m, 1H), 5.96-6.09 (m, 1H), 6.10-6.13 (m, 1H), 7.18 (dd, J =                               12.0, 8.0 Hz, 2H), 7.53-7.57 (m, 3H), 11.52 (s, 1H)       55   4-F—Ph   H   H   Me   c-Hex     1 H NMR (DMSO-d 6 ) δ 1.20-1.44 (m, 12H), 1.60-1.71 (m, 4H), 3.75-                               4.02 (m, 2H), 3.94-4.02 (m, 1H), 4.19-4.26 (m, 2H), 4.59-4.61 (m,                               1H), 5.57 (t, J = 8.4 Hz, 1H), 5.85-6.06 (m, 3H), 7.17-7.23 (m, 4H),                               7.54 (d, J = 8.4 Hz, 1H), 11.50 (s, 1H); MS, m/e 587.92 (M + 1) +         56   4-Br—Ph   H   H   Me   c-Hex     1 HNMR (400 MHz, DMSO-d 6 ): δ = 1.18-1.46 (m, 12H), 1.61-1.69 (m,                               4H), 3.75-3.82 (m, 2H), 3.95-4.08 (m, 1H), 4.25-4.28 (m, 1H), 4.38 (s,                               1H), 4.60-4.62 (m, 1H), 5.56-5.60 (m, 1H), 5.82-5.95 (m, 1H), 6.02-                               6.20 (m, 2H), 7.09-7.20 (m, 2H), 7.53-7.57 (m, 3H), 11.52 (s, 1H)                               MS, m/e 650.0 (M + 3) +         57   Ph   H   H   Et   i-Pr     1 HNMR (400 MHz, DMSO-d 6 ): δ = 0.75-0.82 (m, 3H), 1.12-1.26 (m,                               9H), 1.52-1.59 (m, 2H), 3.55-3.68 (m, 1H), 3.72-3.85 (m, 1H), 3.95-                               4.08 (m, 1H), 4.18-4.28 (m, 1H), 4.32-4.41 (m, 1H), 4.83-4.86 (m,                               1H), 5.55 (m, J = 7.6 Hz, 1H), 5.99-6.04 (m, 2H), 6.05-6.10 (m, 1H),                               7.14-7.21 (m, 3H), 7.33-7.37 (m, 2H), 7.52-7.54 (m, 1H), 11.53 (s,                               1H); MS, m/e566.07(M + 23) +         58   Ph   H   H   Et   c-Hex     1 HNMR (400 MHz, DMSO-d 6 ): δ 0.75-0.88 (m, 3H), 1.26-1.46 (m,                               9H), 1.52-1.69 (m, 6H), 3.60-3.63 (m, 1H), 3.72-3.90 (m, 1H), 4.02-                               4.03 (m, 1H), 4.24-4.27 (m, 1H), 4.37-4.38 (m, 1H), 4.63-4.65 (m,                               1H), 5.55 (dd, J = 8.0 Hz, 4.4 Hz, 1H), 5.80-5.95 (m, 1H), 6.00-6.07                                (m, 2H), 7.15-7.22 (m, 3H), 7.34-7.38 (m, 2H), 7.54 (d, J = 8.0Hz, 1H),                               11.55 (s, 1H); MS, m/e 584.01 (M + 1) + , 606.17 (M + 23) +         59   4-F—Ph   H   H   Et   c-Hex     1 H NMR (DMSO-d 6 ) δ 0.75-0.84 (m, 3H), 1.24 (d, J = 22.8 Hz, 3H),                               1.29-1.47 (m, 6H), 1.51-1.70 (m, 6H), 3.59-3.66 (m, 1H), 3.77-3.84                               (m, 1H), 3.98-4.04 (m, 1H), 4.21-4.27 (m, 1H), 4.34-4.41 (m, 1H),                               4.60-4.65 (m, 1H), 5.56-5.60 (m, 1H), 5.84-5.90 (m, 1H), 6.00-6.08                               (m, 2H), 7.20-7.24 (m, 4H), 7.56(d, J = 8.0 Hz, 1H), 11.49 (s, 1H); MS,                               m/e 602.00(M + 1) +         60    Ph   H    H    Me    F—CH 2 —CH 2 —     1 H NMR (DMSO-d 6 ) δ 1.18-1.25(m, 6H), 3.71-3.89 (m, 2H), 3.92-3.99                               (m, 1H), 4.19-4.27 (m, 4H), 4.48-4.61 (m, 2H), 3.94-3.98 (m, 2H),                               4.11-4.23 (m, 4H), 5.47-5.52 (m, 1H), 6.01-6.11 (m, 1H), 5.90-6.14                               (m, 2H), 7.15-7.21 (m, 3H), 7.32-7.36 (m, 2H), 7.46-7.57 (m, 1H),                               11.49 (s, 1H); MS, m/e 533.86 (M + 1) +         61    Ph   H    H    Me    F 2 CH—CH 2 —     1 H NMR (DMSO-d 6 ) δ 1.17-1.24 (m, 6H), 3.67-3.81 (m, 1H), 3.89-                               3.98 (m, 2H), 4.21-4.36 (m, 4H), 5.48-5.53 (m, 1H), 5.82-6.05 (m,                               2H), 6.18-6.22 (m, 2H), 7.15-7.20 (m, 3H), 7.32-7.36 (m, 2H), 7.51 (s,                               1H), 11.50 (s, 1H); MS, m/e 551.92 (M + 1) + ;       62    Ph   H    H    Me    (CF 3 ) 2 —CH—     1 H NMR (DMSO-d 6 ) δ 1.13-1.29 (m, 6H), 3.67-3.81 (m, 1H), 3.94-                               4.32 (m, 4H), 5.47 (t, J = 8 Hz 1H), 5.82-6.01 (m, 2H), 6.33-6.36 (m,                               1H), 6.70-6.78 (m, 1H), 7.09-7.15 (m, 3H), 7.28-7.32 (m, 2H), 7.43-                               7.46 (m, 1H), 11.44 (s, 1H); MS, m/e 637.90 (M + 1) +         63    Ph   H    H    Me    (CH 2 F) 2 —CH—     1 H NMR (DMSO-d 6 ) δ 1.20-1.29 (m, 6H), 3.70-3.90 (m, 1H), 3.91-                               4.12 (m, 2H), 4.20-1.33 (m, 1H), 4.35-4.48 (m, 1H), 4.52-4.55 (m,                               2H), 4.63-4.67 (m, 2H), 5.20-5.35 (m, 1H), 5.56 (t, J = 8.4 Hz, 1H),                               5.80-5.95 (m, 1H), 5.95-6.10 (m, 1H), 6.18-6.21 (m, 1H), 7.18-7.23                               (m, 3H), 7.35-7.39 (m, 2H), 7.54 (s, 1H), 11.55 (s, 1H); MS, m/e                               565.98 (M + 1) +         64    Ph   H    H    Me    c-Pr-CH 2 —     1 H NMR (DMSO-d 6 ) δ 0.20-0.24(m, 2H), 0.47-0.48(m, 2H), 0.76-                               0.84(m, 3H), 1.03-1.05(m, 1H), 1.23(dd, J = 22.4 6.8 Hz 3H), 1.55-                               1.60(m, 2H), 3.61-3.68(m, 1H), 3.81-3.89 (m, 3H), 3.98-4.03(m, 1H),                               4.23-4.29(m, 1H), 4.35-4.41 (m, 1H), 5.56-6.00(m, 1H), 5.88-5.91 (m,                               1H), 6.04-6.10(m, 2H), 7.20-7.24(m, 4H), 7.55 (d, J = 7.6 Hz                               1H), 11.53 (s, 1H); MS, m/e 573.17 (M + 1) +         65    Ph   H    H    Et    c-Pen     1 H NMR (DMSO-d 6 ) δ 0.75-0.83 (m, 3H), 1.20-1.28 (m, 3H), 1.49-                               1.63 (m, 8H), 1.76-1.80 (m, 2H), 3.58-3.60 (m, 1H), 3.70-3.82 (m,                               1H), 3.98-4.05 (m, 1H), 4.24-1.26 (m, 1H), 4.37-1.42 (m, 1H), 5.03                               (s, 1H), 5.54-5.57 (m, 1H), 5.90-6.00 (m, 1H), 6.02-6.07 (m, 2H), 7.15-                               7.22 (m, 3H), 7.35-7.39 (m, 2H) 7.55 (d, J = 8.0 Hz, 1H), 11.55 (s,                               1H); MS, m/e 570.03 (M + 1) +                 *R 2  and R 3b  together are —(CH 2 ) 3 — as derived from L-proline            
The Purification Procedure by Prep-HPLC:
 
     Crude products were dissolved in methanol. Injection volumes of these solutions were 5 mL. 
     The preparative HPLC system including 2 sets of Gilson 306 pumps, a Gilson 156 UV/Vis detector, a Gilson 215 injector &amp; fraction collector, with Unipoint control software. A Ymc 25×30×2 mm column was used. The mobile phase was HPLC grade water (A), and HPLC grade acetonitrile (B). Fractions were collected into 100*15 mm glass tubes. 
     HPLC gradient is shown in Table 1. Once the gradient was selected, acetonitrile solution was injected into HPLC system, and then fractions collected according to UV peaks. After the separation, each glass tubes were run MS test to collect the desired compounds. The fractions with target MS were combined in a well-weighted flask. Most of acetonitrile was removed under reduce pressure and the remaining solution was freeze-dried to give desired compound. 
     
       
         
           
               
             
               
                 TABLE 1 
               
             
            
               
                   
               
               
                 Preparative HPLC gradient 
               
            
           
           
               
               
               
               
               
            
               
                   
                 Time (min) 
                 Flow rate (mL/min) 
                 % A 
                 % B 
               
               
                   
                   
               
            
           
           
               
               
               
               
               
            
               
                   
                 0 
                 15 
                 90 
                 10 
               
               
                   
                 30 
                 15 
                 60 
                 40 
               
               
                   
                   
               
            
           
         
       
     
     Preparation of Example 66 
                                           
Preparation of Compound (b)
 
     To a solution of compound a (1 g, 2.69 mmol) in anhydrous THF (30 mL) was added dropwise 1 M solution of LiAl(OBu-t) 3 H in THF (2.69 mL, 2.69 mmol) at −20° C. The reaction mixture was stirred for 2-3 h at the same temperature. EtOAc (100 mL) was added followed by saturated NH 4 Cl solution (10 mL) and reaction mixture was slowly brought to room temperature. Reaction mixture was extracted with EtOAc and washed with 1N HCl and water. Combined organic phase was evaporated to give 0.8 g of crude compound b as transparent oil, which was used directly for next reaction. 
     Preparation of Compound (d) 
     To a solution of compound b (0.8 g, 2.1 mmol), compound c (0.45 g, 2.5 mmol) and Ph 3 P (0.56 g, 2.1 mmol) in anhydrous THF (20 mL) under nitrogen atmosphere was added DEAD (1.8 mL). The reaction mixture was stirred at room temperature overnight. The reaction solution was concentrated under reduce pressure. The residue was separated by preparative layer chromatography (hexanes:EtOAc=3:1) to give crude compound d (0.8 g). The crude compound d was used to the next step without further purification. 
     Preparation of Compound (e) 
     Compound d (0.8 g, 1.57 mmol) was dissolved in THF (2 mL) and THF saturated with ammonia (5 mL) was then added to this solution. The reaction mixture was heated to 90° C. overnight. After 18 hours, the solution was cooled to room temperature by ice water, then the solvent was removed under reduced pressure and the residue was purified by column to give compound e (0.75 g) for the next step. 
     Preparation of Compound (f) 
     Compound e (0.5 g, 1.01 mmol) was dissolved in methanol (2 mL) and methanol was saturated with ammonia (5 mL) was then added to this solution. The reaction mixture was stirred at room temperature overnight. After 18 hours, the solvent was removed under reduced pressure and the residue was purified by column to give crude compound f (0.15 g) for the next step. 
     Preparation of Compound (i) 
     A solution of triethylamine (1.07 g, 10.6 mmol) in anhydrous dichloromethane (15 mL) was added dropwise to a solution of compound g (1.16 g, 5.3 mmol) and compound h (1.31 g, 5.3 mmol) in dichloromethane (10 mL) with vigorous stirring at −78° C. over a period of 2 hours. After completion of addition, the reaction temperature was allowed to warm to room temperature gradually and stirred over night. Then the solvent was removed under vacuum and anhydrous ether 20 mL was added and the precipitated salt was filtered and the precipitate was washed with ether. The combined organic phase was concentrated to give the colorless oil of compound i (1.0 g). 
     Preparation of Compound 66 
     To a solution of compound j (0.1 g, 0.35 mmol) dissolved in 10 mL of anhydrous THF, stirred and added 0.4 g NMI till the solution became clear, added compound i (0.8 g, 2.89 mmol) in 10 mL THF dropwise, stirred at r.t. overnight. Compound purity and identification was confirmed by LCMS. The solvent was evaporated and purified by Prep-HPLC to afford 66. (25 mg, Yield: 13.6%).  1 H NMR (DMSO-d 6 ) δ 1.08 (d, J=22.8 Hz, 3H), 1.17-1.24 (m, 3H), 3.50-3.52 (m, 3H), 3.78-3.83 (m, 1H), 4.10-4.13 (m, 1H), 4.24-4.44 (m, 2H), 5.85-5.92 (m, 1H), 6.01-6.11 (m, 1H), 6.2-6.27 (m, 1H), 7.08-7.19 (m, 4H), 7.31-7.38 (m, 3H), 8.15 (s, 1H), 8.26 (s, 1H); MS, m/e 525 (M+1) + . 
     Example numbers 67-74, identified below, were prepared using similar procedures disclosed for Example 66, above. 
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
               
             
               
                   
               
               
                 Example 
                 R 11   
                 R 10   
                 NMR/MS 
               
               
                   
               
             
            
               
                 67 
                 OH 
                 NH 2   
                   1 H NMR(DMSO-d 6 ) δ 1.06-1.13 (m, 3H), 1.20-1.24 (m, 3H), 
               
               
                   
                   
                   
                 3.27-3.33 (m, 3H), 3.56 (s, 1H), 3.82-3.88 (m, 1H), 4.07-4.13 
               
               
                   
                   
                   
                 (m, 1H), 4.25-4.40 (m, 2H), 5.85-5.87 (m, 1H), 5.98-6.09 (m, 
               
               
                   
                   
                   
                 2H), 6.59 (s, 32H), 7.14-7.37 (m, 3H), 7.35-7.37 (m, 2H), 
               
               
                   
                   
                   
                 7.79 (d, J = 7.2 Hz, 1H), 10.69 (s, 1H); MS, m/e 541 (M + 1) + ; 
               
               
                 68 
                 NH 2   
                 NH 2   
                   1 H NMR (DMSO-d 6 ) δ 1.07 (d, J = 22.8 Hz, 3H), 1.19 (d, 
               
               
                   
                   
                   
                 J = 7.2 Hz, 3H), 3.51 (s, 3H), 3.62 (s, 1H), 3.75-3.81 (m, 1H), 
               
               
                   
                   
                   
                 4.05-4.11 (m, 1H), 4.27-4.42 (m, 2H), 5.79-5.83 (m, 1H), 
               
               
                   
                   
                   
                 5.92 (s, 2H), 6.00-6.09 (m, 2H), 6.75 (s, 2H), 7.08-7.17 (m, 
               
               
                   
                   
                   
                 3H), 7.31-7.35 (m, 2H), 7.78 (s, 1H); MS, m/e 540 (M + 1) + ; 
               
               
                 69 
                 NH 2   
                 c-Pentyl-NH— 
                   1 H NMR (DMSO-d 6 ) δ 1.05 (d, J = 22.8 Hz, 3H), 1.09-1.19 
               
               
                   
                   
                   
                 (m, 3H), 1.48 (s, 4H), 1.66 (s, 1H), 1.86 (s, 1H), 3.54 (d, 
               
               
                   
                   
                   
                 J = 14 Hz, 3H), 3.65 (s, 1H), 4.25-4.43 (m, 4H), 5.71-5.82 (m, 
               
               
                   
                   
                   
                 1H), 5.94-6.04 (m, 4H), 7.11-7.24 (m, 3H), 7.26-7.34 (m, 
               
               
                   
                   
                   
                 2H), 7.77 (d, J = 3.6 Hz, 1H); MS, m/e 608 (M + 1) +   
               
               
                   
               
               
                 70 
                 NH 2   
                 
                   
                     
                     
                         
                         
                     
                   
                 
                   1 H NMR (DMSO-d 6 ) δ 1.07 (d, J = 22.4 Hz, 3H), 2.35-2.38 (m, 2H), 3.54 (d, J = 9.2 Hz, 3H), 3.59-3.62 (m, 2H), 3.65 (s, 1H), 3.75-3.82 (m, 1H), 4.01-4.13 (m, 2H), 4.22-4.40 (m, 6H), 5.75-5.85 (m, 1H), 6.00-6.07 (m, 4H), 7.15-7.21 (m, 
               
               
                   
                   
                   
                 3H), 7.32-7.35 (m, 2H), 7.79 (d, J = 4.0 Hz, 1H); MS, m/e 580 
               
               
                   
                   
                   
                 (M + 1) +   
               
               
                   
               
               
                 71 
                 NH 2   
                 Et 2 N— 
                   1 H NMR (DMSO-d 6 ) δ 1.06-1.28 (m, 12H), 3.55 (d, J = 4.8 
               
               
                   
                   
                   
                 Hz, 3H), 3.79-3.87 (m, 4H), 4.07-4.12 (m, 2H), 4.29-4.42 (m, 
               
               
                   
                   
                   
                 3H), 5.75-5.82 (m, 1H), 5.94 (s, 2H), 6.04-6.10 (m, 2H), 
               
               
                   
                   
                   
                 7.14-7.22 (m, 3H), 7.31-7.37 (m, 2H), 7.82 (d, J = 4.4 Hz, 
               
               
                   
                   
                   
                 1H); MS, m/e 596 (M + 1) +   
               
               
                 72 
                 NH 2   
                 n-Propyl-NH— 
                   1 H NMR (DMSO-d 6 ) δ 0.84 (t, J = 7.2 Hz, 3H), 1.01-1.01 (m, 
               
               
                   
                   
                   
                 3H), 1.09-1.12 (m, 3H), 1.51-1.56 (m, 2H), 3.48 (d, J = 15.2 
               
               
                   
                   
                   
                 Hz, 3H), 3.79-3.82 (m, 1H), 4.04-4.05 (m, 1H), 4.27-4.38 (m, 
               
               
                   
                   
                   
                 3H), 5.72-5.79 (m, 1H), 5.98-6.04 (m, 4H), 7.13-7.20 (m, 
               
               
                   
                   
                   
                 3H), 7.26-7.32 (m, 2H), 7.76 (d, J = 5.2 Hz, 1H); MS, m/e 582 
               
               
                   
                   
                   
                 (M + 1) +   
               
               
                 73 
                 NH 2   
                 c-Butyl-NH— 
                   1 H NMR (DMSO-d 6 ) δ 1.02-1.08 (m, 3H), 1.18 (d, J = 4.8 Hz, 
               
               
                   
                   
                   
                 3H), 1.44-1.61 (m, 2H) , 2.02-2.17 (m, 4H), 3.51 (d, J = 10.8 
               
               
                   
                   
                   
                 Hz, 3H), 3.78-3.83 (m, 1H), 4.03-4.06 (m, 1H), 4.27-4.38 (m, 
               
               
                   
                   
                   
                 2H), 4.53-4.62 (m, 1H), 5.68-5.79 (m, 1H), 5.95-6.04 (m, 
               
               
                   
                   
                   
                 4H), 7.11-7.18 (m, 3H), 7.29-7.35 (m, 2H), 7.51-7.58 (m, 
               
               
                   
                   
                   
                 1H), 7.78 (d, J = 5.2 Hz, 1H); MS, m/e 594 (M + 1) +   
               
               
                   
               
               
                 74 
                 NH 2   
                 
                   
                     
                     
                         
                         
                     
                   
                 
                   1 H NMR (DMSO-d 6 ) δ 0.97-1.20 (m, 6H), 2.18 (s, 3H), 2.19 (s, 4H), 3.43-3.47 (m, 3H), 3.75 (s, 1H), 4.01-4.06 (m, 4 H), 4.22-4.35 (m, 3H), 5.69-5.75 (m, 1H), 5.98-6.05 (m, 3H), 7.09-7.15 (m, 3H), 7.25-7.29 (m, 2H), 7.77 (d, 
               
               
                   
                   
                   
                 J = 3.6 Hz, 1H); MS, m/e 623 (M + 1) +   
               
               
                   
               
            
           
         
       
     
     Example numbers 75-80 are prepared using similar procedures disclosed for Example 66, above. 
     
       
         
         
             
             
         
       
     
     
       
         
           
               
               
               
             
               
                   
               
               
                 Example 
                 R 11   
                 R 10   
               
               
                   
               
             
            
               
                 75 
                 H 
                 n-propyl—NH— 
               
               
                 76 
                 H 
                 c-Butyl—NH— 
               
               
                 77 
                 H 
                 c-Pentyl—NH— 
               
               
                   
               
               
                 78 
                 H 
                 
                   
                     
                     
                         
                         
                     
                   
                 
               
               
                   
               
               
                 79 
                 H 
                 
                   
                     
                     
                         
                         
                     
                   
                 
               
               
                   
               
               
                 80 
                 H 
                 
                   
                     
                     
                         
                         
                     
                   
                 
               
               
                   
               
            
           
         
       
     
     Example 81 
     Certain exemplified compounds were obtained as mixture of diastereomers because of the chirality at phosphorous. The diastereomers were separated on a Chiralpak-AS-H (2×25 cm) column under Supercritical Fluid Chromatography (SFC) conditions using 20% methanol in carbon dioxide as solvent. The absolute stereochemistry of the P-chiral center of the diastereomers were not determined. However, chromatographic resolution of these two diastereomers provides for isomers that are characterized as fast eluting and slow eluting isomers. Some examples are shown below. 
     
       
         
           
               
               
               
             
               
                   
                   
               
               
                   
                 Compound 
                 EC90 (uM) 
               
               
                   
                   
               
             
            
               
                   
               
            
           
           
               
               
               
            
               
                   
                 Example 15 (Diastereomeric mixture) 
                 0.86 
               
               
                   
                 Fast Moving isomer of Example 15 
                 1.35 
               
               
                   
                 Slow Moving isomer of Example 15 
                 0.26 
               
               
                   
                 Example 39 (Diastereomeric mixture) 
                 0.47 
               
               
                   
                 Fast Moving isomer of Example 39 
                 0.78 
               
               
                   
                 Slow Moving isomer of Example 39 
                 0.02 
               
               
                   
                 Example 49 (Diastereomeric mixture) 
                 0.126 
               
               
                   
                 Fast Moving isomer of Example 49 
                 0.03 
               
               
                   
                 Slow Moving isomer of Example 49 
                 5.78 
               
               
                   
                   
               
            
           
         
       
     
     Example 82 
     HCV replicon assay. HCV replicon RNA-containing Huh7 cells (clone A cells; Apath, LLC, St. Louis, Mo.) were kept at exponential growth in Dulbecco&#39;s modified Eagle&#39;s medium (high glucose) containing 10% fetal bovine serum, 4 mM L-glutamine and 1 mM sodium pyruvate, 1×nonessential amino acids, and G418 (1,000 μg/ml). Antiviral assays were performed in the same medium without G418. Cells were seeded in a 96-well plate at 1,500 cells per well, and test compounds were added immediately after seeding. Incubation time 4 days. At the end of the incubation step, total cellular RNA was isolated (RNeasy 96 kit; Qiagen). Replicon RNA and an internal control (TaqMan rRNA control reagents; Applied Biosystems) were amplified in a single-step multiplex RT-PCR protocol as recommended by the manufacturer. The HCV primers and probe were designed with Primer Express software (Applied Biosystems) and covered highly conserved 5′-untranslated region (UTR) sequences (sense, 5′-AGCCATGGCGTTAGTA(T)GAGTGT-3′, and antisense, 5′-TTCCGCAGACCACTATGG-3′; probe, 5′-FAM-CCTCCAGGACCCCCCCTCCC-TAMRA-3′). 
     To express the antiviral effectiveness of a compound, the threshold RT-PCR cycle of the test compound was subtracted from the average threshold RT-PCR cycle of the no-drug control (ΔCt HCV ). A ΔCt of 3.3 equals a 1-log 10 reduction (equal to the 90% effective concentration [EC 90 ]) in replicon RNA levels. The cytotoxicity of the test compound could also be expressed by calculating the ΔCt rRNA  values. The ΔΔCt specificity parameter could then be introduced (ΔCt HCV -ΔCt rRNA ), in which the levels of HCV RNA are normalized for the rRNA levels and calibrated against the no-drug control. 
     
       
         
           
               
               
               
               
             
               
                   
               
               
                   
                   
                 Log10 
                   
               
               
                   
                   
                 Reduction at 
                 EC90 
               
               
                 Ex # 
                 Compound 
                 50 μM 
                 (μM) 
               
               
                   
               
             
            
               
                   
               
            
           
           
               
               
               
               
            
               
                  5 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 −1.21 
                 3.0 
               
               
                   
               
               
                  6 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 −0.45 
                 ND 
               
               
                   
               
               
                  7 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0.31 
                 ND 
               
               
                   
               
               
                  8 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 −1.48 
                 2.11 
               
               
                   
               
               
                 10 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 −1.25 
                 19.15 
               
               
                   
               
               
                 11 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 −0.55 
                 ND 
               
               
                   
               
               
                 12 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 0.31 
                 ND 
               
               
                   
               
               
                 15 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 ND 
                 0.86 
               
               
                   
               
               
                 25 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 −2.22 
                 0.39 
               
               
                   
               
               
                 27 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 −2.25 
                 0.66 
               
               
                   
               
               
                 28 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 −2.16 
                 0.75 
               
               
                   
               
               
                 36 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 −1.64 
                 21.9 
               
               
                   
               
               
                 39 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 −1.78 
                 0.47 
               
               
                   
               
               
                 49 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 −2.69 
                 0.126 
               
               
                   
               
               
                 53 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 −1.33 
                 &lt;0.3 
               
               
                   
               
               
                 54 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 −1.55 
                 0.57 
               
               
                   
               
               
                 55 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 −2.38 
                 &lt;0.3 
               
               
                   
               
               
                 69 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 −2.25 
                 &lt;0.3 
               
               
                   
               
               
                 70 
                 
                   
                     
                     
                         
                         
                     
                   
                 
                 −2.25 
                 &lt;0.3 
               
               
                   
               
               
                   1 (4-BrPh): 4-bromo—phenyl. 
               
            
           
         
       
     
     The entire contents of U.S. Provisional Application Nos. 60/909,315, filed Mar. 30, 2007, and 60/982,309, filed Oct. 24, 2007, are hereby incorporated by reference in the present application so far as needed to supplement the present disclosure and/or rectify any errors. Moreover, the patent and non-patent references disclosed herein are incorporated by reference. In the event that the incorporated patent and non-patent reference contains a term that conflicts with a term disclosed in either one of the two Provisional Applications or the present application text, the meaning of the term contained in the present application text and the two Provisional Applications controls provided that the overall meaning of the incorporated subject matter is not lost.