PEPTIDE COMPOUNDS FOR PREVENTION AND/OR TREATMENT OF NO-MEDIATED DISEASES

Abstract: New peptide compounds of formula (I) wherein W is a group of formula (a) [in which R<1> is hydrogen, halogen, lower alkyl, etc., Q is CH or N, L is a bivalent radical (b) (in which Y is CH or N, Z is NH, O or S, and <u>---</u> is a single bond or a double bond), etc.,], etc., A<1> is lower alkylene, -NHCO-, (c) (in which V is O or S), or -SO2-, T is hydrogen, aryl which may have suitable substituent(s), heterocyclic group, hydroxy, etc., A<2> is lower alkylene, R<8> is hydrogen or lower alkyl, etc., R<3> is hydrogen, aryl which may have suitable substituent(s), hydroxy, protected hydroxy, etc., A<3> is bond or lower alkylene, R<9> is hydrogen or lower alkyl, etc., and R<4> is carboxy, protected carboxy, heterocycliccarbonyl which may have suitable substituent(s), or a group of formula (d) (in which R<5> is hydrogen or lower alkyl, and R<6> is hydrogen, aryl, ar(lower)alkyl which may have suitable substituent(s), etc.), etc., and a pharmaceutically acceptable salt thereof which are useful as a medicament.

Description: DESCRIPTION PEPTIDE COMPOUNDS FOR PREVENTION ANDOR TREATMENT OF NO-MEDIATED DISEASES TECHNICAL FIELD This invention relates co new peptide compounds and pharmaceutically acceptable sale thereof whic are useful as a medicament. BACKGROUND ART Some peptide compounds have been known as described, for example, in EP 0 394 989 A2. DISCLOSURE OF INVENTION This invention relates co new peptide compounds. One object of this invention is to provide the new and useful peptide compounds and pharmaceutically acceptable salts thereof which possess a strong inhibitory activity on the production of nitric oxide (NO) . Another object of this invention is to provide process for preparation of the peptide compounds and salts thereof. A further object of this invention is to provide a pharmaceutical composition comprising said peptide compounds or a pharmaceutically acceptable salt thereof. Still further object of this invention is to provide a use of said peptide compounds or a pharmaceutically acceptable salt thereof as a medicament for prophylactic and therapeutic treatment of NO-mediated diseases such as adult respiratory distress syndrome, cardiovascular ischemia, myocarditis, heart failure, synovitis, shock (e.g., septic shock, etc.), diabetes (e.g. insulin-dependent diabetes mellitus, etc.), diabetic nephropathy, diabetic retinopathy, diabetic neuropathy, glomerulonephritis, peptic ulcer, inflammatory bowel disease (e.g., ulcerative colitis, chronic colitis, etc.), cerebral infarction, cerebrai ischemia, migraine, rheumatoid arthritis, gouc, neuritis, postherpetic neuralgia, osteoarchritis, osteoporosis, systemic lupus erythematosis, rejection by organ transplantation, asthma, metastasis, Alzheimer's disease, arthritis, CNS disorders, and the like in human being and animals. The object peptide compounds of che present invention are novel and can be represented by che following general formula (I) : wherein W is lower alkyl, aryl which may have suitable substituent(s) , fluorenyl which may have suitable substituent(s) , hetero onocyclic group which may have suitable substituen (s) , or a group of the formula : [ in which R 1 is hydrogen, halogen, lower alkyl, nitro, di (lower)alkylamino, amino, protected amino, hydroxyamino or lower alkoxy, Q is CH or N, L is a bivalent radical selected from (in which Y is CH or N, Z is NH, 0 or S, and is a single bond or a double bond) and (in which M is CH or N, and J is CH or N) ], V A 1 is lower alkylene, -NHCO-, -C- (in which V is 0 or S) , or -S0 2 -, T is hydrogen, aryl which may have suitable substituent (s) , heterocyclic group, hydroxy, acyloxy, ar(lower)alkoxy, sulfooxy, mercapt^ r --lower alkylchio, mono(or di or cri) ar(lower)alkylthio, acylthio, amino, protected amino, guanidino, acylguanidinc or a group cf the formula : (in which R 2 is hydroxy, ar (lower)alkoxy, morpholinyl, piperazinyi which may have suitable substituent (s) , piperidyl which may have suitable substituen (s) , pyrrolidinyl, thiomorpholinyi, homopiperazinyl which may have suitable substituent (s) , piperazinio which may have suitable substituent (s) , piperidyloxy which may have suitable substituen (s) , or amino - _ - having one or two suitable substituent (s) , A 2 is lower alkylene, R 8 is hydrogen or lower alkyl, or R 8 and a group of the formula : -A 2 -T are linked cogecher to form R 3 is hydrogen, aryl which may have suitable substituent (s) , hydroxy, protected hydroxy, cyclo (lower)alkyl, lower alkylchio, or heterocyclic group which may have suitable substicuent (s) , A 3 is bond or lower alkylene, R^ is hydrogen or lower alkyl, or R 9 and a group of the formula : -A 3 -R- are linked cogether to form and R 4 is carboxy, protected carboxy, hecerocyciiccarbonyl which may have suicable substituent (s) , or a group of che formula : (in which R 5 is hydrogen or lower alkyl, and R 6 is hydrogen, aryl, ar(lower) alkyl which may have suitable substituent (s) , [di (lower) alkylaminoj (lower) alkyl, or heterocyclic (lower)alkyl which may have suitable substituent(s) ) , or R 4 and a group of the formula : -A 3 -R 3 are linked together to form (in which R 10 is ar(lower) alkyl) , with proviso that when M is CH, and J is CH, then Q is N. The main object compound (I) of the present invention can be prepared by the following processes. Process fl) (III) or its reactive derivative, or a salt thereof - o - (Ic) or a salt thereof Process .2. (Ic) or its reactive derivative at che carboxy group, or a salt thereof erivative, 16981 - 7 - (lb) or a salt thereof ?-r.r.- ~ - .3. (ID or a salt thereof (Id) or a salt thereof Process .4) i) W-A -CHO or a salt thereof i reduction (II) or a salt thereof (Ie) or a salt thereof Prnπass (5) (ID or a salt thereof (if) or a salt thereof wherein W, T, A 1 , A 2 , A 3 , V, R 3 , R 4 , R 8 and R 9 are each as defined above , and A 4 is bond or Cι- - alkylene, X is a leaving group, is morpholino, piperazino which may have suitable substituent(s) , piperidino which may have suitable substituent(s) , pyrrolidi o, thiomorpholino, ho opiperazino which may have suitable substituent (s) , piperazinio which may have suitable substituent (s) or amino having one or two suitable substituent(s) . The other compound (I) of the present invention can be prepared by the following examples or by a conventional method. The starting compound can be prepared by che following processes. Pro ess (A) (Ha) or its reactive derivative at the carboxy group or a salt thereof erivative, (lib) or a salt thereof Process (B . (V ) or a salt thereof Elimination reaction of the amine protective group (II) or a salt thereof Process (C. RI (VI) or its reactive derivative at the carboxy group, or a salt thereof - 11- - ve derivative, reor R ι& _cκ— coKIn Ri< (Villa) or salt thereof Process (Pi (VIII) or a salt thereof elimination reaction of the amine proteccive group (IX) or salt therec: _> rιτoιcress (£ ) I TV \ or its reactive αe πvat ve, cr a salt thereof vative, (V) or a salt thereof 10 .--._ wherein R 5 , R 4 , R 5 , R 6 , R ε , R 9 ,7, A 2 .. A 3 and are each as 1 defined above, ~ ° R and R 1 are each amino protective group. Suitable pharmaceutically acceptable salts cf the object compound (I) are conventional non-toxic salts and may include a salt with base or an acid addition salt such as a salt 20 with ar. inorganic base, for example, an alkali metal salt ;e.g., sodium salt, potassium salt, etc.;, an alkaline earth metal salt ie.g., calcium salt, macnesiur. salt, etc.), an aιr__noni _r. salt; a salt with an organic base, fcr example, an organic amine salt (e.g., triet yiar.ine salt, pyridine salt, 25 picciine salt, etr.anoiamina salt, triethanclarr.ir.e salt, dicyciohexyiair.ir.e salt, N,N 1 -dibεr.zylechyienediair.ine salt, etc.); an inorganic acid addition salt ; e.ς., ydrochlcride, hydrobromice, sulfate, phosphate, etc./,- an organic carboxylic cr sulfonic acid additicr. salt '.e.g., formate, 30 acetate, trifl croacetate, rr.aleate, tartrate, citrate, fu arate, methanesulfonate, benzenesulfonate, tciuenesulfcnate, etc.!; a sa_t with a oasic cr acidic ammo acic e.g., arginine, aspart c acid, ciuta . c acid, etc.: . In the above and subsequent descriptions cf the present specification, suitable examples and illustration of the various definitions which the present invention intends to include within the scope thereof are explained in detail as follows. The tern "lower" is used to intend a group having 1 to 6, preferably 1 to 4, carbon atom(s), unless otherwise provided. The term "higher" is used tc intend a group having 7 to 20 carbon atoms, unless otherwise provided. Suitable "lower alkyl" and "lower alkyl oiety" in the terms "ar (lower)alkyl", "heterocyclic(lower)alkyl", "di (lower)alkylamino", "lower alkylthio", "mono(or di or tri)ar(lower)alkylthio" and " [di (lower) alkylamino] (lower)- alkyl" may include straight or branched one having 1 to 6 carbon atom(s), such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, tert-pentyl, hexyl, and the like, and in which more preferable example may be C_-C 4 alkyl. Suitable "lower alkenyl" may include vinyl, l-(or 2-)propenyl, l-(or 2- or 3-)butenyl, l-(or 2- or 3- or 4-)pentenyl, 1- (or 2- or 3- or 4- or 5-)hexenyl, methylvinyl, ethylvinyl, l-(or 2- or 3-)methyl-l- (or 2-)propenyl, l-(or 2- or 3-)ethyl-1- (or 2-)propenyl, l-(or 2- or 3- or 4-)methyl-l- (or 2- or 3-)butenyl, and the like, in which more preferable example may be 2- 4 alkenyl. Suitable "lower alkynyl" may include ethynyl, 1-propynyl, propargyl, 1-methylpropargyl, 1 cr 2 or 3- butynyl, 1 or 2 or 3 or 4-pentynyl, 1 or 2 or 3 or 4 or 5- hexynyl, and the like. Suitable "lower alkoxy" and "lower alkoxy moiety" in the term "ar(lower)alkoxy" may include methoxy, ethoxy, propoxy, isopropoxy, butoxy, isobutoxy, t-butoxy, pentyloxy, t-pentyloxy, hexyloxy and the like. Suitable "cyclo(lower)alkyl" may include cyciopropyl. . o - cyclobutyl, cyclopentyl, cyclohexyl, cycioheptyl and the like. Suitable "cyclo (lower)alkenyl" may include cyclohexenyl, cyclohexadienyl and the like. Suitable "aryl" and "aryl moiety" in the terms "ar(lower) alkoxy" and "ar (lower) alkyl" may include phenyl, naphthyl and the like. Suitable "halogen" may include fluorine, bromine, chlorine and iodine. Suitable "leaving group" may include acid residue, lower alkoxy as exemplified above, and the like. Suitable "acid residue" may include halogen as exemplified above, acyloxy and the like. Suitable "lower alkylene" may include straight or branched one such as methylene, ethylene, tri ethylene, tetramethylene, pentamethylene, hexamethylene, methylmethylene, l-(or 2-)methyltrimethylene, ethylethylene, propylene, and the like, in which more preferable example may be C^C^ alkylene and the most preferable one may be methylene. Suitable "C 1 -C5 alkylene" may include straight or branched one such as methylene, ethylene, trimethylene, tetramethylene, pentamethylene, methylmethylene, 1- (cr 2-)- methyltrimethylene, ethylethylene, propylene, and the like. Suitable "protected carboxy" may include commonly protected carboxy, and the like. Suitable "commonly protected carboxy" may include esterified carboxy and the like. And suitable example of said ester may be the ones such as lower alkyl ester (e.g., methyl ester, ethyl ester, propyl ester, isopropyl ester, butyl ester, isobutyl ester, t-butyl ester, pentyl ester, t-pentyl ester, hexyl ester, etc.); lower alkenyl ester (e.g., vinyl ester, allyl ester, etc.); lower alkynyl ester (e.g., ethynyl ester propynyl ester, " etc.); lower alkoxy(lower) alkyl ester (e.g., methoxymethyl ester. ethoxymethyl ester, isopropoxymethyl ester, 1-methoxyethyl ester, 1-ethoxyethyl ester, etc.); lower alkylthio (lower)alkyl ester (e.g., methylthiomethyl ester, ethylthiomethyl ester, ethylthioethyi ester, isopropoxythiomethyl ester, etc.); mono (or di or tri)halo(lower) lkyl ester (e.g., 2-iodoεtnyl ester, 2,2,2- trichlcroethyl ester, etc.); lower alkanoyloxy(lower)alkyl ester (e.g., acetoxy ethyl ester, propicnyioxymethyl ester, butyryloxymethyl ester, valeryloxymethyl ester, pivaloyloxymethyl ester, hexanoyloxymethyl ester, 1-acetoxyethyl ester, 2-acetoxyethyl ester, 2-propionyloxyethyl ester, etc.); lower alkcxycarbonyloxy(lower)alkyl ester \ e . g . , methoxycarbonyloxymethyl ester, ethoxycarbonyioxymethyl ester, propoxycarbonyloxymethyl ester, l-(cr 2-)- [methoxycarbonyloxy]ethyl ester, l-(or 2-) [ethoxycarbonyloxyjethyl ester, l-(or 2-) [propoxycarboayloxy]ethyl ester, l-(or 2-) [isopropoxycarbonyloxy]ethyl ester, etc.); lower alkanesulfonyl(lower)alkyl ester (e.g., mesylmethyl ester, 2-mesylethyl ester, etc.); lower alkoxycarbonyloxy(lower) alkyl ester (e.g., methoxycarbonyloxymethyl ester, ethoxycarbonyioxymethyl ester, propoxycarbonyloxymethyl ester, t-butoxycarbonyloxymethyl ester, l-(or 2-)methoxycarbonyloxyethyl ester, l-(or 2-)ethcxycarbonyloxyethyl ester, l-(or 2-) isopropoxycarbonyloxyethyl ester, etc.); phthalidylidene (lower) alkyl ester; (5-lower alkyl-2-oxo-l, 3-dioxoi-4-yI) (lower) alkyl ester [e.g., (5-methyl-2-oxo-l,3-dioxol-4-yl)methyl ester, (5-ethyl-2-oxo-l,3-dιoxol-4-yl)methyl ester, (5-propyl-2-oxo- 1, 3-dioxoi-4-yl) ethyl ester, etc.]; mono(or di or tri)aryl (lower) alkyl ester, for example, mono (or di or tri)phenyl (lower)alkyl ester which may have one cr more - 1 3 - suitable substituent (s) (e.g., benzyl ester, 4-methoxybenzyi ester, 4-nitrobenzyl ester, phenethyl ester, trityl ester, benzhydryl ester, bis (methoxyphenyl)methyl ester, 3, -dimethoxybenzyl ester, 4-hydroxy-3, 5-di-t-butyibenzyi ester, etc.); aryl ester which may have one or more suitable substituent (s) such as substituted cr unsubstituted phenyl ester (e.g., phenyl ester, toiyi ester, t-butylphenyl ester, xylyl ester, mesityl ester, cumenyl ester, 4-chlorophenyi ester, -methoxyphenyl ester, etc.); tri (lower) alkylsilyl ester; lower alkylthioester (e.g., ethylthioester, ethylthioester, etc.) and the like. Suitable "hydroxy protective group" in the term "protected hydroxy" may include acyl, mono (or di or tri(phenyl (lower)alkyl which may have one or more suitable substituent (s) (e.g., benzyl, 4-methoxybenzyl, trityl, etc.), trisubstituted silyl [e.g., tri (lower)alkylsilyl (e.g., trimethylsilyl, t-butyldimethylsilyl, etc.), etc.], tetrahydropyranyl and the like. Suitable "amino protective group" may include acyl or a conventional protective group such as mono(or di or tri)aryl- (lower) alkyl, for example, mono(or di or tri)phenyl (lower) - alkyl (e.g., benzyl, trityl, etc.) or the like. Suitable "protected amino" may include acylamino or an amino group substituted by a conventional protecting group such as mono (or di or tri) aryl (lower) alkyl, for example, mcno(or di or tri)phenyl (lower)alkyl (e.g., benzyl, trityl, etc. ! cr the like. Suitable "acyl" and "acyl moiety" in the terms "acylamino", "acyloxy", "acylthio" and "acylguanidino" may include carba oyl, aliphatic acyl group and acyl group containing an aromatic ring, which is referred to as aromatic acyl, or heterocyclic ring, which is referred to as heterocyclic acyl. Suitable example cf said acyl may be illustrated as follows : Carba oyl; Thiocarbamoyl; Aliphatic acyl such as lower or higher alkanoyl (e.g., for yl, acetyl, propanoyl, butanoyi, 2-methyipropanoyl, pentanoyl, 2,2-dimethylpropanoyI, hexanoyl, heptanoyl, octanoyl, nonanoyl, decanoyl, undecanoyl, dodecanoyl, tridecanoyl, tetradecanoyl, pentadecanoyi, hexadecanoyl, heptadecanoyi, octadecanovl, nonadecanov!, icosanoyl, etc.); lower or higher alkoxycarbonyi (e.g., methoxycarbonyl, ethoxycarbonyl, t-butoxycarbonyl, t-pentyloxycarbonyl, heptyloxycarbonyl, etc.); lower or higher alkylsuifonyl (e.g., methyisulfonyi, ethylsulfonyl, etc.); lower or higher alkoxysulfonyl (e.g., methoxysulfonyl, ethoxysulfonyl, etc. ) ; cyclo(lower)alkylcarbonyl (e.g., cyclopentylcarbonyi, cyclohexylcarbonyl, etc.); or the like; Aromatic acyl such as aroyl (e.g., benzoyl, toluoyl, naphthoyi, etc.); ar (lower)alkanoyl [e.g., phenyl (lower)alkanoyl (e.g., phenylacetyl, phenyIpropanoyl, phenylbutanoyl, phenylisobutanoyl, phenylpentanoyl, phenylhexanoyl, etc.), naphthyl (lower)alkanoyl (e.g., naphthylacetyl, naphthylpropano l, naphthylbutanoyl, etc.), etc.}; ar(lower)alkenoyl [e.g., phenyl(lower)alkenoyl (e.g., phenylpropenoyl, phenylbutenoyl, phenylmethacryloyl, phenylpentenoyl, phenyIhexenoyl, etc.), naphthyl (lower)alkenoyl (e.g., naphthylpropenoyl, naphthylbutenoyi, etc.), etc.]; ar(lower) alkoxycarbonyi [e.g., phenyl (lower)alkoxycarbonyi (e.g., benzyloxycarbonyl, etc.), etc.]; aryloxycarbonyl (e.g., phenoxycarbonyl, naphthyloxycarbonyl, etc.) ; aryloxy(lower) alkanoyl (e.g., phenoxyacetyl. phenoxypropionyl , etc . ) ; arylglyoxyloyl (e . g . , phenylglycxyloyl, naphthylglyoxyloyl, etc . ) ; arylsulfonyl (e.g., phenylsuifonyl, p-tolylsulfonyl, etc.); or the like; Heterocyclic acyl such as heterocycliccarbonyl; heterocyclic(lower)alkanoyl (e.g., heterocyciicacetyi, heterocyclicpropanoyl, heterocyclicbutanoyl, heterocyclicpentanoyl, heterocyclichexanoyl, etc.); heterocyclic(lower)alkenoyl (e.g., heterocyclicpropenoyl, heterocyclicbutenoyl, heterocyclicpentenoyl, heterocyclichexεnoyl, etc.); heterocyclicglyoxyloyl; or the like; in which suitable "heterocyclic moiety" in the terms "heterocycliccarbonyl", "heterocyclic(lower) alkanoyl", heterocyclic(lower)alkenoyl" and "heterocyclicglycxyloyl" as mentioned above means, in more detail, saturated or unsaturated, monocyclic or pclyc clic heterocyclic group containing at least one hetero-atom such as an oxygen, sulfur, nitrogen atom and the like. And, especially preferable heterocyclic group may be heterocyclic group such as unsaturated 3 to 8-membered (more preferably 5 or 6- membered) heteromonocyclic group containing 1 to 4 nitrogen atom(s), for example, pyrrolyl, pyrrolinyl, imidazolyl, pyrazolyl, pyridyl, dihydropyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, triazolyl (e.g., 4H-1,2, -triazolyi, lK-1,2,4- triazolyl, 1K-1,2,3-triazolyl, 2H-1,2.3-triazolyI, etc.), tetrazolyl (e.g., IH-tetrazolyi, 2H-tetrazolyl, etc.,, etc.; saturated 3 to 8-membered (more preferably 5 or 6- membered) heteromonocyclic group containing 1 to 4 nitrogen atom(s) , for example, pyrrolidinyl, imidazolidinyl, piperidyl, piperazinyl, etc.; unsaturated condensed heterocyclic group containing 1 to 4 nitrogen atom(s), for example, indolyl, iscindclyl, indolinyl, indoiizinyl, benzimidazolyl (e.g. 1H- benzimidazolyi, etc.), quinolyi, isoquinoiyi, tetrahydroisoquinolyl (e.g. 1,2, 3, -tetrahydroiscquinolyi, etc.) indazolyl, benzotriazoiyl, quinazciinyi, ςuinoxalinyl, phthalazinyl, etc.; unsaturated 3 to 8-membered (more preferably 5 cr 6- membered) heteromonocyclic group containing 1 to 2 oxygen atom(s) and I to 3 nitrogen atom(s), for example, oxazciyl, iscxazolyl, oxadiazolyl (e.g., 1,2,4-cxaaiazoiyl, 1,3,4- oxadiazolyl, 1,2, 5-oxadiazolyl, etc.), etc.; saturated 3 to 8-membered (mere preferably 5 or 6- membered) heteromonocyclic group containing 1 to 2 oxygen atom(s) and 1 to 3 nitrogen atom(s), for example, morpholinyl, sydnonyl, etc.; unsaturated condensed heterocyclic group containing 1 to 2 oxygen atom(s) and 1 to 3 nitrogen ato (s; , for example, benzoxazolyl, benzoxadiazolyi, etc.; unsaturated 3 to 8-membered (more preferably 5 or 6- membered) heteromonocyclic group containing 1 to 2 sulfur atom(s) and 1 to 3 nitrogen atom(s), for example, thiazolyl, isothiazolyl, thiadiazolyl (e.g., 1,2, 3-thiadiazoiyI, 1,2,4- thiadiazolyl, 1, 3,4-thiadiazoiyl, 1,2, 5-thiaciazolyi, etc.), dihydrothiazinyl, etc.; saturated 3 to S-membered (more preferably 5 or 6- me bered) heteromonocyclic group containing 1 to 2 sulfur atom(s) and 1 to 3 nitrogen atom(s), for example, thiomorpholinyl, thiazolidinyl, etc.; unsaturated 3 to 8-membered (more preferably 5 or 6- membered) heteromonocyclic group containing 1 to 2 sulfur atom(s), for example, thienyl, dihydrocithiinyl, dihydrodithionyl, etc.; unsaturated condensed heterccyclic group containing 1 to 2 sulfur atom(s) and i to 3 nitrogen atom(s) , for example, benzothiazolyl, benzothiadiazolyl, etc.; unsaturated 3 to 8-membered (more preferably 5 or β- membered) heteromonocyclic group containing an oxygen atom, for example, furyl, etc.; unsaturated 3 to 8-membered (more preferably 5 or 6- membered) heteromonocyclic group containing ar: oxygen atom and 1 to 2 sulfur atcm(s), for example, dihy rocxathiinyl, etc. ; unsaturated condensed heterocyclic group containing 1 to 2 sulfur atom(s), for example, benzothienyl, benzodithiinyl, etc.; unsaturated condensed heterocyclic group containing an oxygen atom and I to 2 sulfur ato is., for example, benzoxathiinyl, etc.; and the like. The acyl moiety as stated above may have one to ten, same or different, suitable substituent (s) such as lower alkyl as exemplified above, lower alkoxy as exemplified above, lower alkylthio wherein lower alkyl moiety is as exemplified above, lower alkylamino wherein lower alkyl moiety is as exemplified above, di (lower)alkylamino wherein lower alkyl moiety is as exemplified above, cyclo (lower) alkyl as exemplified above, cyclo (lower) alkenyl as exemplified above, halogen as exemplified above, aryl as exemplified above, amino, protected amino as exemplified above, hydroxy, protected hydroxy as exemplified above, cyano, nitro, carboxy, protected carboxy as exemplified above, sulfo, sulfamcyl, imino, oxc, amine (lower)alkyl wherein lower alkyl moiety is as exemplified above, carbamoylcxy, mono (or di cr tri)halo (lower) alkyl wherein halogen moiety and lower alkyl moiety are each as exemplified above, hydroxy(lower) alkyl wherein lower alkyl moiety is as exemplified above, cr the like. Suitable "heterocyclic group" and "heterocyclic moiety" in the terms "heterocycliccarbonyl" and "heterocyclic(lower) alkyl" can be referred to the ones as exemolified above. Suitable "commonly protected amino" may include amine substitutea with a common N-protective group such as substituted or unsubstituted lower alkanoyl (e.g., fcrmyl, acetyl, propionyl, trifiuoroacetyl, etc.), phthaloyl, lower alkoxycarbonyi (e.g., tert-butoxycarbonyi, tert-amyloxycarbonyl, etc.), substitutea or unsubstituted ar(lower) alkanoyl (e.g., benzylcxycarbcnyi, p-nitrobenzyioxycarbonyl, etc.), carbamoyi, substituted carbamoyl [e.g., mono or di (lower alkyl) carbamoyi (e.g., methylcarbamoyl, dimethylcarba oyl, etc.), arylcarbamcyl (e.g., phenylcarbamoyl, etc.), etc.], substituted cr unsubstituted arylsulfonyl (e.g., phenylsulfonyl, tosyl, etc.), nitrophenylsulfenyl, ar (lower)alkyl (e.g., trityl cr benzyl, etc.), or the like. Suitable "heteromonocyclic group" may include unsaturated 3 to 8-membered (more preferably 5 or 6- membered) heteromonocyclic group containing 1 to 4 nitrogen atom(s), for example, pyrrolyl, pyrroiinyi, imidazolyl, pyrazolyl, pyridyl, dihydropyridyl, pyrimidinyl, pyrazinyl, pyridazinyi, triazolyl (e.g., 4H-1, 2 , 4-triazclyl, 1H-1,2,3- triazolyl, 2H-1,2, 3-triazolyl, etc.), tetrazolyl (e.g., IH, tetrazolyl, 2K-tetrazolyl, etc.), etc.; saturated 3 to 8-membered (more preferably 5 or 6- membered) heteromonocyclic group containing 1 to 4 nitrogen atcm(s), for example pyrroiidinyl, imidazolidinyl, piperidyl, piperazinyl, etc.; unsaturated 3 to 8-membered (more preferably 5 or 6- membered) heteromonocyclic group containing 1 to 2 oxygen atom(s) and 1 to 3 nitrogen atom(s), for example, cxazoiyl, isoxazolyl, oxadiazolyi (e.g., 1,2, 4-oxadiazclyl, 1,3,4- oxadiazolyl, 1,2, 5-oxadiazoiyl, etc.), etc.; saturated 3 to S-membered (more preferably 5 or 5- membered) heteromonocyclic group containing 1 to 2 oxygen atom(s) and 1 to 3 nitrogen atom(s) for example, morpholinyl, sydnonyl, etc.; unsaturated 3 to 8-membered (more preferably 5 or 6- membered) heteromonocyclic group containing 1 to 2 sulfur atom(i.; and 1 to 3 nitrogen atom(s), for example, tniazcl isothiazolyl, thiadiazolyi (e.g., 1,2,3-thιadiazoiyl, 1,2, thiadiazolyi, I,3,4-thiadiazolyi, 1,2, 5-thiadiazclyl.. etc dihydrothiazinyi, etc.; saturated 3 to 8-membered (mere preferably Ξ or 6- membered) heteromonocyclic group containing 1 tc 2 sulfur atom(s) and i to 3 nitrogen atcm(s), for example, thiazolidinyl, etc.; unsaturated 3 to 8-membered (more preferably 5 or c- membered) heteromonocyclic group containing i tc 2 sulfur atom(s), for example, thienyl, dihydrodithiinyl, dihydrodithionyl, etc.; unsaturated 3 tc 8-membered (more preferably 5 or 6- membered) heteromonocyclic group containing an oxygen ato for example, furyl, etc.; unsaturated 3 tc 8-memberec (more preferably 5 cr 6- membered) heteromonocyclic group containing an oxygen ato and 1 to 2 sulfur atom(s), for example, dihydrocxathiiny!, etc.; and the like. Suitable "substituent" in the terms "aryl which may h suitable substituent (s) ", "fluorenyl which may have suitab substituent (s) ", "piperidyl which may have suitable substituent(s) " "piperazinyi which may have suitable substituent (s) "piperazinic which may have suitable substituent(s) "hσmopiperazinyl which may have suitable substituent (s) "piperidyloxy which may have suitable substituent (s) "amino having one cr two suitab_e substituent (s) "heterocyclic group which may have suitab substituent(s) "ar(lower)alkyl which may have suitable substituent(ε) "heterocycliccarbonyl which may have suitable substituent(s) ", "heterocyclic(lower)alkyl which have suitable substituent(s) ", "heteromonocyclic group whi may have suitable substituent (s) ", "piperazino which may h suitable substituent (s) ", "piperidino which may have suitable substituent (s) " and "homopiperidino which may have suitable substituent (s) " may include lower alkyl as exemplified above, lower alkoxy as exemplified above, lower alkenyl as exemplified above, lower al ynyi as exemplified above, mono (or di or tri)halo (lower) alkyl wherein halogen moiety and lower alkyl moiety are each as exemplified above, cyclo (lower)alkyl as exemplified above, cycle (lower)alkenyl as exemplified above, halogen as exemplified above, carboxy, protected carboxy as exemplified above, hydrcxy, protected hydroxy as exemplified above, aryl as exemplified above, ar(lower)alkyl wherein aryl moiety and lower alkyl moiety are each as exemplified above, carboxy(lower)alkyl wherein lower alkyl moiety as exemplified above, protected carboxy(lower)alkyl wherein protected carboxy moiety and lower alkyl moiety are each as exemplified above, nitro, amino, protected amino as exemplified above, di (lower) alkylamino wherein lower alkyl moiety is as exemplified above, amino(lower) lkyl wherein lower alkyl moiety is as exemplified above, protected amino (lower) lkyl wherein protected amino moiety and lower alkyl moiety are each as exemplified above, acyl as exemplified above, cyano, sulfc, oxo, sulfa oyl, carbamoyloxy, mercaptc, lower alkylthio wherein lower alkyl moiety is as exemplified above, hydroxy, protected hydroxy as exemplified above, heterocyclic group which may have lower alkyl wherein heterocyclic moiety and lower alkyl moiety are each as exemplified above, iminc, [di (lower)alkylamino] (lower) alkyl wherein lower alkyl moiety is as exemplified above, [di (lower)alkylamino] (lower) alkoxy wherein lower alkyl moiety and lower alkoxy mciety are each as exemplified above, mono (or ai or tri) (protected hydroxy) (lower) alkyl wherein protected hydroxy moiety and lower alkyl moiety are each as exemplified above, mono(or di or tri. (hydroxy) (lower) alkyl wherein lower alkyl moiety is as exemplified above, methylenedicxy and the like. The processes fcr preparing the object and starting compounds are explained in detail in the following. Prnr.es - .1. The compound (Ic) or a salt thereof can be prepared by reacting the compound (II} or its reactive derivative or a salt thereof with the compound (III) or ts reactive derivative at the carboxy group, or a salt thereof. Suitable reactive derivative cf the compound (II) may include Schiff's base type i ino cr its tautcmeric enamine type isomer formed by the reaction of the compound (II) with a carbonyl compound such as aldehyde, ketone cr the like; a silyl derivative formed by tne reaction of the compound (II) with a silyl compound such as N,0-bis (trimethylsilyl)acetami e, N-trimethyisilyiacetamide or the like; a derivative formed by the reaction of the compound (II) with phosphorus trichloride or phosgene, and the like. Suitable reactive derivative of the compound (III) may include an acid halide, an acid anhydride, an activated ester, and the like. The suitable example may be an acid chloride; acid azide; a mixed acid anhydride with an acid such as substituted phosphoric acid (e.g., dialkylphosphoric acid, phenylphosphoric aci , diphenylphcsphoric acid, dibenzylphosphoric acid, halogenated phosphoric acid, etc.), dialkylphosphorous acid, sulfurous acia, thiosulfuric acid, alkanesulfonic acid (e.g., methanesuifonic acid, ethanesulfonic acid, etc.), sulfuric acid, alkyicarbonic acid, aliphatic carboxylic acid (e.g., pivaiic acid, pentanoic acid, isopentanoic acid, 2-ethylbutyric acid, trichioroacetic acid, etc.); aromatic carboxylic acid (e.g., benzole acid, etc.); a symmetrical acid anhydride; an activated amide with imidazole, 4-substituted imiaazole, dimethylpyrazole, tria∑ole or tetrazoie; an activated ester (e.g., cyanomethyi ester, methoxymethyl ester. dimethyliminomethyl [ (CH 3 ) 2 + N β CH-] ester, vinyl ester, propargyl ester, p-nitrophenyl ester, 2, 4-dinitrophenyi ester, trichlorophenyl ester, pentachlcrophenyl ester, mesylphenyl ester, phenylazophenyl ester, phenylthio ester, p-nitrophenyi thioester, p-cresyl thioester, carboxymethyl thioester, pyranyl ester, pyridyl ester, pipericyl ester, 8-quinolyl thioester, etc.); an ester with a λ : -hyaroκy compound (e.g., N,N-dimethyihydroxyiamine, i-hydroxy-2- (IK)- pyridone, N-hydroxysuccinimide, N-hydroxybenzctriazole, N-hydroxyphthalimide, l-hydroxy-6-chIcro-lH-benzctriazoIe, etc.); and the like. These reactive derivatives can optionally be selected from them according tc the kind cf the compound (III) to be used. The reaction is usually carried cut in a conventional solvent such as water, acetone, dioxane, acetonitrile, chloroform, methylene chloride, ethylene chloride, tetrahydrofuran, ethyl acetate, N,N-dimethyiformamide, pyridine or any other " or anic solvents which do not adversely affect the reaction, or the mixture thereof. When the compound (III) is used in free acid form or its salt form in the reaction, the reaction is preferable carried out in the presence of a conventional condensing agent such as N,N'-dicyclohexylcarbodiimide; N-cyclohexyl-N'-morpholinoethylcarbodiimide; N-cyclohexyl-N'- (4-diethylaminocyclohexyi)carbodiimide; N, '-diisopropylcarbodiimide; N-ethyl-N'-(3-dimethylaminopropyI)carbodiimide; N,N-carbonyl-bis (2-methylimidazole) ; pentamethyleneketene-N-cyclohexyiimine; diphenylketene-N-cyclohexylimine; ethoxyacetylene; 1-alkoxy-l-chIoroethyiene; trialkyl phosphite; isopropyl polyphosphate; phosphorous oxychioride (phosphoryl chloride) ; phosphorous trichloride; thionyl chloride; oxalyi chloride; triphenylphosphitε; 2-ethyl-7-hydroxybenzisoxazolium salt; 2-ethyl-5- (m-sulfophenyl) isoxazolium. hydroxide intra¬ molecular salt; 1- (p-chlorobenzenesuifonyioxy) -6-chicrc-lH- benzotriazole; so-called Viismeier reagent prepared by the reaction of N,N-dimethylformamide with thionyi chloride, phosgene, phosphorous oxychloride, etc.; cr the like. The reaction may be also be carried out in the presence of an organic cr inorganic base such as an alkali metal bicarbonate, tri (lower)alkylamine, pyridine, N- (lower)- alkylmorphorine, N,N-di (lower) ikylbenzylamme, cr the like. The reaction temperature is not critical, and the reaction is usually carried out under cooling to heating. Pro ess (2> The compound (lb) or a salt thereof can be prepared by reacting the compound (Ia) or its reactive derivative at the carboxy group, or a salt thereof with the compound (IV) or its reactive derivative, or a salt thereof. This reaction can ~ 5e ' carried out in a similar manner to that of the aforementioned Process (1) . and therefore the reagents tc be used and the reaction conditions (e.g., solvent, reaction temperature, etc.) can be referred to those of the Process (I) . Process (3) The compound (Id) or a salt thereof can se prepared by reacting the compound (II) or a salt thereof w th the compound (XI) or a salt thereof. The reaction can be carried out in the manner disclosed in Example 12 or similar manners thereto. Process <4) The compound (Ie) or a salt thereof can be prepared by reacting the compound (II) or a salt thereof with the compound (XII) and then by subjecting the resultant compound to reduction reaction. The reaction can be carried out in the manner disclosed in Example 13 cr similar manners thereto. Process (?. The compound (If) or a salt thereof can be prepared by reacting the compound (II) or a salt thereof with the compound (XIII) or a salt thereof. The reaction can be carried out in the manner disclosed in Exaππole 35 cr similar manners thereto. Process (A) The compound (lib) cr a salt thereof can be prepared by reacting the compound (Ha) or its reactive derivative at the carboxy group, or a salt thereof with the compound (IV) cr its reactive derivative, or a salt tnereof. This reaction can be carried out in a similar manner to that of the aforementioned Process .1i . and therefore the reagents to be used and the reaction conditions (e.g., solvent, reaction temperature, etc.} can be referred tc those of the Process χ \ . Process (B. The compound (II) or a salt thereof can be prepared by subjecting the compound (V) or a salt thereof to elimination reaction cf the amine protective group. Suitable method cf this elimination reaction may include conventional one such as hydrolysis, reduction and the like. (i, For Hydrolysis : The hydrolysis is preferably carried out tne presence cf base or an acid including Levis acid. Suitable base may include an inorganic base and an organic base such as an alkali metal [e.g., sodium, potassium., etc.:, an alkaline earth metal [e.g., magnesium, ca_cium, etc.}.. the hydroxide or carbonate cr hydrogencarbonate thereof, triaikylamine [e.g., trimethylamine, triethylamine, etc.], picoline, I, 5-dia∑abicycIo[ .3.0]-non-5-ene, cr the like. Suitable acid may include an organic acid [e.g., fcrmic acid, acetic acid, propionic aciα, trichioroacetic aci , trifluoroacetic acid, etc.}, and an inorganic acid .e.g., hydrochloric acid, hydrobromic acid, sulfuric acid, hydrogen chloride, hydrogen bromide, etc.]. The elimination using Lewis acid such as trihaloacetic acid [e.g., trichioroacetic acid, trifluoroacetic acid, etc.], or the like is preferably carried out in the presence of cation trapping agents [e.g., anisole, phenol, etc.]. This reaction is usually carried out in no solvent. The reaction may be carried out in a conventional solvent such as water, alcohol (e.g., methancl, ethanol, isopropyl alcohol, etc.), tetrahydrofuran, dioxane, toluene, methylene chloride, ethylene dicnlcride, chloroform, N,N-dimethylformamide, N,N-dimethyiacetamiae or any other organic solvents which do not adversely affect the reaction, or the mixture thereof. The reaction temperature is net critical and the reaction is usually carried out under coding to warming. (ii) For reduction : Reduction is carried out in a conventional manner, including chemical reduction and catalytic reduction. Suitable reducing reagent to be used in chemical reduction are hydrides (e.g., hydrogen iodide, hydrogen sulfide, lithium aluminum hydride, sodium bcrchydride, sodium cyanoborohydride, etc.), or a combination cf a metal (e.g., tin, zinc, iron, etc.) or metallic compound (e.g., chromium chloride, chromium acetate, etc.) and an organic acid or an inorganic acid (e.g., formic acid, acetic acid, propionic acid, trifluoroacetic acid, p-toluenesulfonic acid, hydrochloric acid, hydrobromic acid, etc.). Suitable catalysts to be used in catalytic reduction are conventional ones such as platinum catalysts (e.g., platinum plate, spcngy platinum, platinum black, colloidal platinum, platinum oxide, platinum wire, etc.}, palladium catalysts (e.g., spongy palladium, palladium black, palladium oxide, palladium on carbon, colloidal palladium, palladium or. barium sulfate, palladium on barium carbonate, etc.), nickel catalysts (e.g., reduced nickel, nickel oxide, Raney nickel, etc.), cobalt catalysts (e.g., reduced cobalt, Raney cobalt, etc.), iron catalysts (e.g., reduced iron, Raney iron, Ullman iron, etc.), and the like. The reduction is usually carried cut in a conventional solvent such as water, alcohol (e.g., methanol, ethanol, isopropyl alcohol, etc.), tetrahydrofuran, dicxane, toluene, methylene chloride, ethylene dicnlcride, chloroform, N,N-dimethylformamide, N,N-dimethylacetamide or any other organic solvents which do not adversely affect the reaction, or the mixture theree~f~. Additionally, in case that the abcve-mentioneo acids to be used in chemical reduction are in liquid, they can also be used as a solvent. The reaction temperature of this reduction is net critical and the reaction is usually carried out under cooling to warming. Process C The compound (Villa) or a salt thereof can be prepared by reacting the compound (VI) or its reactive derivative at the carboxy group, or a salt thereof with the compound (VII) or its reactive derivative, or a salt thereof. This reaction can be carried out in a similar manner to that of the aforementioned Process .1 ) . ana therefore the reagents to be used and the reaction conditions (e.g., solvent, reaction temperature, etc.) can be referred tc those of the Process .1) . Process ( T) ) The compound (IX) or a salt thereof can be prepared by subjecting the compound (VIII) or a salt thereof tc elimination reaction of the amino protective group. This reaction can be carried out in a similar manner tc that of the aforementioned Process (B' . and therefore the reagents to be used and the reaction conditions .'e.g., solvent, reaction temperature, etc.) can be referred to these of the Process (S) • Process I K ) The compound (V) cr a salt thereof can be prepared by reacting the compound (IX) or its reactive derivative, or a salt thereof with the compound (X) or its reactive derivative at the carboxy group, cr a salt thereof. This reaction can be carried out in a similar manner to that of the aforementioned Process (1) . and therefore the reagents to be used and the reaction conditions (e.g., solvent, reaction temperature, etc.) can be referred to those of the Process (1) . Suitable salts of the object, starting compounds and their reactive derivatives in Processes (I) -(5) and (A.) -(E) can be referred to the ones as exemplified for the compound (I) • The compounds obtained by the above processes can be isolated and purified by a conventional method such as pulverization, recrystallization, column chromatography, reprecipitation, or the like. It is to be noted that the compound (I) and the other compounds may include one or more stereoiso er(s) such as optical isomer(s) and geometrical isomer(s) due tc asymmetric carbon atom(s) and double bond(s), and ail of such isomers and mixture thereof are included within the scope cf this invention. The ob ect compounds (I) and pharmaceutically acceptable salts thereof possess a strong inhibitory activity on the production of nitric oxide (NO) . Accordingly, the object compounds (I) and pharmaceutically acceptable salts thereof are expected to possess a nitric oxide synthase (NOS)-inhibitory activity or a NOS-production inhibitory activity. Accordingly, they are useful for prevention and/or treatment cf NO-mediated diseases such as adult respiratory distress syndrome, cardiovascular ischemia, myocarditis, heart failure, synovitis, shock (e.g., septic shock, etc.), diabetes (e.g., insulin-dependent diabetes ellitus, etc.), diabetic nephropathy, diabetic retinopathy, diabetic neuropathy, glomerulonephri is, peptic ulcer, inflammatory bowel disease (e.g., ulcerative colitis, chronic colitis, etc.), cerebral infarction, cerebral ischemia, migraine, rheumatoid arthritis, gout, neuritis, postherpetic neuralgia, osteoarthritis, osteoporosis, systemic lupus erythe atosis, rejection by organ transplantation, asthma, metastasis, Alzheimer's disease, arthritis, CNS disorders, and the like. In order to illustrate the usefulness of the object compound (I), the pharmacological test data of the representative compound of the compound (I) are shown in the following. Test Compounds : \ - Test: Assay for Inhibitory activity on the production cf Nitric Oxide The murine macrophage ceil line RA.W264.7 (American Type Culture Collection, No. TIB71! were used in this study. RAW264.7 cells were grown on F75 plastic culture flasks at 37°C, 5-. in Duibecco's modified Eagles medium (DMEM) supplement with L-glutamine, penicillin, streptomycin and 10 ? . heat-inactivated fetal bovine serum. They were removed from culture flasks by rubber cell scraper and were centrifuged and resuspended in DMEM without phenol red. They were plated in 96-well microliter plates (10 2 ceils per well} and allowed to adhere for 2 hours. The test samples were added and preincubated for 1 hour. Thereafter the cells were activated by both of lipopolysaccharide (LPS) (I μg/mi) and interferon γ (INF γ) (3 u/ml) for 18-24 hours ana were mixed with an equal volume of Griess reagent (1% sulfanilamide/O.1 % N- naphthylethylenedia ine dihydrochloride/2.5 > H3PO4) and incubated at room temperature for 10 minutes. The absorbance was read at 570 n using microplatereader and N0 was measured using NaN0 2 as a standard. Test result For therapeutic administration, the object compounds (I! of the present invention and pharmaceutically acceptable salts thereof are used in a form of the conventional pharmaceutical preparation in admixture with a conventional pharmaceutically acceptable carrier such as an organic or inorganic solid or liquid excipient which is suitable fcr oral, parenteral or external administration. The - 3c - pharmaceutical preparation may be compounded in a solid fo such as granule, capsule, tablet, dragee or suppository, o in a liquid form such as solution, suspension or emulsion injection, intravenous drip, ingestion, eye drops, etc. I needed, there may be.included in the above preparation auxiliary substance such as stabilizing agent, wetting or emulsifying agent, buffer cr any other commonly used additives. The effective ingredient may usually be administered with a unit dose of 0.C01 mg/kg to 500 mg/kg, preferably 0. mg/kg to 10 mg/kg, 1 to 4 times a day. However, the above dosage may be increased or decreased according to age, wei and conditions of the patient or the administering method. Preferred embodiments of the object compound (I) are follows. W is lower alkyl, 1,2-methylenedioxyphenyI, phenyl, naphth fluorenyl which may have oxo, pyrrolyl, pyridyl, fury which may have phenyl, thienyl or a group cf the formula : [in which -"- is hydrogen, halogen, lower alkyl, nitro, di (lower) alkylamino, amino, hydroxyamm or lower alkoxy, Q is CH or N, L is a bivalent radical selected from - 3 ' m which Y is CH or N, Z is NH, 0 or Ξ, and ZZZ. is a single bond or a double bond) and (m whicn M is CH or N, ana J is CH cr N) , A- is lower alkylene (more preferably Cη - ^ alkylene; V more preferably methylene), -NHCO-, -C- ( which V is 0 or S) , or -S0 2 ~, T is hydrogen, phenyl or naphthyi, each cf which may have 1 to 3 (more preferably one or two; most preferably one) substituent (s) selected from the group consisting of hydroxy, protected hydroxy (more preferably acyloxy) , halogen, lower alkoxy and lower alkyl; imidazolyl; pyridyl; indolyl; thienyl; furyl; hydroxy; lower alkanoyloxy; heterocycliccarbonylcxy(more preferably pyridylcarbcnyloxy) ; heterocyclic(lower) alkanoyloxy (more preferably pyridyi_(lower) alkanoyloxy cr piperidyi (lower) alkanoyloxy) ; [di (lower) alkylamino] (lower)alkanoyloxy; ar (lower)alkoxy (more preferably phenyl (lower)alkoxy) ; sulfooxy; mercaptc; lower alkylthio; mono (or di or tri)phenyl (lower) alkylthio; [di (lower)- alkylamino] .lower) aikanoylthic; am o; acyla inc [mere preferably aroylammo (more preferaoiy benzcylam o) , lower alkanoylamino or ar(lower■alκoxycarbonylammo ( more preferably phenyi (lower)alkoxycarbonylam o) ] ; guanidmo or guanidmo naving pnenylsulfcnvl substitute with 3 lower alkyl and lower alkoxy; or a group of the formula : (in which R 2 is hydroxy, phenyl (lower)alkoxy (more preferably benzyloxy) ; morpholinyl; piperazinyl which may have 1 tc 3 (mere preferably one cr two--_=πtost preferably one) suitable substituent(s) (more preferably substituent selected from the group consisting of lower alkyl, carboxy, protected carboxy (more preferably esterified carboxy; most preferably lower alkoxycarbonyi), carboxy(lower) alkyl, protected carboxy(lower) alkyl (more preferably esteπfieα carboxy(lower) alkyl; most preferably lower alkoxycarbonyi (lower) alkyl) , heterocyclic group (more preferably pyridyl or pyrimidinyl) , cycle (lower)alkyl, aryl (more preferably phenyl), hydroxy(lower)alkyl, protected hydroxy(lower)alkyl (more preferably acyloxy(lower) alkyl) , di (lower) alkylamino(lower) alkyl and acyl (more preferably lower alkanoyl or lower aikoxycaroonyl) ; piperidyi wnich may have I tc 3 ( _πore preferably one or two; most preferably one) suitable substituent (s) (mere preferably heterocyclic group; most preferably piperidyl) ; pyrrolidinyl; thiomorphoiinyl; homopiperazinyl which may have 1 to 3 (more preferably one or two; most preferably one) suitable substituent (s) (more preferably lower alkyl); piperazinio which may have two or three (more preferably two) suitable substituent (more preferably lower alkyl) ; piperidyloxy which may have 1 to 3 (more preferably one or twc; most preferably one) suitable substituent (s) (more preferably lower alkyl) ; or amino having one or two substituent(s) selected from the group consisting of lower alkyl, ar(lower)alkyl (more preferably phenyl (lower) alkyl) , cyclo(lower) alkyl, heterocyclic group (more preferably morpholinyl or pyrazolyl), mono (or di or tri)hydroxy(lower) alkyl (more preferably di(or tri)hydroxy(lower)alkyl) , mono(or di or tri) (protected hydroxy) (lower)alkyl (more preferably di (or tri)acyloxy(lower)alkyl) and [di (lower)alkylamino] (lower) alkyl [more preferably mono(or di) (lower)alkylamino, cyclo(lower)alkylamino, phenyl (lower) alkylamino, morpholinyiamino, pyrazolylamino, [di (lower)alkylamino] (lower)alkylamino, amino having lower alkyl and [di (lower) alkylamino] (lower)alkyl, di (or tri)hydroxy(lower) alkylamino] ; A 2 is lower alkylene (more preferably C- | _-C 2 alkylene) , R 8 is hydrogen or lower alkyl, or R 8 and a group of the formula : -A 2 -T are linked together to form a group of the formula : R 3 is hydrogen; phenyl which may have 1 to 3 (more preferably one or two; most preferably one) suitable substituent (s) [more preferably substituent selected from the group consisting of hydroxy, protected hydroxy (more preferably phenyl (lower) alkoxy) , lower alkoxy and halogen] ; hydroxy; protected hydroxy (more preferably acyloxy); cyclo(lower)alkyl; lower alkylthio; pyridyl; imidazolyl which may have acyl (more preferably tolylsulfonyl) ; thienyl; or furyl; A 3 is bond or lower alkylene, R 9 is hydrogen or lower alkyl, or R 9 and a group of the formula : -A 3 -R 3 are linked together to form a group of the formula : R^ is carboxy, esterified carboxy (more preferably lower alkoxycarbonyi), piperazinylcarbonyl which may have lower alkyl, tetrahydroquinolylcarbonyl, or a group of the formula : R- -CO-N (in which R 5 is hydrogen cr lower alkyl, ana R 6 is hydrogen; phenyl; phenyl (lower)alkyl which may have 1 to 3 (more preferably one or two; most preferably one) suitable substituent(s) (more preferably.substituent selected from the group consisting of lower alkyl, lower alkoxy, carboxy, protected carboxy (more preferably esterified carboxy; most preferably lower alkoxycarbonyi) , mono(or di or tri)halo(lower) alkyl (more preferably trihalo(lower) alkyl) , di (lower)alkylamino, [di (lower)alkylamino] (lower) alkyl, [di (lower)alkylamino] (lower)alkoxy, halogen and heterocyclic group (more preferably triazolyl, piperazinyl, pyrazolyl or imidazolyl) which may have lower alkyl) ; [di (lower)alkylamino] (lower)alkyl; pyridyl(lower)alkyl which may have 1 to 3 (more preferably one or two; most preferably one) suitable substituent (s) (more preferably substituent selected from the group consisting of lower alkyl, lower alkoxy, halogen, di(lower)alkylamino, protected amino (more preferably acylamino; lower alkanoylamino) , heterocyclic group (more preferably pyridyl) and lower alkylthio), quinolyl (lower)alkyl, quinoxalinyl (lower)alkyl, pyrimidinyl (lower) alkyl, pyrazinyl(lower)alkyl, pyrazolyl (lower)alkyl or benzimidazolyl (lower)alkyl) , or R 4 and a group of the formula : -A-^-R- 5 are linked together to form (in which R i0 is phenyl (lower) alkyl) , with proviso that when M is CH, and J is CH, then Q is N. More preferred embodiment(s) cf the object compound (i: are represented by the following formulae (A) - (D) . wherein W is lower alkyl, I,2-methylenedicxyphenyl, phenyi, naphthyl, fiuorenyl which may have oxo, pyrrolyl, pyridyl, fury! which may have phenyl, thienyi cr a group of the formula : • in which R- is hydrogen, halogen, lower alkyl, itro, di (lower) alkylamino, amino, hydroxyamino or lower alkoxy, Q is CH or N, L is a bivalent radical selected from in which Y is CH or 2 , Z is NH, C cr S, an ZZZ. is a single bond or a double oor.d. and 1 (in which M is Cr. or N, ana N)], A. 1 is lower alkylene (more preferably C-.- alkylene; V II more preferably methylene) , -MHCO-, -C- (in which V is 0 or S) , or -SO ? -, P. is morpholinyl, A ~ is lower alkylene (more preferably Cτ_-C 6 alkylene) , R 8 is hydrogen or lower alkyl, R J is hydrogen; phenyl which may have 1 to 2 (more preferably one or two; most preferably one) suitable substituent(s) [more preferably substituent selected from the group consisting of hydroxy, protected hydroxy (more preferably phenyl (lower) alkoxy) , lower alkoxy and halogen] ; hydroxy; protected hydroxy (more preferably acyloxy); cyclo (lower)alkyl; lower alkylthio; pyridyl; imidazolyl which may have acyi (more preferably tolylsulfonyl) ; thienyl; or furyl; A~ is bond or lower alkylene, R 9 is hydrogen or lower alkyl, or R 9 and a group of the formula : -A. -R- 3 are linked together to form a group of the formula : R 4 is carboxy, esterified carboxy (more preferably lower 81 - 44 - alkoxycarbonyi), piperazinylcarbonyi which may have lower alkyl, tetrahydroquinolylcarbonyi, or a group of the formula : (in which R 5 is hydrogen or lower alkyl, and R 6 is hydrogen; phenyl; pyridyl(lower) alkyl substituted with 1 to 3 (more preferably one or two; most preferably one) suitable substituent (s) (more preferably substituent selected from the group consisting of lower alkyl, lower alkoxy, halogen, di (lower)alkylamino, protected amine (more preferably acylamino; lower alkanoylamino) , heterocyclic group (more preferably pyridyl) and lower alkylthio), quinclyi .lower) alkyl, quinoxalinyl (lower)alkyl, pyrimidinyl (lower) alkyl, pyrazinyl (lower)alkyl, pyrazolyl (lower) alkyl or benzimidazolyl (lower) alkyl; , or R 4 and a group of the formula : -A. 3 -R J are linked together to form (in which R 10 is phenyl (lower) alkyl) , with proviso that - when M is CH, and J is CH, then Q is N. wnerem W is lower alkyl, 1,2-methylenedioxyphenyI, phenyl, naphthyl, fluorenyl which may have oxo, pyrrolyl, pyridyl, furyl which may have phenyl, thienyl or a group of the formula : [in which R- is hydrogen, halogen, lower alkyl, nitro, di (lower)alkylamino, amine, hydroxyamino or lower alkoxy, Q is CH or N, L is a bivalent radical selected from (in which Y is CH or N, Z is NH, 0 or S, and ZΣ is a single bond or a double bond) and 1 - 46 - (in which M is CH or N, and J is CH or N) ] , A 1 is lower alkylene (more preferably Ci -C Δ alkylene; V more preferably methylene), -NHCO-, -C- (in which V is or S) , or -S0 2 -, R ~ is lower alkylpiperazinyl, A 2 is lower alkylene (more preferably d-C 2 alkylene), p R is hydrogen or lower alkyl, R 3 is hydrogen; phenyl which may have 1 to 3 (more preferab one or two; most preferably one) suitable substituent ( [more preferably substituent selected from the group consisting of hydroxy, protected hydroxy (more preferably phenyl (lower)alkoxy) , lower alkoxy and halogen] ; hydroxy; protected hydroxy (more preferably acyloxy); cyclo(lower)alkyl; lower alkylthio; pyridyl; imidazolyl which may have acyl (more preferably tolylsulfonyl) ; thienyl; or furyl; A 3 is bond or lower alkylene, R 9 is hydrogen or lower alkyl, or R 9 and a group of the formula : -?. -R^ are linked together to form a group of the formula : R 4 is carboxy, esterified carboxy (more preferably lower alkoxycarbonyi), piperazinylcarbonyl which may have lower alkyl, tetrahydroquinolylcarbcnyi, cr a group cf the formula : (in which R 3 is hydrogen cr lower aikyl, and R D is hydrogen; phenyl; phenyl (lower) alkyl which may have 1 to 3 (more preferably one or two; most preferably one) suitable substituent (s) (more preferably substituent selected from the group consisting of lower alkyl, lower aikcxy, carboxy, protected carboxy (more preferably esterified carboxy; most preferably lower alkoxycarbonyi) , mono(cr di or tri)halo (lower) alkyl (more preferably trihalo (lower) alkyl) , di (lower)alkylamino, [di (lower) alkylamino] (lower) aikyl, [di (lower) - alkylamino] (lower) alkoxy, halogen and heterocyclic group (more preferably triazolyl, piperazinyl, pyrazolyl or imidazolyl) which may have lower alkyl); [di (lower)alkylamino] (lower) alkyl; pyridyl (lower)alkyl which may have " 1 to 3 (mere preferably one or two; most preferably one) suitable substituent (s) (more preferably substituent selected from the group consisting cf lower alkyl, lower alkoxy, halogen, di (lower) alkylamino, protected amino (more preferably acylamino; lower alkanoylamino) , heterocyclic group (more preferably pyridyl) and lower alkylthio), quinoiyl (lower) alkyl, quinoxalinyl (lower)alkyl, pyrimidinyl (lower) alkyl, pyrazinyl (lower)alkyl, pyrazolyl (lower) alkyl or 1 - 48 - benzimidazoiyl (lower) alkyl) , cr R 4 and a group cf the formula : -A 3 -R are linked together to rorm (in which R 10 is phenyi (lower)alkyl) , with proviso that when M is CH, and J is CH, then Q is N. wherein W is lower alkyl, 1,2-methylenedioxyphenyl, phenyl, naphthyl fluorenyl which may have oxo, pyrrolyl, p ' yridyl, furyl which may have phenyi, thienyi or a group of the formula : [in which R~ is hydrogen, halogen, lower alkyl, nitro, di (lower)alkylamino, ammo, hydroxyamino or lower alkoxy, Q is CH or N, L is a bivalent radical selected from (in which Y is CH or N, Z is NH, 0 or S, and Z Σ. is a single bond or a double bond) and (in which M is CH or N, and J is Cή' or N) ], A- is lower alkylene (more preferably C-i-C^ alkylene; V more preferably methylene) , -NHCO-, -C- (in which V is 0 or S) , or -S0 2 -, A .2- is lower alkylene (more preferably C^-C 2 alkylene) I , R 8 is hydrogen or lower alkyl, R 3 is hydrogen; phenyl which may have 1 to 3 (mere preferably one or two; most preferably one) suitable substituent(s) [more preferably substituent selected from the group consisting of hydroxy, protected hydroxy (more preferably phenyl (lower) alkoxy) , lower alkoxy and halogen] ; hydroxy; protected hydroxy (more preferably acyloxy); cyclo (lower)alkyl; lower alkylthio; pyridyl; imidazolyl which may have acyl (more preferably tolylsulfonyl) ; thienyl; or furyl; A. 3 is bond or lower alkylene, R 9 is hydrogen cr lower alkyl, or R 9 and a group of the formula : -A 3 -R 3 are linked together to form a group of the formula : R is carboxy, esterified carboxy (more preferably lower alkoxycarbonyi), piperazinylcarbonyl which may have lower alkyl, tetrahydroquinolylcarbonyl, or a group of the formula : (in which R 5 is hydrogen or lower alkyl, and R 6 is hydrogen; phenyl; phenyl (lower)alkyl which may have 1 to 3 (more preferably one or two; most preferably one) suitable substituent (s) (more preferably substituent selected from the group consisting of lower alkyl, lower alkcxy, carboxy, protected carboxy (more preferably esterified carboxy; most preferably lower alkoxycarbonyi), mono (or di or tri)halo(lower) alkyl (more preferably trihalo (lower)alkyl) , i (lower)alkylamino, [di (lower)alkylamino] (lower)alkyl, [di (lower)- alkylamino] (lower) alkoxy, halogen and heterocyclic group (more preferably triazolyl, piperazinyl, pyrazolyl or imidazolyl) which may have lower - 01 - alkyl); [di (lower)alkylamino] (lower) alkyl; pyridyl (lower)alkyl which may have 1 to 3 (more preferably one or two; most preferably one) suitable substituent ( s ) (more preferably substituent selected from the group consisting of lower alkyl, lower alkoxy, halogen, di (lower) alkylamino, protected amino (mere preferably acylamino; lower alkanoyiamino) , heterocyclic group (more preferably pyridyl) and lower alkylthio), quinolyl (lower)alkyl, quinoxalinyl (lower) alkyl, pyrimidinyl (lower) aikyl, pyrazinyl (lower)alkyl, pyrazolyl 'lower) alkyl or benzimidazolyl (lower)alkyl) , or R 4 and a group of the formula : -A-^-R- 5 are linked together to form (in which R 10 is phenyi (lower) alkyl) , with proviso that when M is CH, and J is CH, then Q is N. wherein W is lower alkyl. 1,2_i:iethylenecliox ^^n y i, p envl, nao^u rluorenyl which may have oxo, Py oly: , ^^ ' wh i ch may have phenyl, thienyl or ' a group cf the formula : fin which Rl is hydroαen, halogen, l0Hβr ,,,.„., ^ di ( lower ) aUcyl it aino, amino. hydroxyamin or lower alkoxy, Q is CH or N, 1 is a bivalent radical selec t ed from ( in which Y is CH or N, Z is NH, 0 or S, and is a single bond or a double bond) and ( m which M is CH or N, and J is Cή ' or N) ] , s lower alkylene (more preferably Cτ_-C 4 alkylene ; - -ϊ - V more preferably methylene), -NHCO-, -C- (in which V is 0 or S) , or -S0 2 -, T is hydroxy or lower alkylthio, A'' is lower alkylene (more preferably C-j-C 2 alkylene), R 8 is hydrogen or lower alkyl, R J is hydrogen; phenyi which may have 1 to 3 (more preferably one or two; most preferably one) suitable substituent (s) [more preferably substituent selected from the group consisting of hydroxy, protected hydroxy (more preferably phenyl (lower) alkoxy) , lower alkoxy and halogen] ; hydroxy; protected hydroxy (mere preferably acyloxy); cycle(lower) aikyl; lower alkylthio; pyridyl; imidazolyl which may have acyi (more preferably tolylsulfonyl) ; thienyl; or furyi; A 3 is bond or lower alkylene, R 9 is hydrogen or lower alkyl, or R 9 and a group of the formula : -A 3 -R" are linked together to form a group of the formula : R 4 is carboxy, esterified carbox (more preferably lower alkoxycarbonyi), piperazinylcarbonyl which may have lower alkyl, tetrahydroquinclylcarbcnyi, cr a group o: the formula : -CO-N (in which R,5 is hydrogen or lower alkyl, and ,6 is hydrogen; phenyl; [di (lower)alkylamino] (lower)alkyl; pyridyl (lower)alkyl substituted with 1 to 3 (more preferably one or two; most preferably one) suitable substituent (s) .more preferably substituent selected from the group consisting of lower alkyl, lower alkoxy, halogen, di (lower)alkylamino, protected amine (more preferably acylamino; lower alkanoylamino) , heterocyclic group (more preferably pyridyl) and lower alkylthio), quinolyi (lower) alkyl, quinoxalinyl (lower)alkyl, pyrimidinyl (lower) aikyl, pyrazinyl (lower)alkyl, pyrazolyl (lower) alkyl or benzimidazolyl (lower) alkyl) , or R^ and a group of the formula : -A. 3 -R 3 are linked together to form (in which R 0 is phenyl (lower) alkyl) , with proviso that when M is CH, and J is CH, then C is N. The following Preparations and Examples are given for the purpose of illustrating the present invention in detail In the following Examples and Preparations, there are employed the other abbreviations addition to the abbreviations adopted by the IUPAC-IUB (Commission on Biological Nomenclature) . The abbreviations used are as follows. Ac acetvi cHex I 3-cyclohexyl-L-alanme -Ala- 3- (2-furyl)-L-alanine 3- (3-furyl)-L-alanine - (2-thienyl)-L-alanine Arg L-arginine Asp L-aspartic acid D-Asp D-aspartic acia Boc t-butoxycarbonyl Bz benzoyl Bzl benzyl Bzl(4-COOH) 4-carboxybenzyl Bzl(4-COOMe) 4-methoxycarbonylbenzyl Bzl(4-OH) 4-hydroxybenzyl Bzl(4-NMe 2 ) 4-dimethylaminoben∑yl Bzl(4-CH 2 NMe 2 ; 4- (dimethylaminomethyl)benzy] Bzl (4-C1) 4-chlorobenzyi Bzl(4-Br) 4-bromobenzyi Bzl(4-F. 4-fluorobenzyi Bzl(4-OMe) 4-methoxybenzyl Bzl (2-Me) 2-methylbenzyl Bzl (3-Me) 3-methylbenzyi Bzl ( -Me) 4-methylbenzyi Bzl(4-CF 3 ) 4-trifluoromethylbenzyi Bzl (4-0-(CH 2 ) 2 -NMe 2 ) 4- (2-dimethylaminoethoxy)benzyl N Bzl(4—N 4- (1-iH-imidazolyl)benzyl Bzl(4--N N-Me) 4- (l-methylpiperazin-4-yl)benzyJ Bzl(4 -Me, 4-(l-methyipyrazoi-3-yl)benzyl Bzl(4~N ' ^J) 4- (l-lH-triazolyl)benzyi \___-N Cys L-cysteine Et ethyl Glu L-glutamic acid Gly glycine His L-histidine Leu L-leucine Lys L-lysine Me methyl MePhe N-methyl-L-phenyialanine Met L-methionine INal 3- (1-naphthyl) -L-aianine 2Nal 3-(2-naphthyl) -L-alanine INaph 1-naphthyi 2Naph 2-naphthyl Nle L-norleucine Nva L-norvaline Orn L-ornithine n Pr n-propyl Phe L-phenylalanine D-Phe D-phenylalanine Phe(4-Cl) 3- (4-chlorophenyl) -L-alanine Phe(4-Me) 3-(4-methylphenyl)-L-alanine Phg (S) -2-phenylglycine 4Pm 4-Pyrimidinyl 2Pyala 3-(2-pyridyl)-L-alanine 3Pyala 3- (3-pyridyl)-L-alanine 4Pyala 3- (4-pyridyl)-L-alanine 2Py 2-pyridyl 3Py 3-pyridyl 4Py 4-pyridyi 3Py(6-NHAc) (6-acetylaminopyridin-3-yl) 3Py(5-Br) (5-bromopyridin-3-yl) 3Py(6-Cl) (6-chloropyridin-3-yl) 3Py(6-NMe 2 ) (6-dimethylaminopyridin-3-yl) 3Py(β-OEt) (6-ethoxypyridin-3-yl) 3Py(4-OMe) (4-methcxypyridin-3-yl) ~ 3Py(5-OMe) (5-methoxypyridin-3-yl) 3Py(6-OMe) (6-methoxypyridin-3-yl) 3Py(6-Me) (6-methylpyridin-3-yi) 3Py(6-SMe) (6-methylthiopyridn-3-yi) 3Py(6-n-Pr (6-n-propylpyridin-3-yl) 3Py(6-2Py) [6- (2-pyridyl)pyridin-3-yl] 3Py(6-3Py) [6- (3-pyridyl)pyridin-3-yi] 2Qu 2-quinolyl 3Qu 3-quinolyl 6Qu 6-quinolyl - 55 - 7Qu 7-quinolyl Ser L-serine Thr L-threonine Tos p-toiuenesulfonyl Trt trityl Tyr L-tyrcsine Val L-vaiine Z benzyloxycarbonyi Z(2-Ci; 2-chiorobenzyioxycarbonyi - to be continued on the next page - The Starting Compounds used ana the Object Compounds obtained in the following Preparations and Examples are given m the Table as below, in which tne formulae cf the Starting Compounds are in the upper and the formulae of the Ob:ect Compounds are in the lower, respectively. T a i_ - O '-' - Preυaration No rcrmu-_.a Boc l c_ Preparation No. or u a 5-(4! 5-(5) Preparation Mo. Formula 3oc-Asp-0Me 9-(l) H-2 Boc-?he-N- (CH 2 ) 2 N ( M « ) 2 Me 9- (2: - oo - o / - Preparation No. Me 14-(1) Me 14-(2; : ~ - - 7 ■ 981 - 73 - - I H - 1 Preparation Nc. c r mu — a 36 37 TCS τ| Boc-Hiε-OH 38 .cs ^ Me / BGC-HIS-N \ 3zl 981 o - - 76 - -1 ) Boc-Phe-M Boc-Phe-OH 39-(16) Boc-?he-N 'CH 2 -3Py (6-Ci: Boc-Phe-OH 39-(17] .Me Boc-Phe-N 'CH->-3Py(6-Me) Boc-Phe-OH 39-(18) Boc-Phe-OH 39-(19) -3?y (5-Ci 1 - 80 Preparation No, ror ula -Me Boc-Phe-N: -Bzi(4-CH~.NMe~. 42-(3) -Me H-Phe-N; -Bzl(4-CH-.NMe-> 42-(4 -Me Boc-Phe-N: -Bzl(4-Cl) 42-(5) -Me H-Phe-N; -B2K4-C1) -Me Boc-Phe-N -Bzl(4-Br: 42-(61 -Me H-Phe-N! ~Bzl(4-Br! -Me Boc-Phe-N; -5zi(' 42-(7; -Me H-Phe-N: "Bzl(4-F) - 32 - _ o T _ Preparation No, "crmula -Me 3oc-Phe-N; -CH ? -3Py(5-Cl 42- (13) -Me Boc-Phe-N: < --? -3Py 42-(14; -Me H-?he-N: -CH 9 -3?y -Me Boc-Phe-N. -3zi (4-OMe) 42-(15] -Me H-Phe-N: * Bzl ( -OMe) -Me Boc-Phe-N: * Bzl ( 4 -Me) 42-(16) -Me E-Phe-N: ά. -Ma -Me Bcc-Ser-N -Bzl 42-(17) -Me HCl-H-Ser-N: • Bzl Preparation Nc. Formula -M. 5oo-Leu-N; 42- (18j Wo HCi -H-Leu-N -Bzl -Me Boc-Phe-N; -3zl(4-CF-s) 42-(19) -Me HCi -H-Phe-N: • Bzl(4-CF 3 ; -Me Bcc-D-Phe-N: -Bzl 42-(20) -Me HCl-H-D-Phe-N: -Bzl 43-(l) 43-(2] -Me Boc-D-AsD-Phe-N-. -Bzl 1 - 85 - Preparation Nc. ; Q J^m. __ ■ -Me Boc-Asp-Phe-N -Bzl 44 - f Boc-D-Asp-D-Phe-N ϋ Bzl 45- Me -Me Boc-D-Asp-D-Phe-N-i -Bz] 45-{2: - 37 - Preparation No, Fcrmu.a Me 46- (5) 3oc-Asp-0H 46-(6) - 39 - Preparation No. | rcr uia 46- (9) 46-(10; Preparation No, Formula 46-(li: 46-(12) 3?y (β-Ci) 6981 1 - 95 - Preparation No, rormula 46-(19; ?v BOC 46-(20) ! 4-OMe) Preparation No Formul 46-(2i) 46- (22! Preparation No. ormu a 46-(23) 3o 46- (24: { -; _ oa _ Preparation No tormu i -Me 3cc-Giv-N ■ Bzl 50- (1) 5o -Me 3oc-?hg-N: • _3Z_ 50-(2) Bzl Me Boc-Tyr-N ^ ' 3zl 50-(3) Preparation No Formula 50- (4) -Me Boc-Tyr-N- -Bzl 50-(5] , ^ __-Me ( Bos-Phe-N . ^J (CH 2 ; 2 50- (6: J 2 Preparation Nc. rormu_a ^-Me Boc-Phe-N-^ ^2D . _ - _. 5C-(10) -Me Boc-Phe-Nl -r '-.- Pv >o-(iι: -Me Boc : he-N ■ CH - •4Py -Me Boc-Phe-N-. -Bzl (4-COOMe) 50- (12) l (4-COOMe; - i . - Preparation No, Formula -Me Soc-Phe-Nl -Ezi (4-COOMe 50-(13) (4-COOMe) -Me Eoc-Phe-N- -3zi (4-NMe ? ) 50-(14) -Me 3oc Fhe-N: -Bzl (4-NMe ) 51-(i; Preparation Nc, Formula Me ^ N' -Me Boc-AsD-Pr.e-N^ -Bzi(4-NMe ) 51-(2) Me Boc " > - 3) Me (4-CH NMe 2 ) ,υc - Preparation No, Formula 51- (6) 51- (7; (4-F) .OS - Preparation No. Formula {€-Cl; 51- (10) 5i-(i: (6-Me) 1 981 Preparation Nc. Formula 51-(14) 5-Ci) 51-(15) -3?y(β- •- ; Preparation No, Form; 51- (16) 3?y 51-(17; . ■ Preparation No. rormu a 51-(18; 51-(19) - 4-0Me. _ - 1 Preparation No. Formula 51- (20) Me I 51-(21) 1 - 115 - Preparation No. Formui. 51-(22) 51-(23) _ i ι c - Preparation No, Formula l (4-COOMe) 51-(28) (4-COOMe) 4 _ C00Me) 51- (29) (4-COOMe) 6981 - 119 - 81 - 120 - 6981 _ 1 ~~ - 6981 - 123 - PreDaration No -CHo- Boc-2Pvala-Phe-N: • -)- ?v "Me 58-(δ) K-90 yaia-Phe-N ^ • 3?v .Me K-Phe- 59 Me -Me Boc-Cvs-Phe-NC H-?he-N: 'ϋn. -3?y(6-c: 60-(i; Me Boc-Ser-Phe-N T CH- -3?v(c-cι; -Me H-Phe-N: -3zi 60-(2) Trt »Me Boc-Cvs-Phe-N T 3z: 60-(3) __. -Me Boc-Ser-Phe-K — _-. _ ^ ,3Qu __,Me HCl-H-Phe-Nd-,,-, 60-(4 ' - ' • ?_. - 81 6981 - ' ~- Preparation No Formula -Me H-Phe-N: -CH- -3?y .6-2?y, 60-(2i: -Me Boc-Ser-?he-N-__-_„ TT _ ^ -3?y ( 6-2?yj "v-.H 'j " -Me H-Phe-N ^,.. -3Py(6-3?y) 60- (22) Me Boc-2Pyala-Phe-ϊC-A- Hr -3Py,β-: -Me H-Phe-N: -CH- -3Py(6-3Py) 60- (23) Me Boc-Ser-Phe-N l _-_-3Py ( 6-3?y) 60-(24; 60- (25) Bcc-Phe-?he--4___ .. , 3 D V 16981 Preoaration No Formula 60-(31) -Me H-Phe-N T CH,-- 3 ^ 6 - 3 ^' 60-(32) Me Boc-Met-Phe-N ^.-.. ^_.3Py(6-3Py Me H-Phe-N βzl 60-(33) -Me H-Phe-Nd, CH- -3Py(6-NMe 2 ) 60-(34) -Me Boc-Ser-Phe-Nd CH __-3Py ! 6-NMe 2 : Preparation No Formula -Me H-Phe-N τ : -CH- -3Qu 60- (35) -Me H-Phe-N: -Bzl 60-(36) -Me H-Phe-N: -Bzl 60-(37; 60- (38) 60- (391 _-_-Me Boc-His-Phe-N--^.-,-, 3Qu 16981 - 131 - Preoaration No. Formula 60- (40) -Me H-Phe-N: -Bz 60- (41 f Me όoc-Tyr-P e- ---l. p H- 60-(42) Boc-2Pyale-Phe-B M CΪ e- 2 J s ^^r^S 60- (43) Me K-P e-U .. -3P 60- ;44 ____.3?y Preoaration No. Formul -Me Boc-2Nal-Phe-N~ -Bzl 61-(15) Me H-2Nal-Phe-N ~ Bzl Me Boc-His-P e-N: -CH- -3?v ( 6-Me: 61- (16) Me H-His-Phe-N T CH- -3Pv(ό-Me Me Boc-MePhe-Phe-N Bzl 61-(17) Me H-MePhe-Phe-N= Bzl Me Boc-2Pyala-Phe-Nd CH- .3Qι 61-(18; -Me H-2Pyala-?he-N _l CH ^ — -3Qu 61-(19) H-Ser 981 - 136 - 981 - 137 - Preoaration No. Formula -Me Boc-Ser-?he-N^ CK ^ 3Py ( β _^ e9 61-(35) Me H-Ser-P e-NtT CH-,--3Py(6-NMeo) Bzl Me Boc-Ser-Phe-N L CH- ) Li 61- (36) 61-(37) 61-(38) Preoaration No. Formula Me Boc-lNal-Phe-N= B2 - 61-(44: Me K-lNal-Phe-NC Bzl Me Boc-His -Phe-N= , CH 3Pv __.- • 61-(45) Me H-His-Phe-l^ CH- -3Py Me Boc-2Pyala-Phe-N ^ CK — 3Py(6-Me) 61-(46] Me H-2Pyala-P e-N= rH — 3Py(6-Me) Me Boc-3Pyala-Phe-N= Bzl 61-147) Me H-3Pyala-?he-Nd Bzl Mg Boc-P e (4 -C1 ) -P e- N dg 61-(48: -Me H-P e(4-Cl)-P e-N=^ 3zi 6981 - 142 - Preparation No Formula 61-(49) Me I H-Cys-OH 62-(i; Me I Boc-Cys-OH 62-(2: H 2 N-Bzl(2-Me) Boc-NH-Bzi (2-Me) 62-(3; H 2 N-Bzi (3-Me; Boc-NH-Bzl (3-Me) Boc-2Nal-0H 63-(l) -Me Boc-2Nal-N= -Bzl Boc-MePhe-OH 63-(2 ' -Me Boc-MePhe-N ^ _ B - Me I Boc-Tyr-OH 63-(3! Me Boc-ϊTvr- —-Mpe -i Preparation No, Formula Boc-Phe-OH 63-(4) Me Boc-Phe-NC B2l (3 _ Me) Boc-Phe-OH 63-(5) _. ... Me Boc-Phe-N ^ B2l(2 _ Me) Boc-Phe-OH 63-(6) Boc-Phe-Nd Me CH - -4Pm Boc-Phe-OH 63-{7) Boc-Phe-OH 63-(8) —Me Boc-Phe-N-_-_ ^cκ _-2Qu Boc-Phe-OH 63-(9! — Me Boc-Phe-N-^ rH _,7Qι Boc-Phe-OH 63-(10! -Me Bcc-Phe-N: -CH 2 j ύ N Preparation No. Formula 3oc-Phe-0H 63-(ll) -Me Boc-Phe-N; -CH,-3Py(6-3Py) Boc-Phe-OH 63-(12) Boc-Phe-N -Me ■ cH 9 - 3p y (6 - 2p y ) Boc-Val-OH 63-(13) .Me Boc-Vai-N - B2l cHex Boc-Ala-OH 63-(14) Boc-Phe-OH 63-U5) -Me ^ Boc-Phe-N:: -Bzl ( —N N-Me) Boc-4Pyala-0H 53- (15) Me Boc-4Pyaia-N B_zl Boc-Phe-OH 63-(17) „—Me Boc-Phe-_v-- ^CH^- _3Qu .45 - 81 - 14. 6981 - 14 ' Preoaration No, Formula Boc-3Pvaia-0H 63- (30) -Me Boc-3Pvaia-N= -Bzl 3oc-Nle-0H 63-(31) -Me Boc-2Nal-N= -Bzl 64-(i: Me H-2Nal-N= Bzl Boc-MePhe-N= -Me -Bzl 64-(2) H-Me?he-NF= B2l 64-(3) Me Boc-Phe-N^ * 3zl,(,3,-Me) 64-(4) Me H-Phe-N= 32l(3 _ Me . 16981 - 148 - Preparation No. rormu__5 -Me Boc-?he-N« -3zi(2-Me) 64-(5) -Me H-Phe-N= -Bzi(2-Me, -Me Boc-Phe-N* -CH- ,4?_τ. 64-(6) u_ -Me Phe-N s -CH- ,4Pm 64-(7: 64-(8) H-Phe-Nd ' „ 2 -- -Me Boc-Phe-N ,7Qu -CH- 64-(9) -Me H-Phe-N<. C " E / 7 Qu 6981 - 149 - Preoaration No, Formul 64-(10) -Me Bcc-Phe-N* -CH 9 " -3Py (€-3?v) 64-(li) -Me H-Phe-N^ -3Pv (6-3Pv) -CH - -Me Boc-Phe-N* -CH,- -3?v(6-2Pv 64- (12: H-Phe-N< {j 3Py(6-2Py) -Me Boc-Val-Ns -Bzl 64-(13) .Me H-Val- dg^ 64-(14) 81 - 150 - Preparation No. Formula -Me / 3oc-Phe-N= -Bzl(4--N N-Me) 64- (15) -Me H-Phe-Ndg 21( 4--N N-Me) Me Boc-4 Pyala-N= Bzl 64-U6; -Me H-4Pvala-N= -Bzl Me Boc-Phe-N= -3Qu CH- 64-(17) Me H-PtTe-N= : -3Qu CH- Bcc-Phe-Nd^ 6Qu 64-U8: Me Bcc-Phe-NdA- 3Py(6-NHAo) - h 2 64-(19) H-Phe-N= ^ — - 3Py(6-NHAc) 981 - 151 - 981 - 152 - Preparation No, Formula 64-(24) 64-(25) 64-(26! 64-(27) Me H-Phe(4-Cl)-Nd B R ^zl Preparation No. _. ormui 64-(28) 64-(29) Me H-Phe-Nd ' CH XX -Ms 3oc-lNal-N= 64-(30] Me K-lNal-N- ' Bzl -Me Boc-3?vala-N= -Bz: 64- (31) -Me •3Pyala-N= -3z: -Me Boc- le-N -Bzl 64-(32) H- le-NKlg^ 981 - 154 - 981 - 155 - 981 - 156 - 981 - 157 " Preoaration Nc >u-.a Me ri-.-n .e - d ; • 3] 'V >_ / Dι 65-(13! e K-Val-Nd Bzl 65-(14: 65-(15) 3oc 9-Asc0-Aia-N--A a '' _- Me H-Phe-Nd' Bzl. — N-Me! 65- (16) Preoaration Nc rp cr T-™.U-.ε ,M£ H-4?vaia-N= 65- (17 ' 65- (18) -Me K-Phe- = ,-. — 3Qu 65-(19) _— Me H-Phe-N< ^ .. — t> u 65- (20) ^ ,6Q. 981 - 159 " Precaration Nc : r_nu _ a -Me H-Phe-Nd- v-_.v_n -3Py J (6-NKAc 65- (21 Me H-Phe-Nd ' Bzl 65-(22) Bzl -Me Ecc-Giu-? e-N=C -3 * Z., - -_. 65-(23; 65- (24) 81 - 163 - 981 - 164 - 981 - 166 - 81 - 168 - 981 - 169 - 81 - 170 - Preparation Nc Form la 66-(30) Me Boc-Asp-?he (4- ci;-wd Bzl 66-(31) Me H-AsD-P e 4-CD-W- " 3zi 66-(32) Boc- 0Asp-P e-NdcJ : J 66-(33) 981 - 173 - 6981 - 174 " 81 - 177 - Precarat cn Nc :rmu_. 8C- (2, Me r^>ι H-N-CHf Boc-ASD-Orcl 81 Bcc-Aso-03: NMe 2 BOC-ASD-03Z1 82 NMe-, ! - 3cc-As -0H Bzl I -Me 3oc-Asp-? e-N= -Bzl 83 3cc-Asc-?he-N= -Me -Me Boc-Asc-i :-N= 84 - - 981 - 185 - 981 6981 - 133 - 81 - iV ~ ?reoara ~ icr. Nc . . Fcm .a ~ ] -__--Me 3oc-Met-N_.e-N ! ^^ .._. _,3Qu IOC- (ό) 100-(7) Me „ H-His-Nle-N= :H 3 u Boc 100-(8) 3oc y-Asp-? e ( -Me ) - β - p® , .00-(9) - 981 - 190 - Preoaration No Forir.ula 100- Me V -Me K-Aso-Phe-Ns --•• -3Pv ( 6-G--?r o "1 I Me Boc-Asp-Phe-N^,-.^- _,3Py ( δ-OMe'. Boc-Phe-OH iθl-(i) 3oc-?he(4- e , -OH lCi-{2) -M- Boc-Phe < -Me) -M' Boc-Nva-OH loi- (3; , Me Boc-Nva-N ! --.2 Z ι Q? - 6981 .94 - Preparation No. Formula 106-(8) .Me H-Phe-N ,3Py(5-OMe) * CH- 106-(9) .Me H-Phe-N ,3Py( 4-OMe) CH- 106-(10) .Me H-Phe-N ,3Py(5-Br) * CH> Preparation No, Formula 112-U) Me Boc-2Pyala-Met-N ; ,3Py(6-Me) CH- 112-(2) 112-(3) 16981 - 209 - Ξxamcle No -ormu ^ a 2-(l) 6981 - 210 - EκaitiDle No :ormu_a l 2-(2: 2-(3) . ' 6981 - 211 - 6981 - 212 - Example No. Formula 2-( 2-(7; 16981 - 213 - 16981 - 214 - 6981 - 215 - ExamDle No. Formula 2-(l -- . OBzl H-Asp-Phe-OEt • HCI 2-(13) 981 - 216 - Example No Formula 4-(i; 4-(2) 6981 - 217 - Examcie Nc. Formula 4- (3) COOEt 4-(4) 16981 - 218 - 6981 - 219 - Example No Formula 4-(β: 4-(9) 981 - 221 - Example No, Formula 4- (12! 4-(13) 981 - 222 - 6981 - 223 - 6981 - 224 - 6981 - 225 - Example No. Formula 4-(23) 4-(24) 6981 - 226 - Example No rormu.a 4-(25) 4-(26) 6981 - 227 - 16981 - 228 - ExaitiDle No. Formula l 4-(30) 4-(31) 6981 - 229 - Example No Formula 6981 - 230 - Example No. Formula Compound A 9-(l) 981 - 231 - 6981 - 232 - 1 - 233 - Example No. rormu.-.a 9- (6; 9-(7) 6981 - 234 - Examcie No. Formula 9-(8) 9-(9) 6981 - 235 - Example No. Formula 9-(10) 981 - 236 - 981 - 237 - 981 - 238 - 6981 - 239 - 6981 - 241 - 981 - 243 - 16981 -244 - 16981 - 245 - Example No Formula Me 10-(13) Me I 4-F) Me 10-(14) Me I 6981 - 246 - Examcl No Formula Me 10-(15) Me I Me I 10-{16) Me i -3?y(β-OMe) - 247 - Example No, Formula Me I 10-(17; Me Me I 10-(18: Me I ExamDle No, Formula Me 10- (19! Me Me I 10-(20) Me I (6-Cl) Example No. Formula Me I 10-(21 Me Me I 10-(22) Me I -3?y(6-Cl) Example No. Formula Me I 10-(23) Me Me I , 10-(24: Me I (6-Me Example No. rormuia Me I (6-Me: 10-(25) Me 10-(26) Example No. Formula 10-(27; 10-(28) Example No. Formula Me 10-{29] Me Me I ιo-(3o: Me I 6981 - 254 - Example No. Formula Me I 10-(31) Me I Me 10-(32) Me I - 255 - Example No. Formula Me 10-(33) Me I Me I (5 _ cl , 10-(34) Me I /16981 - 256- /16981 - 257 - 81 - 259 - 16981 - 260 - Example No. Formula 10-(43) 10-(44) 16981 - 261 - /16981 - 262 - Example No Formula K 10-(47 Me 10-(48: Me I (4- Me) Example No. Formula 10-(49] Me I 10-(50) Me - 264 - Example No, Formula 10-(5i; Me I 10-(52) Me I -CF 3 ) /16981 - 265 - - 266 - Example No. Formula 10-(55) Me H -Asp-Phe-N: -Bzl 10-(56) 10-(57) 6/16981 - 267 - - 268 - - 270 - Example No Formula 10-(64) 10-(65) 10-(66) - 271 - Example No. rrormuia 10-(67; 10-(68: 10-(69) 6981 - 272 - Example No, Formula 10-(70) ιo-(7i: 10-(72) 16981 - 273 - Example No. Formula 10-(73: 10- (74 l 10-(75; 16981 - 274 - Example No. Formula 10-(76) 10-(77: 10-(78) /16981 - 275 - 16981 - 276 - Ξxamcie No. •orπtu-a 10- (82) CKo-COOEt 4-COOMe) CH 9 -COOEt -COOMe) 10-(83) H- 5 -COOEi 4-COOMe: 16981 - 277 - Example No. Formula 10-(84) ) 4 . C00Me) 10-(85) 4 _ COOMe Examϋle No. Formula C HH 2 -COOEt l 10-(86; CH 2 -COOEt 10-(87) H 2 -COOEt l 16981 - 279 - Example No. Formula Me 10-{88: 10-(89) - 280 - Example No. Formula 10-(90; Me Me -COOMe) 4-C00Me: 6 - 281 - Example No, Formula 10-(92! n-(i: CH 2 CH 2 NMe 2 ll-(2) Boc I - 282 - 16981 - 283 - - 284 - Example No, Formula ll-(9) 12 6/16981 - 286 - /16981 - 287 - /16981 - 288 - Example No. Formula 18-(2: H 9 19 rCOOH -HO- COOH -H 2 0 L COOH /16981 - 289 - Example No Formula 20-(l) 20-(2) Example No Formula 20-(3! 21 - 291 - - 292 - - 308 - - 309 - - 310 - - 311 - O 9 1 - 312 - Example No. Formula Me H-Asp— Phe-_ Bzl (2-Me) 3 7 -(12) Me Me H-As — Phe-N: Izl (2 -Me) 3 7 -(13) 981 - 352 - 6981 - 353 - 96/16981 - 354 - Example No, Formula -U4) Me H-Ser-Nle-N ,3Py(6-Me> "CH2- -(15) Example No Formula -(16) -(17) _^ y ( J-OMe) Example No. Formula -(18) - (19) Me H-Asp-Phe-N 3Py(5-Br) H 2 / ,/ 3Py(5 - Br) Example No, Formula Me H-2Pyala-Phe-N .3Py * CH- -(l) Me H-2Pyala-Met-N ,3Py (6-Me) CH. -(2) .Me H-2Pyala-Met-N 3 Py ( 6-Me ) CH. 3py(6 . Me| Example No . Formula -(6) -(7) .Me H-Met-Met-N ,3Py(6-Me) CH- -(8; .Me H-Met-Met-N ,3Py(δ-Me) -CH- Pre p arat-mη 1 Start i ng Compound ( 2.00 g) , l-methylpipera r.e ( 414 mg ) , and 1- ydroxybenzotrιazole (559 mg) were dissclveα _.__ methylene chloride ( 50 ml) . The mixture was ce-coolec and : > l-ethyl-3- ( 3-dιmethylammopropyl ) carbodnmιαe nyαrochloriαe ( 793 mg ) was added thereto. The mixture was stirred ar tn i s temperature for 1 nour and at room temperature for 4 nours . The m i xture was concentrated under vacuum and tne res αue was d i luted i n water ana extracted with chloroform. Tne organ i c layer was washed with saturated sodium hyαrogencarbonate solut i on and brine. After evaporation, tne cru d e mater i al obta i ned was purified on a column of silica gel elut i ng w i th chloroform-methanol ( 60:1) to give Object Compound ( 2.34 g ) as an amorphous solid. MASS (FAB) (m/z) : 566 (M+H) + MR ( CDC1 3 , δ ) : 1.42 (9H, s) , 2.29 (3H, s) , 2.32-2.47 ( 4H, m ) , 2.52 (3 x 2/3H, s), 2.55-2.61 (IK, m ) , 2-77 ( 3 x 1/3H, s), 2.95-3.10 (2K, m) , 3.16-3.27 ( IH, m ) , 3.42-3.50 (2H, m) , 3.57-3.63 (2H, m ) , 4.07-4.32 (2 x 2/3H, ) , 4.47-4.58 (IH, m) , 4 . β2 ( 2 x 1/3H, d, J=15Hz) , 5.09-5.17 (1 H , m ; , 6.00-6.07 ( IK, m ) , 6.83-6.90 (IH, ) , 7.00-7.05 (IH, mj , 7.18-7.30 ( 8H, m) , 7.40 (1 x 1/3H, d, =8Hz ) , 7.43 ( 1 x 2/3H, d, J=8Hz) Pre p are n n ? The following object compound was obtained according tc a s i milar manner to tnat of Preparation 1. Mass ( FAB) (m/z) : 553 (M+H) ~ NMR ( CDCI3, δ ) : 1.43 (9H, s), 2.50-2.62 ( H, m ) , 2.54 ( 3 x 2/3H, s ) , 2.79 (3 x 1/3H, s), 2.96-3.10 ( 2H, m ) , 3.15-3.25 ( IH, m) , 3.42-3.48 (2H, m, , 3.58-3.62 ( 2H, m ) , 3.65-3.72 (4H, m) , 4.04-4.33 (2 x 2/3H, m >' 4.50-4.58 (IH, m, , 4.62 (2 x 1/3H, α, J=15H Z} / 5.08-5.17 (IH, m) , 6.00 (IH, d, J=8K=), 6.37-7.05 (2H, m) , 7.18-7.27 (8H, m) , 7.40 (1 x 1/3H, d, J=8Hz), 7.46 (1 x 2/3H, d, J=8Hz) Prepa ation 3 Starting Compound (2.34 g) was dissolved m methylene chloride (20 mi) and the solution was ice-cooled. To this solution was added trifluoroacetic acid (10 ml; . The mixture was stirred at this temperature for 10 minutes and at room temperature for 1 hour and was concentrated under reduced pressure. The residue was made alkaline with saturated sodium hydrogencarbonate solution and extracted with chloroform. The organic layer was washed with brine and evaporated under reduced pressure to give Object Compound (1.46 g) as an amorphous solid. Mass (FAB) (m/z) : 466 (M+H) + NMR (CDC1 3 , δ) : 2.23-2.50 (5H, m) , 2.29 (3H, s), 2.63 (3 x 2/3H, S), 2.70-2.85 (IH, m) , 2.37 (3 x 1/3H, s), 2.93-3.13 (2H, m) , 3.39 (IH, t, J=5Hz), 3.46 (IH, t, J=5Hz), 3.52-3.73 (3H, m) , 4.31-4.38 (2 x 2/3H, m) , 4.67 (2 x 1/3H, d, J=15Hz), 5.11-5.20 (IH, m) , 6.94-7.13 (2H, , , 7.18-7.31 (8H, ) , 8.04 (1 x 1/3H, d, J=8Hz), 8.15 • (! " x 2/3K, d, J=8Hz) Preparation 4 A mixture of Starting Compound (0.15 g) and trifluoroacetic acid (0.5 mi) was stirred at room temperature for 1 hour. Trifluoroacetic acid was removed under reduced pressure. The residue was dissolved in 10* hydrochloric acid-methanol (0.2 ml) . Evaporation of solvent gave Object Compound (0.15 g) as powder. NMR (CD3OD, δ) : 2.90 (3 x 2/3H, s), 2.97 (3H, s), 3.05 (3 x 1/3K, s), 3.03-3.16 (4H, ml, 3.42-3.62 (8H, m) , 4.27 (IH, m) , 4.50-4.63 (2H, m) , 5.4c ( H, t, J=7Hz), 7.18-7.36 (5H, m) , 7.83-3.04 ( 2H, m ) , 8.48 (IH, m) , 8.76 (IH, d, J=6Hz ) P ep r ion 5 The following object compounds were obtained according to a similar manner to that of Preparation 3 cr 4. ( 1 ) MASS ( FAB) (m/z) : 453 (M + H ) + NMR ( CDCI3, δ ) : 2.43-2.53 (IH, ) , 2.67 ( 3 x 2/3H, s ) , 2.71-2.83 ( IH, m) , 2.87 (3 x 1/3H, s), 2.93-3.13 ( 2H, m ) , 3.37-3.45 (2H, m) , 3.54-3.73 ( 7H, ) , 4.29-4.43 ( 2 x 2/3H, m) , 4.68 (2 x 1/3H, d, J=15Hz ) , 5.12-5.21 (IH, m) , 6.95-7.15 (2H, m ) , 7.20-7.31 ( 8H, ) , 8.07 (1 x 1/3H, d, J=3Hz ) , 8.15 (1 x 2/3H, d, J=8Hz) ( 2 ) MASS ( FAB) (m/z) : 474 (M + H ) + NMR ( CDCI3, δ ) : 2.42-2.63 (IH, m) , 2.67 ( 3 x 2/3H, s ) , 2.81-2.91 (IH, ) , 2.86 (3 x 1/3H, s ) , 2.95- 3.15 ( 2H, m ) , 3.60-3.65 (1 x 1/3H, m) , 3.70-3.74 ( 1 x 2/3H, m) , 4.22-4.41 (2 x 2/3H, m) , 4.6^ ( 2 x 1/3H, d, J=15H∑), 5.08-5.18 (3H, m) , 6.96-7.29 ( 12H, m ) , 7.30-7.41 (3H, m) , 8.00 (1 x 1/3H, d, J=8Hz ) , 8.08 (1 x 2/3H, d, J=8Hz) ( 3 ) NMR ( CDCI3, δ ) : 2.36 (IH, dd, J=7, 15Hz) , 2.72-2.78 ( 2K, m ) , 2.95 (IH, dd, J=7, 15Hz) , 3.22 (3H, s ) , 3.37 ( 2H, ), 3.50-3.70 (7H, ) , 4.77 ( IH, q, J=7Hz ) , 6.87 ( 2H, m) , 6.93 (2H, m) , 7.20-7.22 ( 4H, m ) , 7.31-7.34 (4H, ) , ~ .94 (IH, d, J=7Hz ) ( 4 ) NMR ( CD3OD, δ) : 2.91-3.00 (2H, m) , 2.92 (3 x 1/ 3H , s ) , 3.03 ( 3 x 2/3K, s), 3.41-3.63 (10H, m j , 4.24 ( IK, m ) , 4.50-4.60 (2H, m) , 5.42 (IH, ) , 7.13-7.2; ( 2H, m ) , 7.29-7.36 (3H, m) , 7.76-7.80 ( ~ - m q ->> 16981 - 379 - (IH, m) , 8.67 (IH, m) (5) NMR (CD 3 OD, δ) : 2.87 (6 x 2/3H, s), 2.97 (3H, s,, 2.98 (6 x 1/3H, s) , 3.05-3.14 (4H, m) , 3.22 (IH, m) , 3.35 (IH, m) , 3.49-3.74 (9H, m) , 4.02 (IH, ) , 4.27 (IH, ) , 4.94 (IH, t, J=7Hz) , 7.27-7.35 !5K, m) (6) NMR (CDC1 3 , δ) : 1.77 (IH, m) , 2.18 (3H, s), 2.13-2.33 (3H, m) , 2.49 (IH, dd, J»7, 15Hz), 2.78 (IH, dd, J-3, 15Hz), 3.00 (2H, d, J=7Hz) , 3.02 (IH, , , 3.33 (IH, ) , 3.43 (2H, ) , 3.52-3.72 (9H, m) , 5.12 (IH, q, J=7Hz), 7.19-7.31 (5H, m) , 8.14 (IH, d, J=7Hz) (7) NMR (DMSO-d 6 , δ) : 1.11 (3H, t, J=7Hz) , 2.81-3.10 (4H, m) , 4.03 (2H, q, J=7Hz) , 4.13 (IH, m) , 4.52 (IH, q, J=7Hz), 5.14 (IH, d, J=l5Hz) , 5.19 (IH, d, J=15Hz) , 7.24-7.32 (5H, m) , 7.37-7.41 (4H, m) , 8.28 (3H, ) , 8.94 (IH, d, J=8Hz) Preparation 6 To a stirred mixture of Starting Compound (2.00 g) , 1-methylpiperazine (0.62 g) and 1-hydroxybenzotriazole (0.84 g) in methylene chloride (30 ml) was added l-(3- dimethyla inopropyl)-3-ethylcarbodiimide hydrochloride (1.20 g) in some portions at 0 β C and the mixture was stirred at room temperature for 4 hours. The reaction mixture was washed with 5% aqueous sodium bicarbonate twice and dried. Evaporation of solvent gave a residue which was purified by silica gel column chromatography. Elution with chloroform - 3% methanol-chloroform afforded Object Compound (2.50 g) as powder. MASS (FAB) (m/z) : 406 (M^+l) NMR (CDC1 3 , δ) : 1.42 (9H, s), 2.30 (3H, s) , 2.35 (4H, m), 2.77 (IH, dd, J=4, 16Hz) , 3.15 (IH, d , J=4, /16981 - 380 - 16Hz), 3.42 (2H, t, J=5Hz) , 3.57 (2H, ) , 4.60 (IH, m) , 5.13 (IH, d, J=15H∑) , 5.22 (IH, c, J=15Hz) , 5.82 (IH, d, J=7Hz), 7.33 (5H, m) Preparation 7 The following object compound was obtained according to a similar manner to that of Preparation 6. NMR (CDC1 3 , δ) : 1.44 (9H, s), 2.78 (IH, dd, J=4, 16Hz), 3.11 (IH, dd, J=4, 16Hz), 3.43 (2K, t, J=7Hz), 3.58 (2H, m) , 3.67 (4H, m) , 3.76 (3H, s), 4.58 (IH, td, J=4, 7Hz) , 5.75 (IH, d, J=7Hz) Preparation 8 A mixture of Starting Compound (0.7 g) and trifluoroacetic acid (1.5 ml) was stirred at room temperature for 1 hour. Evaporation of trifluoroacetic acid gave a residue which was made alkaline with IN aqueous sodium hydroxide and extracted with chloroform. The extract was washed with water and dried. Evaporation of solvent gave Object Compound (0.39 g) . NMR (CDC1 3 , δ) : 1.85 (IH, m) , 2.22 (3H, s,, 2.20-2.37 (3H, ) , 2.80 (IH, dd, J=7, 12Hz) , 2.92 (IH, dd, J=7, 12Hz), 3.09 (IH, ) , 3.34 (IH, m) , 3.60 (2H, m) , 3.94 (IH, t, J=7Hz) , 7.17-7.32 (5H, ) Preparation 9 The following object compounds were obtained according to a similar manner to that of Preparation 3, 4 cr 8. (1) NMR (CD3OD, δ) : 2.95 (3 x 1/3H, s), 2.97 (3 x 2/3K, s), 3.45-3.59 (2H, m) , 4.50 (IH, d, J=15Hz), 4.66 (IH, d, J=15Hz), 5.02 (IH, m) , 7.20-7.37 (5H, m) , 7.75-7.82 (2H, m) , 8.28 (IH, m) , 8.71 (IH, d, J=4Hz) (2) NMR (CDC1 3 , δ) : 2.13 (6 x 2/5H, s), 2.26 (6 x 3/5H, s), 2.12-2.33 (IH, m) , 2.40 (IH, t, =7Hz), 2. (3 x 3/5H, s), 2.77 (IH, m) , 2.92 (3 x 2/5K, s} , 2.94 (IH, m) , 3.02 (1 x 2/5H, m) , 3.23 (1 x 2/5H, __) , 3.46 (2 x 3/5H, m) , 3.87 (1 x 2/5H, t, J=7Hz) , 3.91 (1 x 3/5H, t, J=7Hz), 7.19-7.32 (5H, ) Preparation 10 A solution of Starting Compound (2.6 g) in methanol (50 ml) was hydrogenated over 10 palladium on carbon (0.7 g) at 4 kg/cm -2 for 6 hours. The catalyst was filtered off and washed with methanol. The combined filtrate and washings were evaporated to give Object Compound (2.00 g) as powder. MASS (FAB) (m/z) : 316 (M + +l) NMR (CDCI3, δ) : 1.42 (9H, s), 2.78 (3H, s), 2.82 (IH, m) , 3.02-3.20 (5H, m) , 3.83 (4H, m) , 4.43 (IH, ) , 5.89 (IH, d, J=7Hz) Preparation 11 To a stirred solution of Starting Compound (0.5 g) and triethylamine (0.24 ml) in N,N-dimethylformamide (6 mi) was added dropwise trimethylacetyl chloride (0.21 ml) at -10°c and the mixture was stirred at 0°C for 5 minutes. To this solution was added dropwise a solution of N-methylaniline (0.18 g) in N,N-dimethylformamide (1 ml) at -10°C and the mixture was stirred at room temperature overnight. The reaction mixture was diluted with water and extracted with chloroform. The extract was washed with IN aqueous hydrochloric acid and 5% aqueous sodium bicarbonate, and dried. Evaporation of solvent gave a residue which was chromatographed en silica gel. Eluticn with chloroform gave Object Compound (0.49 g) . MASS (FAB) (m/z) : 389 (M^+l) NMR {CDCI3, δ) : 2.72 (IH, dd, J=7, 12H∑) , 2.90 flH, dd, J=7, 12Hz), 3.20 (3H, s) , 4.57 (IH, ς, J=7Hz) , 5.00 (IH, d, J-15HZ) , 5.06 (IH, d, J=15Hz, , 5.43 (IH, d, J=7H=) , 6.83-6.90 (4H, m) , 7.21 (3H, -, , 7.32-7.33 (8H, m) Preparation 12 The following object compounds were obtained according to a similar manner to that of Preparation 1, 6 cr 11. (1) MASS (FAB) (m/z) : 370 (M ÷ +l) NMR (CDC1 3 , δ) : 1.39 (9H, s) , 2.87 (3 x 1/4H, s) , 2.95 (3 x 3/4H, s) , 3.06 (IK, dd, J=7, 14H∑) , 3.22 (IH, dd, J=7, 14Hz) , 4.40 (IH, d, J=15Hz), 4.71 (IH, d, J=15Hz) , 5.14 (IH, m) , 5.48 (IH, d, J=7Hz), 7.14-7.16 (4H, ) , 7.23-7.32 (3H, m) , 7.55 (IH, ir.) , 8.51 (IH, d, J=4Hz) (2) MASS (FAB) (m/z) : 350 (M + +l) NMR (CDCI3, δ) : 1.40 (9H, s) , 2.16 (6 x 1/3H, s), 2.23 (6 x 2/3K, s), 2.10-2.37 (2H, m) , 2.68 (3 x 2/3H, s), 2.88 (3 x 1/3H, s), 2.95 (2H, d, J=7Hz) , 2.97-3.12 (2 x 1/3H, m) , 3.27-3.50 (2 x 2/3H, m) , 4.80 (IH, m) , 5.32 (1 x 1/3H, d, J=7Hz) , 5.38 (1 x 2/3H, d, J=7Hz) , 7.19-7.28 (5H, m (3) MASS (FAB) (m/z) : 348 (M^+l) NMR (CDCI3, δ) : 1.42 (9H, s), 1.75 (IH, m) , 2.13 (3H, s) , 2.14-2.32 (3H, m) , 2.89-3.02 (3H, ) , 3.26-3.34 (IH, m) , 3.52-3.57 (2H, m) , 4.82 (IH, m) , 5.42 (IH, d, J=7Hz), 7.17-7.30 (5H, m) (4) MASS (FAB) (m/∑) : 406 (M + +l) NMR (CDC1 3 , δ) : 1.43 (9H, s) , 2.47 (IH, dd, J=7, 16Hz) , 2.80 (2H, t, J=7Hz) , 3.18 (IH, dd, J=4, 16Hz) , 3.35-3.70 (10K, m) , 4.51 (IH, m) , 6.03 ;iH, d, J=7H∑ ) , 6 . 82 ( IK, ) , 7 . 18 -7 . 32 ( 5H, m . Preparation 1? To a stirred solution of Starting Compound (3.3 g) ir. 5 methanol (30 ml) was added dropwise IN aqueous sodium hydroxide (12 ml) at 0°C and the mixture was stirred at room temperature for 4 hours. The reaction mixture was diluted with water and extracted with ether. The aqueous solution was acidified with 10% aqueous citric acid and extracted with 10 chloroform 4 times and dried. Evaporation of solvent gave Object Compound (3.55 g) as powder. NMR (CDC1 3 , δ) : 1.44 (9H, s), 2.70 (IH, dd, J=7, 16Hz), 3.20 (IH, dd, J=4, 16Hz), 3.48 (2H, ) , 3.64-3.75 (6H, m) , 4.55 (IH, dt, J=4, 7Hz), 5.82 I 5 (IH, d, J=7Hz) Preparation 14 The following object compounds were obtained according to a similar manner to that of Preparation 1, 6 or 11. 20 (1) MASS (FAB) (m/z) : 567 (M + +l) NMR (CDCI3, δ) : 1.46 (9H, s) , 2.29 (3H, s), 2.33 (4H, m) , 2.55 (IH, dd, J=5, 15Hz) , 2.82 (3 x 1/3H, s), 2.90 (3 x 2/3H, s), 3.07-3.32 (3H, m) , 3.45 (2H, 25 m) f 3.58 (2H, m) , 4.25 (IH, m) , 4.46-4.65 (2K, m) , 4.79 (IH, dd, J=4, 15Hz), 5.40 (IH, m) , 6.03 (IH, m) , 7.06-7.32 (6H, m) , 7.51-7.62 (2H, m) , 8.47 (1H, d, J=5Hz) 30 (2) MASS (FAB) (m/z) : 554 (M + +l) NMR (CDCI3, δ) : 1.46 (9K, s), 2.82 (3 x 1/3K, s 1 , 2.91 (3 x 2/3H, s) , 3.07-3.33 (4H, m) , 3.42 (2H, m) , 3.56-3.67 (6H, m) , 4.17 (IH, d, J=15Hz), 4.28 (IH, d, J-15HZ), 4.51 (IH, m) , 4.79 (IH, m) , 5.40 35 (IH, m) , 6.02 (IH, m) , 7.07-7.31 (6H, m) , 6981 - 384 - 7.51-7.62 (2H, m) , 8.48 (IH, d, J=5Hz) (3) MASS (FAB) (m/z) 539 (M + +l) NMR :CDCI 3 , δ; 1.45 (9H, s), 2.53 (IH, dd, J=5, 15Hz] 2.72 (IH, dd, J=7, 13Hz) , 2.93 (IH, dd, J=7, 13Hz), 3.16 (3H, s) , 3.16 (IH, m) , 3.43 (2H, ) , 3.57 (2H, m) , 3.66 (4H, m) , 4.52 (IK, m) , 4.74 (IH, m) , 5.97 (IH, d, J=7Hz) , 6.72 (2K, m) , 6.97 (2H, m) , 7.21-7.33 (7H, m) (4) MASS (FAB) (m/z) : 534 (M + +l) NMR (CDC1 3 , δ) : 1.45 (9H, S) , 2.13 (6 x 2/5H, s), 2.22 (6 x 3/5H, s), 2.28 (IH, m) , 2.52 (1 x 2/5H, m) , 2.58 (1 x 3/5H, m) , 2.62 (3 x 3/5H, s) , 2.85 (3 x 2/5H, s), 2.94-3.05 (3H, m) , 3.16-3.29 (2H, m) , 3.41-3.51 (3H, m) , 3.59 (2H, m) , 3.67 (4H, m) , 4.51 (IH, ) , 5.02 (IH, m) , 5.98 (IH, d, J=7H∑) , 7.22-7.27 (5H, m) , 7.35 (1 x 2/5H, d, J=7Hz) , 7.41 (1 x 3/5H, d, J=7Hz) (5) MASS (FAB) (m/z) : 532 (M + +l) NMR (CDCI3, δ) : 1.46 (9H, s), 1.70 (IH, m) , 2.17 (3H, s), 2.11-2.19 (2H, m) , 2.28 (IH, m) , 2.55 (IH, dd, J=5, 16Hz), 2.86-3.06 (3H, m) , 3.18-3.28 (2H, m) , 3.43-3.72 (10H, m) , 4.53 (IH, m) , 5.06 (IH, m) , 6.00 (IH, c, J=7Hz), 7.20-7.30 (5H, m) , 7.42 (IH, d, J=7Hz) (6) NMR (CDCI3, δ) : 1.20 (3H, t, J=7Hz), 1.42 (9H, s), 2.70 (IH, dd, J=7, 16H∑) , 3.08 (2H, d, J=7Hz), 3.07 (IH, dd, J=4, 16Hz), 4.13 (2H, q, J=7H∑) , 4.52 (IH, m) , 4.77 (IH, q, J=7Hz) , 5.10 (IH, d, J=15Hz) , 5.15 (IH, d, J=15Hz), 5.62 (IH, d, J=7Hz) , 6.93 (IH, d, J=7Hz), 7.14 (2H, d, J=8Hz), 7.23-7.35 (8H, m) /16981 - 385 - Preparation 15 The following object compound was obtained according to a similar manner to that of Preparation 1, 6 cr 11. MASS (FAB) (m/z) : 360 (M + +l) NMR (CDC1 3 , δ) : 2.88 (IH, dd, J=4, 16H=) , 3.25 (IH, dd, J=4, 16H∑), 3.42-3.45 (2H, m) , 3.58-3.62 (2H, m) , 3.65-3.69 (4K, m) , 3.77 (3H, s), 5.13 (IH, dt, J=4, 7Hz), 6.99 (IH, s) , 7.14 (IH, t, J=8Hz), 7.29 (IH, t, J=8Hz), 7.42 (IH, d, J=8H∑), 7.55 (IH, d, J=8Hz), 7.66 (IH, d, J=8Hz), 9.25 (IH, br s) Preparation 16 The following object compound was obtained according to a similar manner to that of Preparation 13. MASS (FAB) (m/z) : 346 (M + +l) NMR (CDCI3, δ) : 2.83 (IH, dd, J=7, 16Hz), 3.33 (IH, m) , 3.44 (2H, m) , 3.65 (6H, m) , 5.02 (IH, t, J=7HZ), 7.04 (IH, S), 7.12 (IH, t, J=8Hz) , 7.27 (IH, t, J=8Hz), 7.42 (IK, d, J=8Hz) , 7.64 (IH, d, J=8Hz), 7.69 (IH, br s), 9.57 (IH, br s) Preparation 17 The following object compound was obtained according to a similar manner to that of Preparation 10. NMR (CDCI 3 , δ) : 2.59 (IH, dd, J=7, 14Hz), 2.94 (IH, dd, J=7, 14HZ), 3.22 (3H, s) , 3.55 (IH, t, J=7Hz) , 6.82 (2H, m) , 6.90 (2H, m) , 7.20-7.22 (4H, ) , 7.32-7.35 (4K, m) Preparation 1fl The following object compounds were obtained according to a similar manner to that of Preparation 3, 4 or 8. /16981 - 386 - (1) NMR (CD 3 CD, δ) : 2.77-2.92 (4H, m) , 3.3^-3.4 " (3H, mj , 3.52-3.67 (7H, m) , 4.13 (IH, t, J=lHz l r 7.17-7.32 (5K, m) (2) NMR (CD 3 OD, δ) : 3.03 (IH, dd, J=4, 16Hz) , 3.18 (IH, dd, J=7, 16Hz), 3.50 (2H, t, J=7Hz), 3.56(2H, t, J=7Hz), 3.63-3.70 (4H, m) , 3.82 (3H, s), 4.32 (IH, dd, J=4, 7Hz) Preparation 19 The following object compound was obtained according to a similar manner to that of Preparation 1, 6 or 11. MASS (FAB) (m/z) : 449 (M + +l) NMR (CDCI3, δ) : 2.51 (IH, dd, J=7, 16Hz) , 2.79 (2H, t, J=7Hz), 3.31 (IH, dd, J=4, 16Hz), 3.36-3.60 (6H, m) , 3.62-3.68 (4H, m) , 5.03 (IH, dd, J=4, 7Hz) , 6.95 (IH, d, J=2Hz) , 7.03 (IH, t, J=7Hz), 7.09-7.22 (5H, m) , 7.32 (IH, t, J=8Hz), 7.45 (IH, d, J=8Hz), 7.67 (IH, d, J=8Hz), 8.11 (IH, d, J=8Hz) , 9.43 (IK, br s) Preparation ?0 The following object compound was obtained according to a similar manner to that of Preparation 1, 6 or 11. MASS (FAB) (m/z) : 438 (M + +l) NMR (CDCI3, δ) : 2.47-2.65 (2H, m) , 2.62 (3 x 2/3H, s), 2.67 (3 x 1/3H, s), 3.05 (4H, m) , 3.48 (2H, m) , 3.62-3.70 (6K, m) , 4.17 (1 x 1/3H, d, J=15Hz), 4.38 (1 x 2/3H, d, J=15Hz), 4.45 (1 x 1/3H, d, J=15Hz) , 4.62 (1 x 2/3H, d, J=15Hz) , 5.17 (IH, m) , 7.11-7.31 (11H, m) Preparation 21 A mixture of Starting Compound (6.22 g) , 1H-1,2,4- triazole (4.15 g) , and potassium carbonate (3.29 g) m N,N- dimethylformamide (50 mi) was heated to 12C°C fcr 1.5 nours. The mixture was concentrated, thereto added water (150 mi), and extracted three times w th ethyl acetate. The organic layer was washed with water, brine, and dried over magnesium sulfate. The solvent was evaporated, anc the residue was passed through a short column cf silica gel eluting witn a mixture of methylene chloride and ethyl acetate. Evaporation of the solvent gave Object Compound as white crystals. MASS (m/z) : 174 (M+H) ~ NMR (CDC1 3 , δ) : 7.92 (2H, d, J=9Hz) , 8.Co (2H, d, J=9Hz), 8.17 (IH, s), 8.69 (IH, s), 10.07 (IH, s ) Preparation 22 Starting Compound (5.19 g) was dissolved in 30% methylamme in methanol (30 ml) , and heated to 60°C for 1 hour. Evaporation of the solvent gave a solid, and the solid was suspended m ethanol (150 ml), then cooled with ice. To this suspension was added sodium borohydride (1.13 g) m some portions and the mixture was stirred at room temperature fcr 1 hour. The mixture was concentrated, thereto added some water, and extracted five times with dichlorometnane. The organic layer was washed with brine, and dried over potassium carbonate. Evaporation of the solvent, followed by distillation (bp 136-137°C/0.45 mmHg) afforded Object Compound as colorless prisms (4.00 g) . mp : 55-56 β C MASS (m/z) : 189 (M+H) + NMR (CDCI3, δ) : 2.46 (3H, s), 3.80 (2H, s), 7.46 (2H, d, J=8Hz), 7.62 (2K, d, J=8Hz) , 8.10 !1H, s), 3.52 (IK, s) Preparation 7 ~ /16981 - 388 - Starting Compound (729 mg) was dissolved m 30 methylamine in methanol (3 ml), and heated to 60°C for 1.5 hours. Evaporation of the solvent gave an oil, and the residue was redissolved in ethanol (5 ml), then cccied w th ice. To this solution was added sodium borohycride (204 g) in some portions and the mixture was stirred at room temperature for 1 hour. After the mixture was concentratec, added aqueous sodium hydroxide, and extracted tnree times with chloroform. The organic layer was dried over magnesium sulfate and evaporated. The product was purified by column chromatography (silica gel) eluting with a mixture of chloroform and methanol to give Object Compound as a pale- yellow oil (316 mg) . MASS (m/z) : 153 (M+H) + NMR (CDC1 3 , δ) : 2.45 (3H, s), 3.69 (2H, s), 3.92 (3H, S), 6.72 (IH, d, J=9Hz), 7.58 (IH, dd, J=9, 2Hz) , 8.08 (IH, d, J=2Hz) Preparation 74 Object Compound was obtained according to a similar manner to that of Preparation 23. MASS (m/z) : 157 (M+H) + NMR (CDCI3, δ) : 2.46 (3H, s), 3.77 (2H, s;, 7.71 (IK, s), 8.42 (IH, s), 8.48 (IH, s) Preparation ? ~ A mixture of Starting Compound (3.0 g) and 30% methylamme-methanol (30 ml) was stirred at 60°C for 2 hours. Evaporation of methanol gave a residue, which was redisscivec m methanol (30 ml) . To this mixture was added sodium borohydride (0.5 g) in some portions at 0 β C. The mixture was stirred at room temperature for 30 minutes. The reaction mixture was made acidic with IN hydrochloric acid and extracted with ether. The aqueous solution was made alkaline with IN aqueous sodium hydroxide and extracted with 6981 - 389 - chloroform. The extract was washed with water and dried. Evaporation of solvent gave Object Compound (2.4 g) . MASS (m/z) : 190 (M + +l) NMR (CDC1 3 , δ) : 2.45 (3H, s), 3.81 (2H, s) , 7.43 (2H, d, J=8Hz), 7.57 (2H, d, J=8Hz) Preparation 26 To an ice-cooled solution of di-tert-butyl dicarbonate (4.50 g) in dichloromethane (10 ml) was added Starting Compound (2.51 g) , and the mixture was stirred at room temperature for 1 hour. The mixture was diluted with dichloromethane, washed with water, brine, and dried over magnesium sulfate. Evaporation of the solvent afforded Object Compound (4.51 g) as a pale-yellow crystal. mp : 55-57°C MASS (m/z) : 226 (M+H) + NMR (CDCI3, δ) : 1.45 (9H, s) , 4.28 (2H, br d) , 4.84 (IH, br s), 6.93-7.05 (2H, m) , 7.20-7.30 (2H, ) Preparation 27 To an ice-cooled suspension of Starting Compound (5.05 g) in dichloromethane (40 ml) was added triethylamine (5 ml) . Di-tert-butyl dicarbonate (6.78 g) in dichloromethane (20 ml) was added thereto dropwise, and the mixture was stirred at room temperature for 8 hours. The mixture was washed twice with 10% citric acid, once with aqueous sodium hydrogencarbonate, once with brine, and dried over magnesium sulfate. Evaporation of the solvent gave Object Compound (7.89 g) as a white solid. MASS (m/z) : 266 (M+H) + NMR (CDC1 3 , δ) : 1.45 (9H, s) , 3.89 (3H, s) , 4.35 (2H, br s), 4.95 (IH, br s) , 7.33 (2H, d, J=8Hz) , 7.98 (2H, d, J=8Hz) Preparation ?B To an ice-cooled suspension of sodium hydπαe mg) m anhydrous tetrahydrofuran (10 ml) was added αropw se Starting Compound (4.51 g) in anhydrous tetranydrofurar. (10 ml) for 5 minutes. The mixture was heated to 60°C fcr 2 hours. During the heating, the mixture turneα into light yellow. After the mixture was allowed to cool to room temperature, lodomethane (4.56 g) was added thereto dropwise and heated to 30 β C for 2 hours. The reaction mixture was allowed to cool to room temperature. Water was added thereto, and the mixture was extracted three times with ether. The organic layer was washed with brine and cried over magnesium sulfate. After the solvent was evaporatec, the residue was subjected to column chromatography (silica gel, hexane - ethyl acetate) to give Object Compound (3.09 g) as a colorless oil. MASS (m/z) : 240 (M+H) + NMR (CDC1 3 , δ) : 1.48 (9H, s), 2.80 (3H, s), 4.33 (2H, s), 6.92-7.05 (2H, m) , 7.10-7.27 (2H, m) Preparation 29 To an ice-cooled suspension of sodium hydride (0.86 g) in anhydrous tetrahydrofuran (30 ml) was added dropwise Starting Compound (7.89 g) m anhydrous tetrahydrofuran (15 ml) for 10 minutes. The mixture was heated to 40°C for 2 hours. During the heating, the mixture turned into lignt yellow. After the mixture was allowed to cool to room temperature, lodomethane (5.02 g) was added dropwise and heated to 40 β C for 2 hours. The reaction mixture was allowed to cool to room temperature. Water was added to tne mixture, and the mixture was extracted three times with ether. The organic layer was washed with brine and dried over magnesium sulfate. After the solvent was evaporated, the residue was subjected to column chromatography (silica gel, nexane - ethyl acetate) to give Object Compound (5.21 g) as a colorless oil. /16981 - 391 - MASS (m/z) : 280 (M+H) + NMR (CDC1 3 , δ) : 1.46 (9K, br s), 2.80 (1/2 x 2H, br s), 2.88 (1/2 x 2H, br s), 3.90 (3H, s), 4.47 (2H, br s), 7.28 (2K, d, J=8Hz) , 8.00 (2K, d, J=8Hz) Preparation 30 10% Hydrogen chloride in methanol (50 ml) was added tc Starting Compound (7.56 g) and heated to 60°C for 3 hours. The mixture was allowed to cool to room temperature. The white precipitate formed was collected by filtration and washed with ether. The product was recrystallized from ethanol-water (10:1) to give Object Compound (6.15 g) . NMR (D 2 0, δ) : 3.95 (3H, s), 4.28 (2H, s), 7.59 (2H, d, J=8Hz), 8.11 (2H, d, J=8Hz) Preparation 31 Starting Compound (12.09 g) , 37% formaldehyde solution (16.5 ml), and formic acid (9.1 ml) were mixed with ice- cooling and heated to 80 β C for 20 hours. After the mixture was allowed to cool to room temperature, 6N hydrochloric acid (20 ml) was added and washed with ether. The aqueous layer was adjusted to pH 6-7 by adding 28% aqueous ammonia and then concentrated. Acetone was added to the solution, and the white precipitate formed was filtered, washed with acetone and ether, and evaporated in vacuo to give Object Compound (4.34 g) . p : >300°C (dec.) NMR (D 2 0) : 2.89 (6H, S) , 4.38 (2H, s), 7.57 (2H, d, J=8Hz), 7.96 (2H, d, J=8Hz) Preparation 32 A mixture of Starting Compound (3.59 g) , methyiamine hydrochloride (1.36 g) , and l-ethyl-3- (3- dimethylaminopropyl)carbodiimide hydrochloride (4.22 g) in dichloromethane-N,N-dimethyiformamide (1:1, 40 mi) was 16981 - 392 - stirred at room temperature for 12 hours. The reaction mixture was diluted with ethyl acetate, washed w th aqueous sodium hydrogencarbonate, with brine, and dried over magnesium sulfate. After the solvent was evaporated, the residue was subjected to column chromatography (silica gel chloroform-methanol) to give Object Compound as a colorless crystal (185 mg) . mp : 51-52°C MASS (m/z) : 193 (M+H) + NMR (CDC1 3 , δ) : 2.50 (6H, s), 3.01 (3H, d, J=6Hz) , 3.48 (2H, s), 6.16 (IH, br s), 7.38 (2H, d, J=8Hz), 7.72 (2H, d, J=8Hz) Preparation 33 To a suspension of lithium aluminum hydride (56 mg) in anhydrous tetrahydrofuran (2 ml) was added Starting Compound (180 mg) at 0"C. The mixture was heated to reflux for 1.5 hours. The mixture was allowed to cool to room temperature and diluted with ether. To this mixture was added water (56 g) , 15% aqueous sodium hydroxide (56 mg) , and water (110 mg) . Filtration followed by evaporation of the solvent afforded Object Compound (125 mg) as a colorless oil. MASS (m/z) : 179 (M+H) + NMR (CDCI3, δ) : 2.23 (6H, s) , 2.45 (3H, s), 3.40 (2H, s), 3.73 (2H, s), 7.27 (4K, s) Preparation 34 The following object compound was obtained according tc a similar manner to that of Preparation 6. MASS (FAB) (m/z) : 478 (M+H) ÷ NMR (CDCI3, δ) : 1.28 (3H, t, J=8Hz), 1.39 (9H, s), 2.45-2.61 (4H, m) , 2.76 (IH, dd, J=15, 5Hz), 3.13 (IH, dd, J=15, 5Hz), 3.20 (2H, s), 3.43-3.50 (2H, m) , 3.60-3.64 (2H, m) , 4.08-4.22 (2H, m) , 4.56-4.52 (IH, m) , 5.17 (2H, q, J=8Hz) , 5.80 (IH, d, J=8Hz) , /16981 - 393 - 7 .33 ( 5H, br s ) Preparation , ~ ~ The following object compound was obtained according to a similar manner to that of Preparation 10. MASS (FAB) (m/z) : 387 (M+H) + NMR (CDC1 3 , δ) : 1.26 (3H, t, J=8H∑) , 1.39 (9H, s) , 2.50-3.90 (5H, ) , 3.04-3.12 (IK, m) , 3.23 (2H, s), 3.52-3.62 (3H, m) , 3.68-3.80 (IH, m) , 4.18 (2H, q, J=8Hz), 4.38-4.50 (IH, m) , 5.94 (IH, br s) Pre p arat i on " ** Starting Compound (573 mg) was dissolved in a mixture of hydrochloric acid (1 ml) and methanol (5 ml), and stirred at 50 β C for 1 hour. The reaction mixture was evaporated and the remaining solid was dried in vacuo. To this solid was added dichloromethane (5 ml), Boc-Phe-OH (531 mg) , 1- hydroxybenzotriazole (284 mg) and l-ethyl-3-(3- dimethyla inopropyl)carbodiimide hydrochloride (416 mg) , and the mixture was stirred at room temperature for 12 hours. The mixture was diluted with ethyl acetate, washed with aqueous sodium hydrogencarbonate, washed with brine, and dried over magnesium sulfate. Evaporation of the solvent followed by subjecting to column chromatography (silica gel, chloroform-methanol) afforded Object Compound (820 mg) as a colorless oil. MASS (m/z) : 427 (M+K) + NMR (CDCI3, δ) : 1.40 (9H, s) , 2.63 (2/3 x 3H, s), 2.80 (1/3 x 3H, s), 3.0-3.1 (2H, m) , 3.70 (1/3 x 3H, s), 3.90 (2/3 x 3H, s) , 4.19 (1/3 x IH, d, J=17Hz), 4.38 (1/3 x IH, d, J=17Hz) , 4.53 (2/3 x 2H, ABq, A-0.11, J=15Hz) , 4.8-4.9 (IH, m) , 5.30 (1/3 x IH, br d, J=8Hz), 5.38 (2/3 x IH, br d, J=8Hz), 6.9-7.3 (7H, m) , 7.9-8.0 (2H, m) Preparation 37 The following object compound was obtained according to a similar manner to that of Preparation 36. MASS (m/z) : 387 (M+H) + NMR (CDC1 3 , δ) : 1.42 (9H, s), 2.61 (3/4 x 3H, s), 2.79 (1/4 x 3H, z) , 2.93-3.03 (2H, m) , 4.05 (1/4 x IH, d, J=17Hz) , 4.32 (1/4 x IH, d, J=17Hz), 4.45 (3/4 x 2H, ABq, Δ=0.12, J=15Hz) , 4.78-5.00 (IH, m) , 5.30-5.45 (IH, m) , 6.80-7.30 (9H, m) Preparation 38 Starting Compound (4.09 g) was dissolved in tetrahydrofuran (45 ml) and cooled to -15 β C. N-Methyl- morpholine (1.1 ml) and isobutylchloroformate (1.38 g) were added successively to the solution, and stirred at the temperature for 3 minutes. N-Methyl benzylamine (1.22 g) in tetrahydrofuran (5 ml) was added to the mixture, and the whole was stirred at 0"C for 30 minutes. The reaction mixture was diluted with chloroform, washed with aqueous sodium hydrogencarbonate, washed with brine, and dried over magnesium sulfate. Evaporation of the solvent gave Object Compound (5.13 g) as white powder. NMR (CDCI3, δ) : 1.40 (9H, s) , 2.42 (3H, s) , 2.72-3.04 (2H, ) , 2.83 (1/3 x 3H, s) , 2.88 (2/3 x 3H, s), 4.30-4.65 (2H, m) , 4.85-5.04 (IH, m) , 5.32-5.50 (IH, m) , 7.00-7.95 (11H, m) Preparation 39 The following object compounds were obtained according to a similar manner to that of Preparation 1, 6, 11 or 38. (1) NMR (CDCI3, δ) : 1.40 (9H, s), 2.80 (3/4 x 3K, s), 2.85 (1/4 x 3H, s), 4.33 (1/4 x IH, d, J=15Hz), 4.55 (1/4 x IH, d, J=15Hz), 4.60 (3/4 x 2H, ABq, J-14HZ), 5.59 (3/4 x IH, d, J=8Hz), 5.62 (1/4 x IH, d, J=8Hz) , 6.05 (IH, d, J=8Hz) , 6.9-7.4 (10H, m) (2) MASS (m/z) : 389 (M+H) + NMR (CDC1 3 , δ) : 2.93-3.22 (2H, m) , 4.32 (2H, d, J=16Hz), 4.33-4.47 (IH, m) , 5.06 (2H, s) , 5.33 (IH, br s), 5.92 (IH, br s) , 6.98-7.41 (15K, m) (3) MASS (m/z) : 279 (M+H) + NMR (CDCI3, δ) : 1.43 (2/5 x 9H, s) , 1.48 (3/5 x 9H, s), 2.88 (3/5 x 3H, s), 2.99 (2/5 x 3K, s) , 3.95- 4.08 (2H, ), 4.46 (2/5 x 2H, s), 4.61 (3/5 x 2H, s), 5.50-5.62 (IH, br s) , 7.10-7.42 (5H, m) (4) MASS (m/z) : 399 (M+H) + NMR (CDCI3, δ) : 1.42 (9H, S) , 2.60 (2/3 x 3H, s) , 2.78 (1/3 x 3H, s) , 2.95-3.02 (2H, m) , 3.76 (1/3 x 3H, s), 3.79 (2/3 x 3H, s) , 3.98 (1/3 x IH, d, J=17Hz), 4.30 (1/3 x IH, d, J=17Hz) , 4.42 (2/3 x 2H, ABq, Δ=0.13, J=15Hz) , 4.8-5.0 (IH, m) , 5.33 (1/3 x IH, br d, J=9Hz) , 5.40 (2/3 x IH, br d, J=9Hz), 6.78 (1/3 x 2H, d, J=9Hz) , 6.80 (2/3 x 2H, d, J=9Hz), 6.88 (1/3 x 2H, d, J=9Hz) , 7.03 (2/3 x 2H, d, J=9Hz), 7.1-7.3 (5H, m) (5) MASS (m/z) : 475 (M+H) "1" NMR (CDCI3, δ) : 1.40 (1/4 x 9H, s), 1.43 (3/4 x 9H, s), 2.60 (3/4 x 3H, s) , 2.81 (1/4 x 3H, s) , 2.88- 2.98 (2H, m) , 4.22 (1/4 x 2H, ABq, J=17Hz) , 4.48 (3/4 x 2H, ABq, A-0.13, J=15Hz) , 4.75-4.88 (IH, m) , 5.01 (3/4 x 2H, s) , 5.05 (1/4 x 2H, s) , 5.26-5.44 (IH, m) , 6.77-7.45 (14H, m) (6) MASS (m/z) : 383 (M+H) + NMR (CDCI3, δ) : 1.42 (9H, s) , 2.45-2.98 (4H, m) , 2.60 /16981 - 396 - (3/5 x 3H, s), 2.80 (2/5 x 3H, s) , 3.10-3.63 (2K, m) , 4.68-4.85 (IH, m) , 5.25 (2/5 x IH, br d, J=9Hz), 5.35 (3/5 x IH, br d, J=9Hz) , 7.02-7.32 (10H, m) (7) MASS (m/z) : 419 (M+HA NMR (CDC1 3 , δ) : 1.41 (9H, S) , 2.66 (3/4 x 3H, s) , 2.87 (1/4 x 3H, s) , 3.02 (2H, m) , 4.24 (1/4 x IH, d, J=17Hz), 4.53 (1/4 x IH, d, J=17Hz) , 4.67 (3/4 x 2H, ABq, J=15Hz), 4.9-5.0 (IK, m) , 5.40 (1/4 x IH, d, J=9Hz), 5.46 (3/4 x IK, d, J=9Hz) , 7.0-7.3 (6H, m) , 7.4-7.9 (6H, ) (8) MASS (m/z) : 419 (M+H) + NMR (CDCI3, δ) : 1.38 (1/4 x 9H, s), 1.43 (3/4 x 9H, s), 2.60 (3/4 x 3H, s), 2.90 (1/4 x 3H, s) , 2.93- 3.08 (2H, m) , 4.63 (1/4 x 2H, ABq, J=17Hz) , 4.80-4.98 (IH, m) , 5.00 (3/4 x 2H, ABq, Δ=0.16, J=15Hz), 5.32-5.50 (IH, m) , 6.90-8.10 (12H, m) (9) MASS (m/z) : 411 (M + ) NMR (CDCI3, δ) : 1.40 (9H, s) , 2.59 (2/3 x 3H, s), 2.80 (1/3 x 3H, s), 2.93 (6H, s) , 2.98 (2H, at), 3.95 (1/3 x IH, d, J=17Hz) , 4.30 (1/3 x IH, d, J=17Hz) , 4.39 (2/3 x 2H, ABq, , 4.7- 4.8 (2/3 x IH, m) , 4.9-5.0 (1/3 x IH, m) , 5.38 (1/3 x IH, d, J=9Hz), 5.43 (2/3 x IH, d, J=9Hz) , 6.63 (2H, d, J=8Hz) , 6.8-7.3 (7H, m) (10) MASS (m/z) : 426 (M+H) + NMR (CDCI3, δ) : 1.39 (1/3 x 9H, s), 1.42 (2/3 x 9H, s), 2.20 (1/3 x 6H, s), 2.22 (2/3 x 6H, s), 2.61 (2/3 x 3H, s), 2.82 (1/3 x 3H, s), 2.92-3.04 (2H, m) , 3.37 (1/3 x 2H, s), 3.39 (2/3 x 2H, s), 4.08 (1/3 x IH, d, J=17Hz) , 4.34 (1/3 x IH, d, J=17Hz) , 6981 - 397 - 4.48 (2/3 x 2H, ABq, , 4.80-4.95 (IH, m) , 5.30-5.45 (IH, m) , 6.88-7.30 (9H, m) (11) MASS (m/z) : 381 (M+H) + NMR (CDC1 3 , δ) : 1.42 (9H, s), 2.25-2.42 (IH, m) , 2.65-2.80 (IH, m) , 2.90-3.20 (2H, m) , 3.48-3.90 (2H, m) , 3.96 (1/3 x IH, d, J=17Hz) , 4.48 (1/3 x IH, d, J=17Hz), 4.65 (2/3 x 2H, ABq, Δ=0.19, J=17Hz), 4.85-5.00 (IH, ) , 5.38-5.52 (IH, m) , 6.80-7.22 (9H, m) (12) mp : 100-101 β C MASS (m/z) : 403 (M+H) + NMR ( CDCI3, δ) : 1 - 43 (9H ' s) ' 2 ' 62 (3 4 x 3H ' s) ' 2.78 (1/4 x 3H, s) , 2.90-3.10 (2H, m) , 4.19 (1/4 x 2H, ABq, Δ=0.21, J=17Hz) , 4.45 (3/4 x 2H, ABq, Δ=0.12, J=15Hz), 4.78-4.92 (IH, m) , 5.32 (1/4 x IH, d, J=9Hz), 5.38 (3/4 x IH, d, J=9Hz) , 6.80-7.05 (2H, m), 7.09-7.32 (7H, m) (13) MASS (m/z) : 447, 449 (M+H) + NMR (CDCI3, δ) : 1.42 (9H, s), 2.62 (3/4 x 3H, s) , 2.79 (1/4 x 3H, s), 2.90-3.08 (2H, m) , 4.17 (1/4 x 2H, ABq, J=17Hz) , 4.42 (3/4 x 2H, ABq, Δ=0.12, J=15Hz), 4.78-4.93 (IH, m) , 5.25-5.42 (IH, m) , 6.73-7.00 (2H, m) , 7.08-7.45 (7H, m) (14) MASS (m/z) : 400 (M+H) + NMR (CDCI3, δ) : 1.40 (9H, s) , 2.59 (3/4 x 3H, s), 2.75 (1/4 x 3H, s) , 2.90-3.08 (2H, m) , 3.90 (1/4 x 3H, s), 3.93 (3/4 x 3H, s) , 4.34 (1/4 x 2H, ABq, Δ=0.10, J=17Hz), 4.40 (3/4 x 2H, ABq, J=15Hz), 4.74-5.05 (IH, m) , 5.30-5.45 (IH, m) , 6.55-6.70 (IH, m) , 7.03-7.38 (6H, ) , 7.80-8.00 (IH, m) ( 15 ) NMR ( CDC1 3 , δ ) : 0.95 (3/5 x 3H, t, J=7.5Hz ) , 1.02 ( 2/5 x 3H, t, J=7.5Hz), 1.40 (2/5 x 9H, s ) , 1 42 ( 3/5 x 9H, s ) , 2.85-3.55 (4H, m) , 4.19 ( 2/5 x 2H ABq, Δ = 0 .18, J=17Hz ) , 4.33 (3/5 x l H , d , J « i5Hz, ,' 4-73 ( 3/5 x IH, d, J=15Hz) , 4.75-4.92 ( IH, m ) , 5.25-5.42 ( IH, m) , 6.93-7.35 (10H, m ) ( 16 ) MASS (m/z) . 404 (M+H ) ÷ NMR ( CDC1 3 , δ ) : 1.42 (9H, s) , 2.63 (5/6 x 3H, s ) , 2'76 (1/β X 3H ' s) ' 2 -88-3.09 ( 2H, m), 4.04 ύ/6 x IH, d, J-17H Z) , 4.30 ( 1/6 x IH, d, J-l7Hz ) , 4.44 ( 5/6 x 2H, ABq, Δ =0.08, J=15Hz) , 4.76-4.92 ( IH, m ) 5-22-5.38 ( IH, m ) , 7.03-7.40 (7H, m) , 8.05 ( 1/6 x ' IH, d, J=2Hz ) , 8.18 (5/6 x IH, d, J=2Hz ) ( 17 ) MASS (m/z) : 384 (M+H ) + NMR ( CDC1 3 , δ ) : 1.42 (9H, s) , 2.51 ( 1/5 x 3H, s ) , 2.53 ( 4/5 x 3H, s ) , 2.60 (4/5 x 3H, s), 2.78 ' ( 1/5 x 3H, s ) , 2.90-3.06 (2H, m) , 3.98 (1/5 x 1H , d/ J=17Hz ) , 4.32 ( 1/5 x IH, d, J=17Hz) , 4.44 ( 4/5 x 2H, ABq, Δ =0.06, J=15Hz) , 4.75-4.98 (IH, m ) , 5.25- 5-42 ( IH, a ) , 6.98-7.33 (7H, m) , 8.18 ( 1/5 x m, d/ J=2Hz ) , 3.31 (4/5 x IH, d, J=2Hz ) ( 18 ) MASS (m/z) : 436 ( M+H ) + MR ( CDCI3, δ ) : 1.42 (9H, s) , 2.67 (3/4 x 3H. s ) , 2.82 ( 1/4 x 3H, s) , 2.95-3.07 (2H, m) , 4.26 ύ/4 x 2H, ABq, Δ =0.22, J=17Hz) , 4.53 (3/4 x 2K, s) , 4.82- 4-95 ( IH, m ) , 5.28-5.42 (IH, m) , 7.00-7.32 ( 7H, m ) , 7.50-7.62 ( 2H, m) , 8.10 (IH, s), 8.52 ( IH, s ) ( 19 ) MASS (m/z) : 404 (M+H) + R ( CDCI3, ) : 1.42 (9H, s) . 2.61 (5/6 x 3H, s ) , 2-78 ( 1/6 x 3H, s ) , 2.92-3.08 (2H, m) , 3.96 ( 1/6 x IH, d, J=17Hz ) , 4.38 (1/6 x IH, d, J=17Hz ) , 981 - 399 - 4.47 (5/6 x 2H, ABq, Δ=0.07, J=15Hz) , 4.76-4.92 (IH, m), 5.25-5.40 (IH, m) , 7.10-7.35 {5H, m) , 7.50 (IH, s), 8.12 (1/6 x IH, s) , 8.28 (5/6 x IH, s), 8.48 (IH, s) (20) MASS (m/z) : 370 (M+H) + NMR (CDC1 3 , δ) : 1.38 (1/3 x 9H, s), 1.42 (2/3 x 9H, s), 2.77 (2/3 x 3H, s) , 2.89 (1/3 x 3H, s) , 2.90- 3.10 (2H, m) , 4.38 (1/3 x 2H, ABq, Δ=0.10, J=17Hz) , 4.61 (2/3 x 2H, s) , 4.81-4.97 (IH, m) , 5.25-5.44 (IH, m) , 6.87-7.67 (8H, m) , 8.43-8.57 (IH, m) (21) MASS (m/z) : 370 (M+H) + NMR (CDCI3, δ) : 1.39 (1/4 X 9H, s) , 1.42 (3/4 x 9H, s), 2.69 (3/4 x 3H, s) , 2.82 (1/4 x 3H, s) , 2.90- 3.12 (2H, m) , 4.28 (1/4 x 2H, s) , 4.48 (3/4 x 2H, ABq, Δ=0.06, J=15Hz), 4.68-4.98 (IH, m) , 5.20-5.40 (IH, m) , 6.73-7.35 (7H, m) , 8.40-8.52 (2H, m) (22) MASS (m/z) : 370 (M+H) + NMR (CDC1 3 , δ) : 1.40 (1/5 x 9H, s) , 1.42 (4/5 x 9H, s), 2.63 (4/5 x 3H, s), 2.79 (1/5 x 3H, s) , 2.92- 3.06 (2H, m) , 4.08 (1/5 x IH, d, J=17Hz) , 4.35 (1/5 x IH, d, J=17Hz), 4.49 (4/5 x 2H, ABq, Δ=0.09, J=15Hz), 4.79-4.98 (IH, m) , 5.28-5.42 (IH, m) , 7.10-7.35 (7H, ) , 8.28 (1/5 x IH, s), 8.42 (4/5 x IK, s), 8.50-8.55 (IH, m) (23) MASS (m/z) : 399 (M + +l) NMR (CDCI3, δ) : 1.43 (9H, s) , 2.59 (3H x 2/3, s) , 2.78 (3H x 1/3, s) , 2.98 (2H, d, J=7Hz) , 3.78 (3H, s), 3.99 (IH x 1/3, d, J=15Hz) , 4.31 (IH x 1/3, d, J=15Hz), 4.35 (IH x 2/3, d, J=15Hz) , 4.48 (IH x 2/3, d, J=15Hz), 4.83 (IH, m) , 5.40 (IH, ) , 6.80- 7.04 (4H, m) , 7.16-7.25 (5K, m) ( 24 ) MASS (ESI) (m/z) : 383 (M+H) + NMR ( CDC1 3 , lδ ) : 1.42 (9H, s), 2.32 ( 3H, s ) , 2.59 ( 3 x 2/3H, s ) , 2.83 (3 x 1/3H, s), 2.90-3.06 ( 2H, m ) , 4.02-4.53 (2H, m) , 4.82-4.96 5.40-5.50 ( IH, m ) , 6.88 (2 x 1/3H, d, ( 2 x 2/3H, d, J=8Hz ) , 7.05-7.10 (2H, m ) , 7.13-7 30 (5H, m) ( 25 ) MASS (m/z) : 309 (M + +l) NMR ( CDCI3, δ ) : 1.38 (9H x 1/3, s), 1.45 ( 9H x 2/3, s ) , 2.93 ( 3H x 1/3, s), 3.05 (3H x 2/3, s ) , 3.26 ( IH, x 2/3, m ) , 3.44 ( IH x 1/3, m) , 3.67-3.88 ( 2H, m>, 4.60-4.71 ( 3H, ) , 5.70 (IH, m) , 7.17-7.38 ( 5H, m) ( 26 ) MASS (m/z) : 335 (M + +l) NMR ( CDCI3, ) : 0.84 (6H x 2/7, t/ J=7Hz) , 0 . 9 (3H x 5/7, d, J=7Hz ) , 1.00 (3H x 5/7, d , J=7Hz ) , 1.45 OH, s ) , 1.34-1.76 ( 3H, m) , 2.92 (3H x 2/7, S) , 2.97 ( 3H x 5/7, s) , 4.48 (IH x 5/7, d, J=15Hz ) , 4.67 ( IH x 5/7, d, J=15Hz) , 4.65-4.72 ( 2H x 2/7, m ) , 5.19 ( IH x 2/7, d, J=7Hz) , 5.28 (IH x 5/7, _ '_, J=7Hz), 7.20-7.34 (5H, ) ( 27 ) MASS (m/z) : 437 (M + +l ) NMR ( CDC1 3 , δ ) : 1.40 (9H x 1/3, s) , 1.45 ( 9H x 2/3, s ) , 2.67 ( 3H x 2/3, s) , 2.83 (3H x 1/3, s ) , 3.02 ( 2H, d, J=8Hz ) , 4.22 (IH x 1/3, d, J=15Hz ) , 4.37 ( IH x 1/3, d, J=15Hz ) , 4.50 (IH x 2/3, d, J=15Hz ) , 4.58 ( IH x 2/3, d, J=15Hz) , 4.90 (IH, m ) , 5.36 ( IH, m ) , 7.02-7.28 (7H, ) , 7.53 (2H, d, J=8Hz ) ( 28 ) MASS (m/z) : 369 (M + +l) NMR ( CDCI3, δ ) : 1.42 (9H, s) , 2.62 (3H x 2/3, s ) , 2 " 82 (3H x 1/ , s ) , 3.00 ( 2H, d, J=7Hz), 4.1l' ( i H x 6981 - 401 - 1/3 , d, J=15Hz) , 4 .36 ( IH x 1/3, d, J=15Hz ) , 4 . 43 ( IH x 2/3 , d, J=15Hz ) , 4 . 54 ( IH x 2/3 , d, J=15Hz ) , 4 . 86 ( IH, m) , 5 . 41 ( IH, m) , 6. 96-7 .28 ( 10H, m) Preparation 40 Starting Compound (801 mg) was dissolved in dichloromethane (10 ml) . Boron tribromide solution in dichloromethane (0.43 ml) was added to the above solution at room temperature, and the whole was stirred at the same temperature for 12 hours. Water (5 ml) was added to the mixture and stirred for 30 minutes. The mixture was neutralized by adding aqueous sodium hydrogencarbonate and then extracted three times with chloroform. The organic layer was dried over potassium carbonate. Evaporation of the solvent gave Object Compound (406 mg) as an oil. MASS (m/z) : 285 (M+H) + NMR (CDCI3, δ) : 2.74 (2/3 x 3H, S) , 2.75-2.85 (IH, m) , 2.90 (1/3 x 3H, s), 3.00-3.10 (IH, m) , 3.92 (1/3 x IH, d, J=17Hz), 3.95-4.05 (IH, m) , 4.10 (2/3 x IH, d, J=15Hz), 4.34 (1/3 x IH, d, J=17H∑) , 4.82 (2/3 x IH, d, J=15Hz), 6.60-7.35 (9H, m) Preparation 41 Starting Compound (2.56 g) was dissolved in dichloromethane (5 ml) and cooled to 0°C. Trifluoroacetic acid (5 ml) was added to the solution and the mixture was stirred at 0 β C for 3 hours. Aqueous sodium hydroxide was added to the solution with ice-cooling to make basic, and the solution was extracted three times with chloroform. The organic layer was washed with brine and dried over magnesium sulfate. Evaporation of the solvent gave Object Compound (2.02 g) as an oil. MASS (m/z) : 413 (M+H) + NMR (CDCI3, δ) : 2.43 (3H, s) , 2.61-2.75 (IH, m) , 2.80-2.95 (4H, m) , 3.98-4.18 (IH, m) , 4.33 (1/3 x 981 - 402 - IH, d, J=17HZ) , 4 .57 (2/3 x 2K, ABq, . 16, J=15Hz) , 4 . 61 ( 1/3 x IH, d, J=17Hz) , 7 . 00-7 . 43 (11H, m) , 7. 75-7 . 97 (3H, ) Preparation 42 The following object compounds were obtained according to a similar manner to that of Preparation 3, 4 or 8. (1) MASS (m/z) : 255 (M+H) ÷ NMR (CDCI3, δ) : 2.75 (2/3 x 3H, s) , 2.95 (1/3 x 3H, s), 4.22 (1/3 x IH, d, J=17Hz) , 4.58 (1/3 x IH, d, J=15Hz) , 4.74 (1/3 x IH, s), 4.77 (2/3 x IH, s), 6.92-7.45 (10H, m) (2) NMR (CDCI3, δ) : 2.70 (3/5 x 3H, s) , 2.72-2.85 (IH, m), 2.89 (2/5 x 3H, s), 2.93 (6H, s), 2.95-3.05 (IH, m) , 3.90-4.00 (IH, ) , 4.08 (2/5 x IH, d, J=17Hz), 4.35 (2/5 x IH, d, J=17Hz) , 4.48 (3/5 x 2H, ABq, , 6.62-7.33 (9H, m) (3) MASS (m/z) : 326 (M+H) + NMR (CDCI3, δ) : 2.23 (6H, s) , 2.71 (3/5 x 3H, s) , 2.72-2.85 (IH, m) , 2.91 (2/5 x 3H, s) , 2.92-3.05 (IH, ), 3.41 (2H, s) , 3.88 (2/5 x IH, t, J=7Hz) , 3.97 (3/5 x IH, t, J=7Hz) , 4.28 (2/5 x 2H, ABq, Δ=0.21, J=17Hz), 4.55 (3/5 x 2H, ABq, Δ=0.16, J=15Hz), 6.95-7.34 (9H, m) (4) MASS (m/z) : 281 (M+H) + NMR (CDCI3, δ) : 2.42-3.06 (4H, m) , 3.22-3.88 (2H, m) , 3.97-4.05 (IH, m) , 4.14 (1/3 x IH, d, J=17Hz) , 4.52 (1/3 x IH, d, J=17Hz), 4.71 (2/3 x 2H, ABq, Δ=0.12, J=17Hz), 6.88-7.32 (9H, m) 16981 - 403 - (5) MASS (m/z) : 303 (M+H) + NMR (CDC1 3 , δ) : 2.70 (3/4 x 3H, s) , 2.73-3.08 (2H, m) , 2.89 (1/4 x 3H, s) , 3.80-4.02 (IH, m) , 4.25 (1/4 x 2H, ABq, Δ=0.17, J=17Hz) , 4.50 (3/4 x 2H, ABq, Δ-0.21, J=15Hz) , 6.88-7.34 (9H, m) (6) MASS (m/z) : 347, 349 (M+H) + NMR (CDC1 3 , δ) : 2.70 (3/4 x 3H, S) , 2.73-3.08 (2H, ) , 2.89 (1/4 x 3H, s) , 3.79-4.02 (IH, m) , 4.23 (1/4 x 2H, ABq, Δ=0.17, J=17Hz) , 4.39 (3/4 x IH, d, J=15Hz), 4.59 (3/4 x IH, d, J=15Hz) , 6.82-7.45 (9H, m) (7) MASS (m/z) : 287 (M+H) + NMR (CDC1 3 , δ) : 2.70 (3/4 x 3H, s) , 2.73-3.08 (2H, m) , 2.88 (1/4 x 3H, s) , 3.84-4.02 (IH, m) , 4.25 (1/4 x 2H, ABq, J=17HZ) , 4.52 (3/4 x 2H, ABq, J=17Hz), 6.90-7.35 (9H, m) (8) MASS (m/z) : 300 (M+H) + NMR (CDC1 3 , δ) : 2.69 (3/4 x 3H, s) , 2.74-3.10 (2H, m) , 2.87 (1/4 x 3H, s), 3.88-3.98 (IH, m) , 3.93 (3H, s), 4.20 (1/4 x 2H, ABq, Δ=0.25, J=17Hz) , 4.44 (3/4 x 2H, ABq, Δ=0.20, J=15HZ) , 6.64-6.72 (IK, ) , 7.10-7.45 (8H, m) , 7.85-8.02 (IH, m) (9) MASS (m/z) : 283 (M+H) + NMR (CDC1 3 , δ) : 1.03 (1/2 x 3H, t, J=7Hz) , 1.C7 (1/2 x 3H, t, J=7Hz), 2.70-3.25 (3H + 1/2 x IH, m) , 3.50-3.97 (IH + 1/2 x IH, m) , 4.22 (1/2 x 2H, ABq, , 4.80 (1/2 x IH, d, J-15HZ), 7.00-7.39 (10H, m) (10) MASS (m/z) : 303 (M+H) + NMR (CDC1 3 , δ) : 2.49 (5/6 x 3H, s) , 2.72 (1/6 x 3H, 16981 - 404 - s), 2.98-3.23 (2H, m) , 3.70 (1/6 x IH, d, J=17Hz) , 4.23 (1/6 x IH, d, J-17HZ) , 4.40 (IH, t, J=7Hz) , 4.42 (5/6 x 2H, ABq, Δ=0.07, J=15Hz) , 7.08-7.52 (7H, m) , 8.06 (1/6 x IH, d, J=2Hz), 8.20 (5/6 x IH, d, J=2Hz) (11) MASS (m/z) : 284 (M+H) + NMR (CDC1 3 , δ) : 2.53 (3H, s), 2.70 (3/4 x 3H, s) , 2.73-3.08 (2H, m) , 2.88 (1/4 x 3H, s), 3.84-4.02 (IH, m) , 4.12 (1/4 x IH, d, J=17Hz) , 4.37 (1/4 x IH, d, J=17Hz), 4.51 (3/4 x 2H, ABq, Δ=0.17, J=15Hz), 7.02-7.45 (7H, m) , 8.26 (1/4 x IH, s) , 8.34 (3/4 x IH, s) (12) MASS (m/z) : 336 (M+H) + NMR (CDC1 3 , δ) : 2.72 (2/3 x 3H, s) , 2.72-3.10 (2H, m) , 2.91 (1/3 x 3H, s), 3.88 (1/3 x IH, t, J=7Hz) , 4.01 (2/3 x IH, t, J«7Hz), 4.34 (1/3 x 2H, ABq, Δ=0.17, J=17Hz), 4.60 (2/3 x 2H, ABq, Δ=0.16, J=15Hz), 7.08-7.37 (7H, m) , 7.53-7.65 (2H, m) , 8.09 (IH, s), 8.52 (IH, s) (13) MASS (m/z) : 304 (M+H) + NMR (CDC1 3 , δ) : 2.70 (5/6 x 3H, s) , 2.78-3.08 (2H, m) , 2.88 (1/6 x 3H, s) , 3.84 (1/6 x IH, t, J=7Hz) , 3.97 (5/6 x IH, t, J=7Hz), 4.28 (1/6 x 2H, ABq, Δ=0.22, J=17Hz), 4.52 (5/6 x 2H, ABq, Δ=0.24, J=15Hz), 7.10-7.36 (5H, m) , 7.54 (IH, s) , 8.22 (1/6 x IH, s), 8.32 (5/6 x IH, s) , 8.50 (IH, s) (14) MASS (m/z) : 270 (M+H) + NMR (CDC1 3 , δ) : 2.71 (3/4 x 3H, s) , 2.76-3.10 (2H, m) , 2.88 (1/4 x 3H, s) , 3.82-4.02 (IH, m) , 4.28 (1/4 x 2H, ABq, Δ=0.20, J=17Hz) , 4.55 (3/4 x 2H, ABq, Δ=0.21, J=15Hz) , 7.11-7.55 (7H, m) , 981 - 405 - 8.32-8.58 (2H, m) (15) NMR (CDC1 3 , δ) : 2.69 (3H x 2/3, s), 2.78 (IH, m) , 2.89 (3H x 1/3, s) , 2.97 (IH, m) , 3.78 (3H, s), 3.93 (IH, m) , 4.10 (IH x 1/3, d, J=15Hz) , 4.35 (IK x 1/3, d, J=15Hz), 4.40 (IH x 2/3, d, J=15Hz) , 4.57 (IH x 2/3, d, J=15Hz), 6.81-6.85 <2H, m) , 6.94-7.29 (7H, m) (16) MASS (ESI) (m/z) : 283 (M+H) + NMR (CDC1 3 , δ) : 2.32 (3H, S) , 2.68 (3 x 2/3H, s), 2.73-2.81 (IH, m) , 2.89 (3 x 1/3H, s) , 2.94-3.02 (IH, m) , 3.82-4.00 (IH, ) , 4.12 (2 x 1/4H, d, J=16Hz), 4.37 (2 x 1/4H, d, J=16Hz) , 4.43 (2 x 1/4H, d, J=15Hz), 4.58 (2 x 1/4H, d, J=15Hz), 6.92 (IH, d, J=8Hz), 7.02-7.31 (8H, m) (17) NMR (CDC1 3 , δ) : 2.68 (3H x 2/7, s) , 2.85 (3H x 5/7, s), 3.92-4.61 (4H, m) , 4.86 (IH, br s), 7.11-7.20 (5H, m) , 8.30 (2H, br s) (18) NMR (CDC1 3 , δ) : 0.86 (6H x 2/9, t, J=7Hz) , 0.96 (3H x 7/9, d, J=7Hz), 1.02 (3H x 7/9, d, J=7Hz) , 1.52 (IH, m) , 2.05 (2H, ) , 2.86 (3H x 1/3, s) , 2.91 (3H x 2/3, s), 3.95 (2H x 1/2, s) , 4.20 (IH x 1/2, d, J=15Hz), 4.62 (IH, m) , 4.85 (IH x 1/2, d, J=15Hz) , 7.18-7.34 (5H, m) , 8.57 (2H, br s) (19) NMR (CDC1 3 , δ) : 2.53 (3H x 4/5, s) , 2.80 (3H x 1/5, s), 3.06 (IH, dd, J=8, 13Hz) , 3.32 (IH, dd, J=6, 13Hz), 3.77 (IH X 1/5, d, J=15Hz) , 4.31 (IH x 1/5, d, J=15Hz), 4.54 (2H x 4/5, s) , 4.68 (IH, dd, J=6, 8Hz), 7.10-7.39 (7H, m) , 7.56 (2K, t, J=8Hz) (20) NMR (CDC1 3 , δ) : 2.37 (3H x 3/4, s) , 2.65 (3H x 1/4, 981 - 406 - s), 3.22 (IH, m) , 3.60 (IH, m) , 3.60 (IH x 1/4, d, J-l β Hz) , 4.11 (IH x 3/4, d, J=15Hz) , 4.28 (IH x 1/4, d, J=16Hz) , 4.67 (IH x 3/4, d, J=15H∑), 4.89 (IH, m) , 6.98-7.26 (10H, m) , 8.77 (2H, br s) Preparation 43 The following object compounds were obtained according to a similar manner to that of Preparation 10. (1) MASS (m/z) : 482 (M + -l) NMR (CDCI3, δ) : 1.45 (9H, s) , 2.60 (3H x 2/3, s) , 2.78 (3H x 1/3, s), 2.72-3.16 (4H, m) , 4.21 (IH x 2/3, d, J=15Hz), 4.23 (IH x 1/3, d, J=15Hz) , 4.31 (IH x 1/3, d, J=15Hz), 4.52 (IH, m) , 4.67 (IH x 2/3, d, J-15HZ), 5.22 (IH, m) , 6.17 (IH, m) , 6.82- 7.25 (10H, m) , 7.99 (IH, d, J=8Hz) (2) MASS (m/z) : 484 (M + +l) NMR (CDCI3, δ) : 1.47 (9H, s) , 2.62 (IH, m) , 2.69 (3H x 2/3, s), 2.78 (3H x 1/3, s) , 2.93-3.05 (3H, m) , 4.23-4.33 (IH, m) , 4.48-4.62 (2H, m) , 5.14 (IH, m) , 5.92-6.01 (IH, m) , 6.92 (2H, m) , 7.06 (IH, m) , 7.18-7.22 (7H, m) , 7.83-7.94 (IH, m) Preparation 44 l-tert-Butoxycarbonyl-4-ethylpiperazine (477 mg) was dissolved in a mixture of hydrochloric acid (1 ml) and methanol (2 ml), and heated to reflux for 3 hours. The reaction mixture was allowed to cool to room temperature, evaporated, and dried in vacuo to give a white solid. To this solid was added dichloromethane (5 ml), Starting Compound (972 mg) , 1-hydroxybenzotriazole (278.1 mg) , and triethylamine (0.3 ml). The mixture was cooled in ice, added l-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (360 mg) , then stirred at room temperature for 12 hours. The 981 - 407 - reaction mixture was diluted with ethyl acetate, washed with aqueous sodium hydrogencarbonate, washed with brine, and dried over magnesium sulfate. Evaporation of the solvent followed by subjecting to column chromatography (silica gel, chloroform-methanol) afforded Object Compound (961 mg) as a white powder. MASS (m/z) : 580 (M+H) + NMR (CDC1 3 , δ) : 1.09 (3H, t, J=7Hz) , 1.48 (9H, s) , 2.34-2.65 (7H, m) , 2.54 (2/3 x 3H, s) , 2.78 (1/3 x 3H, s), 2.93-3.30 (3H, m) , 3.40-3.68 (4H, ) , 4.18 (1/3 x 2H, ABq, A-0.17, J=17Hz) , 4.30 (2/3 x IH, d, J=15Hz), 4.45-4.60 (IH, m) , 4.62 (2/3 x IH, d, J=15Hz), 5.08-5.20 (IH, m) , 5.97-6.11 (IH, m) , 6.82-7.32 (10H, m) , 7.32-7.50 (IH, m) Preparation 45 The following object compounds were obtained according to a similar manner to that of Preparation 1, 6 or 11. (1) MASS (m/z) : 566 (M + +l) NMR (CDCI3, δ) : 1.46 (9H, s) , 2.30 (3H, s) , 2.35-2.45 (4H, m) , 2.53 (3H x 2/3, s) , 2.60 (IH, m) , 2.78 (3H x 1/3, s), 2.95-3.13 (2H, m) , 3.22 (IH, m) , 3.46 (2H, m) , 3.61 (2H, m) , 4.08 (IH x 1/3, d, J=15Hz) , 4.27 (IH x 1/3, d, J=15Hz), 4.29 (IH x 2/3, d, J-15HZ), 4.52 (IH, m) , 4.63 (IH x 2/3, d, J=15Hz) , 5.12 (IH, m) , 6.03 (IH, d, J=7Hz) , 6.87-7.04 (2H, m) , 7.20-7.27 (8H, m) , 7.38 (IH x 1/3, d, J=8Hz) , 7.45 (IH x 2/3, d, J=8Hz) (2) MASS (m/z) : 566 (M + +l) NMR (CDC1 3 , δ) : 1.46 (9H, s) , 2.29 (3H, s), 2.33-2.53 (5H, m), 2.58 (3H x 2/3, s), 2.84 (3H x 1/3, s) , 2.94-3.21 (3H, m) , 3.43 (2H, m) , 3.59 (2H, m) , 4.15 (IH x 1/3, d, J=15Hz), 4.30 (IH x 1/3, d, J=15Hz) , 4.33 (IH x 2/3, d, J=15Hz) , 4.54 (IH, m) , 4.66 (IH x 2/3, d, J=15Hz) , 5.13 (IH, m) , 5.92-5.99 (IH, m) , 6.94-7.29 (10H, m) , 7.52 (IH, d, J=8Hz) (3) MASS (FAB) (m/z) : 638 (M+H) + NMR (CDC1 3 , δ) : 1.27 (3H, t, J=8Hz) , 1.47 (9H, s) , 2.53 (3 x 2/3H, s), 2.50-2.62 (5H, m) , 2.78 (3 x 1/3H, s), 2.95-3.13 (2H, m) , 3.17-3.26 (IH, m) , 3.22 (2H, s), 3.47-3.52 (2H, m) , 3.62-3.69 (2H, m) , 4.08-4.32 (2 x 2/3H, m) , 4.19 (2H, q, J=8Hz) , 4.47- 4.57 (IH, m) , 4.62 (2 x 1/3H, d, J=15Hz) , 5.08-5.17 (IH, m) , 6.02 (IH, d, J=8Hz) , 6.85-6.89 (2 x 1/3H, m) , 7.01-7.03 (2 x 2/3H, m) , 7.16-7.30 (8H, m) , 7.40 (1 x 1/3H, d, J=8Hz) , 7.45 (1 x 2/3H, d, J=8Hz) Preparation 46 The following object compounds were obtained according o a similar manner to that of Preparation 1, 6, 11 or 38. (1) MASS (m/z) : 697 (M+H) + NMR (CDC1 3 , δ) : 1.46 (9H, s) , 2.42 (3H, s) , 2.48-2.62 (IH, m) , 2.80-2.95 (IH, m) , 2.82 (1/3 x 3H, s), 2.88 (2/3 x 3H, s) , 2.95-3.10 (IH, m) , 3.10-3.26 (IH, m) , 3.35-3.72 (8H, m) , 4.28-4.68 (3H, m) , 5.10-5.25 (IH, m) , 5.94-6.06 (IH, m) , 7.02-7.90 (12H, m) (2) MASS (m/z) : 552 (M+H) + NMR (CDCI3, δ) : 1.44 (9H, s) , 2.23-2.42 (4H, m) , 2.26 (3H, s), 2.45-2.70 (IH, m) , 2.81 (2/3 x 3H, s), 2.85 (1/3 x 3H, s) , 3.00-3.25 (IH, m) , 3.30-3.65 (4H, m), 4.32 (1/3 x IH, d, J=17Hz) , 4.42-4.61 (IH + 1/3 x IH, m) , 4.60 (2/3 x 2H, ABq, J=15Hz), 5.73-5.87 (IH, m) , 5.98-6.12 (IH, m) , 6.90-7.47 (10H, m) , 8.03-8.25 (IH, m) (3) MASS (m/z) : 569 (M+H) + NMR (CDC1 3 , δ) : 1.48 (9H, s) , 2.50 (2/3 x 3H, s), 5 2.50-2.65 (IH, m) , 2.74 (1/3 x 3H, s), 2.95-3.25 (3H, m), 3.38-3.70 (8H, m) , 3.77 (2/5 x IH, d, J=17Hz), 4.20 (2/5 x IH, d, J=17Hz) , 4.35 (3/5 x 2H, ABq, Δ=0.10, J=15Hz) , 4.48-4.62 (IH, ) , 5.02- 5.22 (IH, m), 6.02 (IH, br d) , 6.28 (2/3 x IH, br ° s), 6.60-7.55 (10H + 1/3 x IH, m) (4) MASS (m/z) : 608 (M + ) NMR (CDC1 3 , δ) : 1.46 (9H, s) , 2.30 (3H, s) , 2.30-2.63 (5H, m), 2.50 (3/5 x 3H, s), 2.73 (2/5 x 3H, s) , 5 2.90 (2/5 x 6H, s) , 2.92 (3/5 x 6H, s) , 2.97-3.12 (2H, m), 3.12-3.30 (IH, m) , 3.37-3.70 <4H, m) , 3.87 (2/5 x IH, d, J=17Hz), 4.19 (2/5 x IH, d, J=17Hz) , 4.22 (3/5 x IH, d, J=15Hz) , 4.47-4.58 (IH, m) , 4.50 (3/5 x IH, d, J=15Hz), 5.00-5.25 (IH, m) , 5.93-6.10 0 (IH, br d) , 6.42-7.52 (10H, m) (5) MASS (m/z) : 623 (M+H) + NMR (CDC1 3 , δ) : 1.47 (9H, s) , 2.23 (1/3 x 6H, s), 2.25 (2/3 x 6K, s), 2.30 (3H, s) , 2.32-2.50 (4H, 5 ) , 2.50-2.64 (IH, m) , 2.53 (2/3 x 3H, s) , 2.78 (1/3 x 3H, s), 2.92-3.30 (3H, m) , 3.39 (1/3 x 2H, s), 3.42 (2/3 x 2H, s), 3.42-3.70 (4H, m) , 4.17 (1/3 x 2H, ABq, Δ=0.17, J-17HZ) , 4.28 (2/3 x IH, d, J=15Hz), 4.43-4.60 (IH, m) , 4.62 (2/3 x IH, d, 0 J=15Hz), 5.03-5.20 (IH, m) , 5.96-6.10 (IH, m) , 6.80-7.50 (10H, m) (6) MASS (m/z) : 578 (M+H) + NMR (CDC1 3 , δ) : 1.46 (9H, s) , 2.18-2.82 (7H, m) , 2.30 5 (3H, s), 2.92-3.12 (2H, m) , 3.12-3.30 (IH, m) , 81 - 410 - 3.37-3.85 (6H, m) , 3.89 (1/3 x IH, d, J=17Hz), 4.32 (1/3 x IH, d, J=17Hz), 4.45-4.58 (IH, m) , 4.62 (2/3 x 2H, ABq, Δ=0.15, J=17Hz) , 5.10-5.21 (IH, m) , 5.98-6.10 (IH, m) , 6.78-7.57 (10H, m) (7) MASS (m/z) : 600 (M+H) + NMR (CDC1 3 , δ) : 1.48 (9H, s), 2.30 (3H, s) , 2.32-2.50 (4H, m) , 2.52-2.63 (IH, m) , 2.55 (2/3 x 3H, s) , 2.75 (1/3 x 3H, s) , 2.95-3.30 (3H, m) , 3.38-3.68 (4H, m) , 4.14 (1/3 x 2H, ABq, Δ=0.09, J=17HZ) , 4.22 (2/3 x IH, d, J=15Hz), 4.45-4.58 (IH, m) , 4.58 (2/3 x IH, d, J=15Hz), 5.05-5.20 (IH, m) , 5.95-6.10 (IH, m) , 6.70-6.95 (2H, m) , 7.12-7.45 (8H, m) (8) MASS (m/z) : 644, 646 (M+H) "1" NMR (CDC1 3 , δ) : 1.48 (9H, s), 2.30 (3H, s) , 2.30-2.50 (4H, m) , 2.50-2.63 (IH, ) , 2.55 (3/4 x 3H, s) , 2.75 (1/4 x 3H, s), 2.90-3.30 (3H, m) , 3.38-3.68 (4H, m) , 4.13 (1/4 x 2H, ABq, Δ=0.07, J=17Hz) , 4.22 (3/4 x IH, d, J=15Hz) , 4.46-4.59 (IH, m) , 4.58 (3/4 x IH, d, J=15Hz), 5.03-5.17 (IH, m) , 5.97-6.08 (IH, m) , 6.62-6.91 (2H, m) , 7.15-7.48 (8H, m) (9) MASS (m/z) : 584 (M+H) + NMR (CDC1 3 , δ) : 1.47 (9H, s) , 2.30 (3H, s) , 2.30-2.48 (4H, m) , 2.50-2.65 (IH, ) , 2.54 (3/4 x 3H, s) , 2.73 (1/4 x 3H, s) , 2.92-3.30 (3H, m) , 3.38-3.68 (4H, m) , 4.13 (1/4 x 2H, ABq, Δ=0.14, J=17Hz) , 4.23 (3/4 x IH, d, J=15Hz), 4.45-4.59 (IH, m) , 4.58 (3/4 x IH, d, J=15Hz), 5.05-5.18 (IH, m) , 5.98-6.10 (IH, m) , 6.72-7.03 (4H, m) , 7.15-7.48 (6K, m) (10) MASS (m/z) : 597 (M+H) + NMR (CDC1 3 , δ) : 1.48 (9H, s) , 2.30 (3H, s) , 2.33-2.50 (4H, m) , 2.50-2.63 (IH, ) , 2.52 (3/4 x 3H, s) , 2.71 (1/4 x 3H, s), 2.95-3.28 (3H, m) , 3.38-3.68 (4H, m) , 3.89 (1/4 x 3H, s) , 3.92 (3/4 x 3H, s), 3.92 (1/4 x IH, d, J=17Hz) , 4.18 (1/4 x IH, d, J=17Hz), 4.20 (3/4 x IH, d, J=15Hz) , 4.48-4.58 (IH, m), 4.51 (3/4 x IH, d, J=15Hz) , 5.01-5.27 (IH, m) , 5.95-6.10 (IH, br d) , 6.53-6.68 (IH, m) , 7.12-7.48 (7H, m) , 7.74-7.94 (IH, m) (11) MASS (m/z) : 580 (M+H) + NMR (CDC1 3 , δ) : 0.90 (3/5 x 3H, t, J=7Hz) , 0.98 (2/5 x 3H, t, J=7Hz), 1.45 (9H, s) , 2.32 (3H, s) , 2.35- 2.62 (5H, ) , 2.83-3.32 (5H, m) , 3.35-3.70 (4H, m) , 4.12 (2/5 x 2H, ABq, Δ=0.18, J=17Hz) , 4.18 (3/5 x IH, d, J=15Hz), 4.42-4.62 (IH, m) , 4.78 (3/5 x IH, d, J=15Hz), 4.96-5.18 (IH, m) , 5.92-6.10 (IH, br d), 6.85-7.46 (11H, m) (12) MASS (m/z) : 601 (M+H) + NMR (CDC1 3 , δ) : 1.48 (9H, s) , 2.30 (3H, s) , 2.30-2.51 (4H, ) , 2.51-2.63 (IH, ) , 2.58 (4/5 x 3H, s) , 2.73 (1/5 x 3H, s) , 2.93-3.30 (3H, m) , 3.40-3.70 (4H, m) , 4.16 (1/5 x 2H, ABq, Δ=0.09, J=17Hz) , 4.25 (4/5 x IH, d, J=15Hz), 4.48-4.58 (IH, m) , 4.57 (4/5 x IH, d, J=15Hz), 5.02-5.17 (IH, m) , 5.97-6.10 (IH, m) , 7.10-7.48 (8H, m) , 8.01 (1/5 x IH, d, J=2Hz) , 8.15 (4/5 x IH, d, J=2Hz) (13) MASS (m/z) : 581 (M+H) + NMR (CDC1 3 , δ) : 1.47 (9H, s) , 2.30 (3H, s), 2.30-2.64 (5H, m) , 2.51 (1/4 x 3H, s) , 2.53 (3/4 x 3H x 2, s), 2.72 (1/4 x 3H, s), 2.94-3.30 (3H, m) , 3.39- 3.68 (4H, m), 4.00 (1/4 x IH, d, J=17Hz) , 4.22 (1/4 x IH, d, J=17Hz), 4.27 (3/4 x IH, d, J=15Hz) , 4.46- 4.60 (IH, ) , 4.53 (3/4 x IH, d, J=15Hz) , 5.01-5.21 (IH, m) , 5.95-6.10 (IH, br d) , 6.91-7.50 (8H, ) , 8.14 ( 1/4 x IH, d, J=2Hz), 8.27 ( 3/4 x ι « d J=2Hz) ' ' ( 14 ) MASS (m/z) : 568 (M + H ) + NMR ( CDCI3. δ ) : 1.47 (9H, .,, 2.50-2.63 (1K , m, , 2.51 d/4 x 3H, s ) , 2.53 ( 3/4 x 3H x 2, S ) , 2.73 ( 1/4 x 3H, s ) , 2.95-3.28 ( 3H, m) , 3.38-3.78 ( 8H, m ) , 3 98 ( /4 X IH, d, J=17HZ), 4.23 (1/4 x 1Hf d J=17H2) 4.28 ( 3/4 x IH, d, J=15Hz) , 4.46-4.62 ( l H , m ) , 4 54 ( 3 4 x lH, d, J=15HZ ) , 5.01-5.22 (IH, m, , 5.93-6.08 ( IH, m ) , 6.95-7.52 (8H, m) , 8.15 (1/4 x ι H/ s) 8.28 (3/4 x IH, s) ( 15 ) MASS (m/z) : 633 (M + H ) + NM ( CDC1 3 , δ ) : !.48 (9H, s) , 2.30 (3H, s ) , 2.30-2 63 ( 5H, a ) , 2.61 ( 2/3 x 3H, s) , 2.89 (1/3 x 3H , s ) 2.93-3.30 ( 3H, m ) , 3.37-3.68 (4H, m) , 4.23 ( l/ 3 ' x 2H, ABq, Δ =0.12, J=17Hz) , 4.38 (2/3 x 1H , d, J=15Hz ) , 4.45-4.60 (IH, m) , 4.62 (2/3 x i H ,' d J=15Hz ) , 5.08-5.21 (IH, m) , 5.95-6.10 ( l H , m ) ' 6-91-7.62 ( 10H, m) , 8.11 (1 H , s) , 8.52 ( IH, S) ( 16 ) MASS (m/z) : 601 (M + H ) + ™* ( CDC1 3 , δ ) : i.47 (9H, s) , 2.30 (3H, s ) , 2.3 0 -2 50 ( 4H, m ) , 2.50-2.64 (IH, m) , 2.56 (4/5 x 3H, s ) , 2-75 ( 1/5 x 3H, s ) , 2.93-3.30 (3H, m) , 3.4 0 -3 68 ( 4H, m ) , 4.18 ( 1/5 x 2H, ABq, Δ =0.09, J-l7Hz ) , 4 22 ( 4/5 x IH, d, J=15Hz), 4.46-4.62 (IH, m ) , 4.64 ( 4/5 * IH, d, J-15H Z) , 5.02-5.15 (IH, m) , 5.96-6.10 ( IH »>, 7.10-7.52 ( 7H, m) , 8.08 (1/5 x 1 H , S) , 8.23 ( 4/5 x IH, s), 8.41-8.50 (IH, m ) ( 17 ) MASS (m/z) : 588 (M + H ) + NMR ( CDC1 3 , δ ) : !. 4 7 (9H, s) , 2.50-2.62 ( IH, m ) , 2 . 58 ( 3/4 x 3H, s ) , 2.73 (1/4 x 3H, s) , 2.92-3.28 (3H , 981 - 413 - m) , 3.39-3.78 (8H, m) , 4.15 (1/4 x 2H, ABq, Δ=0.13, J=17Hz), 4.27 (3/4 x IH, d, J=15Hz), 4.48-4.61 (IH, m) , 4.55 (3/4 x IH, d, J=15Hz) , 5.02-5.15 (IH, m) , 5.93-6.08 (IH, m) , 6.92-7.50 (8H, m) , 8.02 (1/4 x IH, m) , 8.15 (3/4 x IH, m) (18) MASS (m/z) : 554 (M+H) + NMR (CDC1 3 , δ) : 1.47 (9H, s) , 2.48-2.62 (IH, m) , 2.55 (3/4 x 3H, s), 2.75 (1/4 x 3H, s) , 2.92-3.28 (3H, m) , 3.35-3.80 (8H, m) , 4.18 (1/4 x 2H, ABq, Δ=0.18, J=17Hz), 4.29 (3/4 x IH, d, J=15Hz) , 4.46-4.62 (IH, m) , 4.61 (3/4 x IH, d, J=15Hz) , 5.00-5.18 (IH, m) , 5.93-6.07 (IH, m) , 7.03-7.50 (8H, ) , 8.18-8.53 (2H, m) (19) MASS (m/z) : 567 (M+H) + NMR (CDC1 3 , δ) : 1.47 (9H, s) , 2.30 (3H, s) , 2.32-2.48 (4H, m) , 2.52-2.63 (IH, m) , 2.54 (3/4 x 3H, s) # , 2.74 (1/4 x 3H, s) , 2.93-3.30 (3H, m) , 3.38-3.68 (4H, m) , 4.18 (1/4 x 2H, ABq, Δ=0.14, J=17HZ) , 4.28 (3/4 x IH, d, J-15HZ), 4.45-4.60 (IH, m) , 4.62 (3/4 x IH, d, J=15Hz) , 5.03-5.20 (IH, m) , 5.93-6.10 (IH, ) , 7.00-7.50 (8H, ) , 8.18-8.53 (2H, m) (20) MASS (m/z) : 596 (M + +l) NMR (CDC1 3 , δ) : 1.44 (9H, s), 2.28 (3H, s) , 2.37 (4H, m) , 2.51 (3H x 2/3, s) , 2.60-2.79 (IH, m) , 2.73 (3H x 1/3, s), 2.95-3.07 (2H, m) , 3.22 (IH, m) , 3.46 (2H, m) , 3.61 (2H, m) , 3.77 (3H x 1/3, s) , 3.78 (3H x 2/3, s), 3.96 (IH x 1/3, d, J=15Hz) , 4.22 (IH x 2/3, d, J=15Hz), 4.41 (IH x 1/3, d, J=15Hz), 4.54 (IH x 2/3, d, J=15Hz), 4.54 (IH, m) , 5.06-5.18 (IH, m) , 6.02 (IH, m) , 6.77-7.00 (4H, m) , 7.08-7.25 (5H, m) , 7.43 (IH, m) ( 21) MASS (ESI) (m/z) : 580 (M+H) + NMR ( CDC1 3 , δ) : 1.43 (9H, s) , 2.25 (3H, s), 2.31 ( 3H, s ) , 2.35-2.48 (4H, m) , 2.52 (3 x 2/3H, s), 2.54- 2.62 ( IH, m), 2.76 (3 x 1/3H, s), 2.97-3.10 (2H, m ) , 3.17-3.28 (IH, m) , 3.42-3.50 (2H, m) , 3.58-3.64 ( 2H, m ) , 4.02 (2 x 1/4H, d, J=16Hz) , 4.22 (2 x 1/4H, d, J=16Hz), 4.27 (2 x 1/4K, d, J=15Hz) , 4.58 ( 2 x 1/4H, d, J=15Hz), 4.48-4.57 (IH, m) , 5.08-5.19 ( IH, m ) , 6.03 (IH, d, J=8Hz) , 6.78 (2 x 1/3H, d, J=8Hz ) , 6.91 (2 x 2/3H, d, J=8Hz), 7.03 (2H, t, J=8Hz), 7.18-7.30 (5H, m) , 7.40 (1 x 1/3H, d, J=8Hz), 7.47 (1 x 2/3H, d, J=8Hz) ( 22) MASS (m/z) : 506 (M + +l) NMR ( CDC1 3 , δ) : 1.46 (9H, s), 2.28 (3H, s) , 2.35-2.42 ( 4H, m ) , 2.57 (IH, m) , 2.93 (3H x 1/3, s), 2.98 (3H x 2/3, s), 3.29-3.75 (6H, m) , 3.86-3.94 (IH, m) , 4.52 ( IH x 2/3, d, J=15Hz) , 4.54 (IH, m) , 4.63 (2H x 1/3, s), 4.71 (IH x 2/3, d-, J=15Hz) , 5.02 (IH, m ) , 5.89 (IH, d, J=8Hz), 7.15-7.35 (5H, m) , 7.53 ( IH x 1/3, d, J=8Hz), 7.61 (IH x 2/3, d, J=8Hz ) ( 23) MASS (m/z) : 532 (M + +l) NMR ( CDC1 3 , δ) : 0.78 (3H x 1/3, d, J=7Hz) , 0.83 ( 3H x 1/3, d, J=7Hz), 0.92 (3H x 2/3, d, J=7Hz) , 0.96 (3H x 2/3, d, J=7Hz), 1.44 (9H, s), 1.43-1.70 (3H, m) , 2.30 ( 3H, s), 2.38 (4H, m) , 2.57 (IH, m) , 2.92 (3H x 1/3, s), 2.97 (3H x 2/3, s) , 3.17 (IH, m) , 3.46 ( 2H, m), 3.59 (2H, ) , 4.42 (IH x 2/3, d, J=15Hz) , 4.53 (IH, m) , 4.57 (IH x 1/3, d, J=15Hz) , 4.69 (IH x 1/3, d, J-15HZ), 4.73 (IH x 2/3 d, J=15Hz) , 4.96 ( IH, m) , 6.05 (IH, m) , 7.17-7.35 (6H, m) ( 24) MASS (m/z) : 634 (M + +l) NMR ( CDC1 3 , δ) : 1.47 (9H, s) , 2.30 (3H, s) , 2.35-2.46 (4H, m) , 2.52-2.61 (IH, ) , 2.59 (3H x 3/4, s), 2.78 (3H x 1/4, s), 2.93-3.26 (3H, m) , 3.45 (2H, m) , 3.60 (2H, m) , 4.27 (2H x 1/4, s), 4.33 (IH x 3/4, d, J=15Hz), 4.53 (IH, m) , 4.65 (IH x 3/4, d, J=15Hz), 5.05 (IH x 1/4, m) , 5.14 (IH x 3/4, q, J=7Hz), 6.02 (IH, m) , 6.90-7.23 (7H, m) , 7.33-7.52 (3H, m) (25) MASS (m/z) : 566 (M + +l) NMR (CDC1 3 , δ) : 1.46 (9H, s), 2.29 (3H, s) , 2.33-2.53 (5H, ) , 2.58 (3H x 2/3, s) , 2.84 (3H x 1/3, s) , 2.94-3.21 (3H, m) , 3.43 (2H, m) , 3.59 (2H, m) , 4.15 (IH x 1/3, d, J=15Hz), 4.30 (IH x 1/3, d, J=15Hz) , 4.33 (IH x 2/3, d, J=15Hz) , 4.54 (IH, m) , 4.66 (IH x 2/3, d, J=15Hz), 5.13 (IH, m) , 5.92-5.99 (IH, m) , 6.94-7.29 (10H, m) , 7.52 (IH, d, J=8Hz) (26) MASS (m/z) : 574 (M + +l) NMR (CDC1 3 , δ) : 1.45 (9H, s) , 2.54 (3H x 2/3, s) , 2.71 (IH, m) , 2.81 (3H x 1/3, s) , 2.92-3.12 (3H, m) , 4.05 (IH x 1/3, d, J=15Hz), 4.28 (IH x 1/3, d, J=15Hz), 4.32 (IH x 2/3, d, J=15Hz) , 4.53 (IH, ) , 4.61 (IH x 2/3, d, J=15Hz) , 5.07-5.18 (3H, m) , 5.58 (IH, ) , 6.89-7.34 (16H, m) (27) MASS (m/z) : 574 (M + +l) NMR (CDC1 3 , δ) : 1.45 (9H, s) , 2.59 (3H x 2/3, s) , 2.68 (IH, dd, J=5, 16Hz) , 2.84 (3H x 1/3, s), 2.95- 3.05 (3H, m) , 4.09 (IH x 1/3, d, J=15Hz) , 4.31 (IH x 1/3, d, J=15Hz), 4.37 (IH x 2/3, d, J=15Hz) , 4.53 (IH, ) , 4.62 (IH x 2/3, d, J=15Hz) , 5.07-5.17 (3H, ) , 5.56 (IH, m) , 6.93-7.36 (16H, m) Preparation 7 Starting Compound (194 mg) was dissolved in methanol (20 ml), and hydrogenated (3 kg/cm 2 ) over 10% palladium on carbon (20 mg) at room temperature for 3 hours. The palladium on carbon was filtered off, and the remaining solution was evaporated and dried in vacuo. The residue was dissolved in dichloromethane (5 ml), and to this solution was added Compound A (153 mg) , 1-hydroxybenzotriazole (65 mg) , and 1- ethyl-3- (3-dimethylaminopropyl) carbodiimide hydrochloride (104 mg) with ice-cooling, then the mixture was stirred at room temperature for 15 hours. The reaction mixture was diluted with chloroform, washed with aqueous sodium hydrogencarbonate, washed with brine, and dried over magnesium sulfate. Evaporation of the solvent followed by subjecting to column chromatography (silica gel, chloroform- methanol) afforded Object Compound (173 mg) as white powder. MASS (m/z) : 539 (M+H) + NMR (CDC1 3 , δ) : 1.36 (9H, s) , 2.58-2.68 (IH, m) , 2.90-3.00 (IH, m) , 3.03-3.12 (IH, ) , 3.25-3.45 (5H, m) , 3.50-3.66 (4H, m) , 4.30-4.45 (3H, m) , 4.60-4.72 (IH, m) , 5.66 (IH, br d) , 6.72-6.90 (2H, m) , 7.08-7.30 (10H, m) Preparation 48 The following object compound was obtained according to a similar manner to that of Preparation 47. MASS (m/z) : 449 (M+H) + NMR (CDC1 3 , δ) : 1.39 (9H, S) , 2.62-2.72 (IH, m) , 2.87-3.14 (2H, ) , 3.22-3.32 (IH, m) , 3.40-3.47 (2H, m) , 3.50-3.57 (2H, m) , 3.62-3.70 (4H, m) , 4.37-4.50 (IH, m) , 4.60-4.70 (IH, m) , 5.31 (IH, br s), 5.75 (IH, br d) , 6.48 (12H, br d) , 6.83 (IH, br d), 7.20-7.35 (5H, ) Preparation 49 Trifluoroacetic acid (4 ml) was added to Starting Compound (700 mg) with ice-cooling, and stirred at room temperature for 1 hour. The reaction mixture was evaporated, and to the remaining oil was added hydrogen chloride in methanol and evaporated, then the remaining solid was dried in vacuo. To this solid was added dichloromethane (4 ml), Compound A (535 mg) , 1-hydroxybenzotriazole (244 mg) , and 1- ethyl-3- ( 3-dimethylaminopropyl ) carbodiimide ( 322 mg) , and the mixture was stirred at room temperature for 12 hours. The reaction mixture was diluted with chloroform, washed with aqueous sodium hydrogencarbonate, washed with brine, and dried over magnesium sulfate. Evaporation of the solvent followed by subjecting to column chromatography (silica gel, chloroform-methanol) afforded Object Compound (728 mg) as white powder. MASS (m/z) : 583 (M+H) + NMR (CDC1 3 , δ) : 1.48 (9H, s) , 2.50 (2/3 x 3H, s) , 2.5-2.6 (IH, m), 2.73 (1/3 x 3H, s) , 3.0-3.1 (2H, m), 3.1-3.2 (IH, m) , 3.4-3.7 (8H, m) , 3.75 (1/3 x 3H, s), 3.78 (2/3 x 3H, s) , 3.95 (1/3 x IH, d, J=17Hz), 4.22 (2/3 x IH, d, J=15Hz) , 4.22 (1/3 x IH, d, J=17Hz), 4.54 (2/3 x IH, d, J=15Hz) , 4.5-4.6 (IH, m) , 5.1-5.2 (IH, m) , 6.00 (IH, br d, J=9Hz) , 6.7-6.8 (1/3 x 4H, m) , 6.78 (2/3 x 2H, d, J=9Hz) , 6.98 (2/3 x 2H, d, J=9Hz) , 7.1-7.2 (5H, m) , 7.40 (1/3 x IH, d, J=8Hz), 7.45 (2/3 x IH, d, J=8Hz) Preparation ~ n The following object compounds were obtained according to a similar manner to that of Preparation 49. (1) MASS (m/z) : 463 (M+H) + NMR (CDC1 3 , δ) : 1.45 (9H, s), 2.48-2.63 (IH, m) , 2.87 (2/3 x 3H, s), 2.98 (1/3 x 3K, s), 3.17-3.78 (9H, m), 4.02-4.22 (3H, m) , 4.47 (1/3 x 2H, s), 4.61 (2/3 x 2H, ABq, Δ=0.09, J=15Hz) , 6.00-6.13 (IH, m) , 7.10-7.70 (6H, m) (2) MASS (m/z) : 539 (M+H) + NMR (CDC1 3 , δ) : 1.43 (9H, s) , 2.5-2.6 (2H, m) , 2.80 (2/3 x 3H, s), 2.85 (1/3 x 3H, s) , 3.0-3.1 (IH, m) , 3.3-3.6 (8H, m) , 4.32 (1/3 x IH, d, J=15Hz) , 4.42 (1/3 x IH, d, J=15Hz), 4.60 (2/3 x 2H, ABq, Δ=0.15, J=15Hz), 5.78 (2/3 x IH, d, J=7Hz) , 5.82 (1/3 x IH, d, J=7Hz), 6.10 (IH, br d, J=7Hz) , 6.9-7.4 (10H, i), 8.12 (IH, br d, J=7Hz) (3) MASS (m/z) : 659 (M+H) + NMR (CDC1 3 , δ) : 1.48 (9H, s) , 2.48-2.62 (IH, m) , 2.54 (2/3 x 3H, s), 2.78 (1/3 x 3H, s) , 2.90-3.05 (2H, m) , 3.10-3.28 (IK, m) , 3.37-3.75 (8H, m) , 4.10 (1/3 x IH, d, J=17Hz), 4.27 (1/3 x IH, d, J=17Hz) , 4.28 (2/3 x IH, d, J=15Hz), 4.46-4.60 (IH, ) , 4.60 (2/3 x IH, d, J=15Hz), 5.01 (2/3 x 2H, s) , 5.02-5.13 (IH, m) , 5.07 (1/3 x 2H, s), 6.00 (IH, br d) , 6.75- 7.48 (15H, m) (4) MASS (m/z) : 672 (M+H) + NMR (CDC1 3 , δ) : 1.46 (9H, s) , 2.29 (3H, s), 2.30-2.49 (4H, m) , 2.50-2.63 (IH, m) , 2.54 (2/3 x 3H, s) , 2.77 (1/3 x 3H, s) , 2.85-3.10 (2H, m) , 3.13-3.30 (IH, m) , 3.35-3.68 (4H, m) , 4.19 (1/3 x 2K, ABq, Δ=0.16, J=17Hz), 4.27 ( 2/3 x IH, d, J=15Hz) , 4.42- 4.62 (IH, m) , 4.62 (2/3 x IH, d, J=15Hz) , 4.94-5.17 (3H, m) , 5.93-6.10 (IH, m) , 6.72-7.50 (15H, m) (5) MASS (m/z) : 569 (M+H) + NMR (CDC1 3 , δ) : 1.47 (9H, s) , 2.48-2.72 (IH, m) , 2.62 (2/3 x 3H, s), 2.81 (1/3 x 3H, s) , 2.82-3.05 (2H, m) , 3.05-3.28 (IH, m) , 3.30-3.75 (8H, m) , 4.28 (1/3 x 2H, ABq, Δ=0.15, J=17Hz) , 4.33 (2/3 x IH, d. J=15Hz), 4.45-4.63 (IH, m) , 4.60 (2/3 x IH, d, J=15Hz), 4.98-5.15 (IH, m) , 5.92-6.12 (IH, br d) , 6.42-7.60 (11H, m) (6) MASS (m/z) : 567 (M+H) + NMR (CDC1 3 , δ) : 1.49 (9H, s) , 2.39-2.77 (4H, m) , 2.58 (3/5 x 3H, s), 2.80 (2/5 x 3H, s) , 2.90-3.05 (2H, m), 3.10-3.40 (2H, m) , 3.40-3.80 (8H, m) , 4.45-4.60 (IH, m) , 4.93-5.10 (IH, m) , 5.92-6.08 (IH, m) , 6.98-7.48 (11H, m) (7) MASS (m/z) : 611 (M+H) + NMR (CDC1 3 , δ) : 1.45 (9H, s), 2.59 (2/3 x 3H, s), 2.5-2.6 (IH, m), 2.79 (1/3 x 3H, s) , 3.0-3.1 (2H, m), 3.1-3.2 (IH, m), 3.4-3.7 (8H, m) , 3.90 (3H, s) , 4.33 (IH, d, J=15Hz), 4.5-4.6 (IH, m) , 4.69 (IH, d, J=15Hz), 5.1-5.2 (IH, m) , 6.02 (IH, br s) , 6.90 (IH, br d, J=9Hz), 7.0-7.3 (7H, m) , 7.8-7.9 (2H, m) (8) MASS (m/z) : 603 (M+H) + NMR (CDC1 3 , δ) : 1.47 (9H, s) , 2.5-2.6 (IH, m) , 2.58 (3/5 x 3H, s), 2.83 (2/5 x 3H, s) , 3.0-3.1 (2H, m) , 3.2-3.3 (IH, ), 3.4-3.7 (8H, m) , 4.23 (2/5 x IH, d, J=17Hz), 4.45 (2/5 x IH, d, J=17Hz) , 4.47 (3/5 x IH, d, J=15Hz), 4.5-4.6 (IH, ) , 4.77 (3/5 x IH, d, J=15Hz), 5.1-5.3 (IH, m) , 6.03 (IH, br d, J=9Hz) , 7.1-7.3 (6H, m), 7.4-7.6 (4H, m) , 7.7-7.9 (3H, m) (9) MASS (m/z) : 603 (M+H) + NMR (CDC1 3 , δ) : 1.48 (9H, s) , 2.42-2.62 (IH, m) , 2.52 (2/3 x 3H, s), 2.88 (1/3 x 3H, s) , 2.93-3.25 (3H, m) , 3.35-3.75 (8H, m) , 4.40-4.60 (IH, m) , 4.65 (1/3 x 2H, ABq, , 4.82 (2/3 x IH, d, J=15Hz), 4.95-5.20 (IH, m) , 5.15 (2/3 x IH, d, J=15Hz), 6.03 (IH, br d), 6.78-8.05 (13H, ) (10) MASS (m/z) : 554 (M+H) + NMR (CDC1 3 , δ) : 1.48 (9H, s) , 2.48-2.62 (IH, m) , 2.70 (2/3 x 3H, s), 2.85 (1/3 x 3H, s), 2.95-3.26 (3H, m) , 3.38-3.75 (8H, m) , 4.30 (1/3 x 2H, ABq, Δ=0.11, J=17Hz), 4.50-4.60 (IH, m) , 4.58 (2/3 x 2H, ABq, Δ=0.15, J=15Hz), 5.05-5.20 (IH, m) , 5.98 (IH, br d) , 6.82-7.63 (9H, m) , 8.48 (IH, m) (11) MASS (m/z) : 554 (M+H) + NMR (CDC1 3 , δ) : 1.48 (9H, s) , 2.48-2.65 (IH, m) , 2.64 (2/3 x 3H, s), 2.80 (1/3 x 3H, s) , 2.90-3.28 (3H, m) , 3.35-3.76 (8H, m) , 4.25 (1/3 x 2H, ABq, Δ=0.12, J=17Hz), 4.31 (2/3 x IH, d, J=15Hz) , 4.50-4.60 (IH, m) , 4.59 (2/3 x IH, d, J=15Hz) , 4.92-5.22 (IH, m) , 6.01 (IH, br d) , 6.55-6.90 (2H, ) , 7.13-7.48 (6H, m) , 8.38-8.51 (2H, ) (12) MASS (FAB) (m/z) : 624 (M+H) + NMR (CDC1 3 , δ) : 1.49 (9H, s) , 2.30 (3H, s) , 2.35-2.48 (4H, m) , 2.52-2.62 (IH, m) , 2.59 (3 x 2/3H, s), 2.68 (3 x 1/3H, s) , 2.94-3.13 (2H, m) , 3.20-3.27 (IH, m) , 3.42-3.50 (2H, m) , 3.58-3.65 (2H, m) , 3.90 (3H, s), 4.23-4.34 (2 x 2/3H, m) , 4.49-4.58 (IH, m) , 4.70 (2 x 1/3H, d, J=15Hz) , 5.04-5.19 (IH, m) , 5.99-6.07 (IH, m) , 6.88 (2 x 1/3H, d, J=8Hz) , 7.03 (2 x 2/3H, d, J=8Hz), 7.18-7.30 (5H, m) , 7.37 (1 x 1/3H, d, J=8Hz), 7.43 (1 x 2/3H, d, J=8Hz) , 7.88 (2 x 1/3H, d, J=8Hz), 7.92 (2 x 2/3H, d, J=8Hz) (13) MASS (FAB) (m/z) : 696 (M+H) + NMR (CDC1 3 , δ) : 1.27 (3H, t, J=8Hz) , 1.47 (9H, s), 2.52-2.65 (5H, m) , 2.62 (3 x 2/3H, s), 2.78 (3 x 1/3H, s), 2.92-3.12 (2H, m) , 3.17-3.30 (IH, m) , 3.26 (2H, s), 3.47-3.54 (2H, m) , 3.61-3.70 (2H, m) , 3.92 (3H, s) , 4.19 (2H, q, J=8Hz) , 4.27-4.32 (2 x 2/3H, m) , 4.48-4.58 (IH, m) , 4.70 (2 x 1/3H, d, J-15HZ), 5.03-5.18 (IH, ) , 5.95-6.08 (IH, m) , 6.88 (2 x 1/3H, d, J=8Hz), 7.03 (2 x 2/3H, d, J=8Hz) , 7.17-7.28 (5H, m) , 7.37 (1 x 1/3H, d, J=8Hz) , 7.44 (1 x 2/3H, d, J=8Hz), 7.88 (2 x 1/3H, d, J=8Hz) , 7.92 (2 x 2/3H, d, J=8Hz) (14) MASS (m/z) : 595 (M+) NMR (CDC1 3 , δ) : 1.48 (9H, s), 2.50 (2/3 x 3H, s) , 2.5-2.6 (2H, m) , 2.75 (1/3 x 3H, s) , 2.91 (1/3 x 6H, s), 2.94 (2/3 x 6H, s), 3.03 (2H, m) , 3.1-3.2 (IH, m) , 3.4-3.7 (8H, m) , 3.87 (1/3 x 2K, d, J=16Hz) , 4.24 (IH, d, J=l5Hz) , 4.47 (2/3 x 2H, d, J=15Hz), 4.5-4.6 (IH, m) , 5.0-5.1 (2/3 x IH, m) , 5.1-5.2 (1/3 x IH, m) , 6.00 (IH, d, J=9Hz) , 6.60 (1/3 x 2H, d, J=7Hz), 6.63 (2/3 x 2H, d, J=7Hz) , 6.80 (1/3 x 2H, d, J=7Hz) , 6.95 (2/3 x 2H, d, J=7Hz), 7.1-7.2 (5H, m) , 7.45 (IH, d, J=7Hz) Preparation 51 The following object compounds were obtained according to a similar manner to that of Preparation 3, 4 or 8. (1) MASS (m/z) : 452 (M+H) + NMR (CDC1 3 , δ) : 2.28 (3H, s) , 2.30-2.65 (5H, m) , 2.81 (2/3 x 3H, s) , 2.85-2.98 (IH, m) , 2.89 (1/3 x 3H, s) , 3.30-3.88 (5H, m) , 4.44 (1/3 x 2H, ABq, Δ=0.22, J=17Hz), 4.60 (2/3 x 2H, ABq, Δ=0.14, J=15Hz) , 5.78-5.92 (IH, m) , 6.90-7.47 (10H, m) , 8.60-8.78 (IH, m) (2) MASS (m/z) : 509 (M+H) + NMR (CDC1 3 , δ) : 2.20-2.48 (5H, m) , 2.31 (3H, s) , 2.63 (3/5 x 3H, s), 2.70-2.88 (IH, m) , 2.82 (2/5 x 3H, s), 2.90-3.15 (2H, m) , 2.92 (2/5 x 6H, s) , 2.94 (3/5 x 6H, s), 3.35-3.76 (5H, m) , 4.23 (2/5 x 2K, ABq, Δ=0.21, J=17Hz), 4.28 (3/5 x IH, d, J=15Hz) , 4.54 (3/5 x IH, d, J=15Hz) , 5.06-5.32 (IH, m) , 6.45-7.33 (9H, m) , 8.02-8.20 (IH, m) (3) MASS (m/z) : 523 (M+H) + NMR (CDC1 3 , δ) : 2.22 (2/5 x 6H, s), 2.24 (3/5 x 6H, s), 2.25-2.52 (5H, m) , 2.30 (3H, s), 2.66(3/5 x 3H, s), 2.70-2.90 (IH, m) , 2.88 (2/5 x 3H, s), 2.90- 3.18 (2H, m) , 3.33-3.75 (7H, m) , 4.32 (3/5 x IH, d, J=15Hz), 4.33 (2/5 x 2H, s) , 4.66 (3/5 x IH, d, J=15Hz), 5.10-5.23 (IH, ) , 6.90-7.32 (9H, m) , 8.02-8.20 (IH, m) (4) MASS (m/z) : 478 (M+H) + NMR (CDC1 3 , δ) : 2.30 (3H, s) , 2.30-2.87 (7H, m) , 2.95-3.30 (3H, ) , 3.38-3.85 (7H, m) , 4.04 (1/2 x IH, d, J=17Hz), 4.53 (1/2 x IH, d, J=17Hz) , 4.67 (1/2 x 2H, ABq, J=17Hz) , 5.14-5-.28 (IH, m) , 6.82-7.25 (9H, ) , 8.10-8.22 (IH, m) (5) MASS (m/z) : 500 (M+H) + NMR (CDC1 3 , δ) : 2.30 (3H, s) , 2.30-2.57 (5H, m) , 2.68 (3/4 x 3H, s), 2.70-2.88 (IH, m) , 2.82 (1/4 x 3H, s), 2.90-3.18 (2H, m) , 3.35-3.75 (5H, m) , 4.25 (3/4 x IH, d, J=15Hz), 4.30 (1/4 x 2H, ABq, Δ=0.05, J=17Hz), 4.64 (3/4 x IH, d, J=15Hz) , 5.05-5.22 (IH, m) , 6.80-7.01 (2H, m) , 7.10-7.30 (7H, m) , 8.05-8.20 (IH, m) (6) MASS (m/z) : 544, 546 (M+H) + NMR (CDC1 3 , δ) : 2.30 (3H, s), 2.30-2.57 (5H, m) , 2.67 (3/4 x 3H, s), 2.70-2.88 (IH, m) , 2.82 (1/4 x 3H, s), 2.90-3.18 (2H, ) , 3.35-3.75 (5H, m) , 4.23 (3/4 x IH, d, J=15Hz), 4.29 (1/4 x 2H, ABq, Δ=0.06, J=17Hz), 4.62 (3/4 x IH, d, J=15Hz) , 5.05-5.21 (IH, m), 6.74-6.95 (2H, m) , 7.11-7.42 (7H, ) , 8.05-8.20 (IH, m) (7) MASS (m/z) : 484 (M+H) + NMR (CDC1 3 , δ) : 2.30 (3H, s ) , 2.3-2.55 (5H, ) , 2.68 (3/4 x 3H, s), 2.72-2.88 (IH, m) , 2.83 (1/4 x 3H, s), 2.90-3.18 (2H, m) , 3.35-3.75 (5H, m) , 4.27 (3/4 x IH, d, J=15Hz), 4.30 (1/4 x 2H, s), 4.62 (3/4 x IH, d, J=15Hz), 5.10-5.22 (IH, m) , 6.83-7.08 (4H, m) , 7.13-7.32 (5H, ) , 8.05-8.20 (IH, m) (8) MASS (m/z) : 497 (M+H) + NMR (CDC1 3 , δ) : 2.30 (3H, s) , 2.30-2.55 (4H, m) , 2.65 (3/4 x 3H, s), 2.75-2.88 (IH, m) , 2.78 (1/4 x 3H, s), 2.93-3.15 (2H, m) , 3.35-3.75 (6H, m) , 3.90 (1/4 x 3H, s), 3.92 (3/4 x 3H, s) , 4.20 (1/4 x 2H, ABq, J=17Hz), 4.24 (3/4 x IH, d, J=15Hz) , 4.55 (3/4 x IH, d, J=15Hz) , 5.05-5.25 (IH, m) , 6.58-6.70 (IH, m) , 7.02-7.35 (6H, m) , 7.80-8.20 (2H, m) (9) MASS (m/z) : 480 (M+H) + NMR (CDC1 3 , δ) : 0.99 (3/5 x 3H, t, J=7Hz) , 1.04 (2/5 x 3H, t, J=7Hz), 2.20-2.50 (5H, m) , 2.28 (3H, s) , 2.68-2.88 (IH, m) , 2.90-3.30 (4H, m) , 3.32-3.75 (5H, m) , 4.23 (3/5 x IH, d, J=15Hz), 4.33 (2/5 x 2H, ABq, Δ=0.05, J=17Hz) , 4.83 (3/5 x IH, d, J=15Hz), 5.00-5.22 (IH, m) , 6.92-7.40 (10H, m) , 8.00-8.20 (IH, m) (10) MASS (m/z) : 501 (M+H) + NMR (CDC1 3 , δ) : 2.30-2.60 (5H, m) , 2.31 (3H, s) , 2.68 (4/5 x 3H, s) , 2.72-2.88 (IH, m) , 2.78 (1/5 x 3H, s), 2.92-3.24 (2H, m) , 3.37-3.75 (5H, m) , 4.28 (4/5 x IH, d, J=15Hz) , 4.29 (1/5 x 2H, s), 4.60 (4/5 x IH, d, J=15Hz), 5.05-5.20 (IH, ) , 7.00-7.37 (9H, m) , 8.02-8.22 (2H, m) (11) MASS (m/z) : 481 (M+H) + NMR (CDC1 3 , δ) : 2.31 (3H, s) , 2.31-2.50 (5H, m) , 2.51 (1/4 x 3H, s), 2.54 (3/4 x 3H, s) , 2.66 (3/4 x 3H, s), 2.72-2.88 (IH, m) , 2.80 (1/4 x 3H, s) , 2.93- 3.20 (2H, m) , 3.38-3.76 (5H, m) , 4.28 (1/4 x 2H, ABq, Δ=0.14, J=17Hz) , 4.31 (3/4 x IH, d, J=15Hz) , 4.59 (3/4 x IH, d, J=15Hz) , 5.06-5.24 (IH, m) , 6.98-7.32 (7H, m) , 8.08-8.33 (2H, m) (12) MASS (m/z) : 468 <M+H) + NMR (CDC1 3 , δ) : 2.38-2.59 (IH, ) , 2.51 (1/4 x 3H, s), 2.53 (3/4 x 3H, s) , 2.65 (3/4 x 3H, s), 2.69- 2.86 (IH, m), 2.79 (1/4 x 3H, s) , 2.92-3.18 (2H, m) , 3.32-3.76 (9H, m) , 4.27 (1/4 x 2H, ABq, Δ=0.16, J=17Hz), 4.32 (3/4 x IH, d, J-15Hz) , 4.57 (3/4 x IH, d, J=15Hz), 5.03-5.22 (IH, m) , 6.98-7.33 (7H, ) , 8.05-8.34 (2H, m) (13) MASS (m/z) : 533 (M+H) + NMR (CDC1 3 , δ) : 2.27-2.58 (5H, ) , 2.30 (3H, s) , 2.70-2.88 (IH, ) , 2.72 (2/3 x 3H, s), 2.85 (1/3 x 3H, s), 2.92-3.21 (2H, m) , 3.33-3.78 (5H, ) , 4.38 (1/3 x 2H, s), 4.41 (2/3 x IH, d, J=15Hz) , 4.67 (2/3 x IH, d, J=15Hz), 5.08-5.24 (IH, m) , 7.00-7.36 (7H, ) , 7.50-7.64 (2H, m) , 8.10 (IH, s) , 8.10-8.22 (IH, m) , 8.52 (IH, s) (14) MASS (m/z) : 501 (M+H) + NMR (CDC1 3 , δ) : 2.31 (3H, s) , 2.31-2.62 (5H, m) , 2.68 (4/5 x 3H, s), 2.71-2.88 (IH, m) , 2.82 (1/5 x 3H, s), 2.95-3.20 (2H, m) , 3.35-3.78 (5H, m) , 4.30 (4/5 x IH, d, J=15Hz), 4.32 (1/5 x 2H, ABq, Δ=0.05, J=17Hz), 4.62 (4/5 x IH, d, J=15Hz), 5.03-5.20 (IH, m) , 7.10-7.32 (5H, m) , 7.48 (IH, s) , 8.08-8.31 (2H, m) , 8.40-8.52 (IH, m) (15) MASS (m/z) : 488 (M+H) + NMR (CDC1 3 , δ) : 2.33-2.62 (IH, m) , 2.68 (4/5 x 3H, s), 2.71-2.85 (IH, m) , 2.79 (1/5 x 3H, s) , 2.90- 3.22 (2H, m) , 3.34-3.77 (9H, m) , 4.28 (1/5 x 2H, ABq, Δ=0.05, J=17Hz) , 4.29 (4/5 x IH, d, J=15Hz) , 4.58 (4/5 x IH, d, J=15Hz) , 5.02-5.18 (IH, m) , 7.00-7.38 (7H, m) , 8.00-8.21 (2H, m) (16) MASS (m/z) : 454 (M+H) + NMR (CDC1 3 , δ) : 2.38-2.61 (IH, ) , 2.67 (3/4 x 3H, s), 2.67-2.85 (IH, ) , 2.82 (1/4 x 3H, s) , 2.92- 3.20 (2H, ) , 3.35-3.76 (9H, ) , 4.32 (1/4 x 2H, ABq, Δ=0.10, J=17Hz), 4.32 (3/4 x IH, d, J=15Hz) , 4.64 (3/4 x IH, d, J=15Hz) , 5.07-5.21 (IH, m) , 7.05-7.43 (7H, m) , 8.06-8.22 (IH, m) , 8.29 (1/4 x IH, s), 8.40 (3/4 x IH, s) , 8.46-8.56 (IH, m) (17) MASS (m/z) : 467 (M+H) + NMR (CDC1 3 , δ) : 2.31 (3H, s) , 2.31-2.58 (5H, m) , 2.67 (3/4 x 3H, s) , 2.70-2.86 (IH, ) , 2.82 (1/4 x 3H, s), 2.94-3.20 (2H, m) , 3.38-3.75 (5H, ) , 4.32 (3/4 x IH, d, J=15Hz) , 4.34 (1/4 x 2H, ABq, J=17Hz), 4.65 (3/4 x IH, d, J=15Hz) , 5.08-5.20 (IH, m) , 7.11-7.42 (7H, m) , 8.07-8.22 (IH, m) , 8.28 (1/4 x IH, s) , 8.41 (3/4 x IH, s) , 8.48-8.56 (IH, m) (18) MASS (m/z) : 480 (M+H) + NMR (CDC1 3 , δ) : 1.09 (3H, t, J=7Hz) , 2.22-2.52 (7H, m), 2.67 (2/3 x 3H, s), 2.69-2.92 (IH, m) , 2.87 (1/3 x 3H, s), 2.92-3.15 (2H, m) , 3.34-3.78 (5H, m) , 4.33 (2/3 x IH, d, J=15Hz) , 4.38 (1/3 x 2H, ABq, Δ=0.07, J=17Hz), 4.68 (2/3 x IK, d, J=15Hz), 5.09-5.23 (IH, m) , 6.92-7.32 (10H, m) , 8.02-8.22 (IH, m) (19) NMR (CDC1 3 , δ) : 2.30 (3H, s) , 2.37 (4H, m) , 2.44 (IK, dd, J=7, 16Hz), 2.65 (3H x 2/3, s) , 2.72-2.85 (IH, m) , 2.83 (3H x 1/3, s), 2.94-3.12 (2H, m) , 3.43 (2H, m) , 3.57-3.74 (3H, m) , 3.79 (3H, s) , 4.20 (IH x 1/3, d, J=15Hz), 4.26 (IH x 2/3, d, J=15Hz) , 4.33 (IH x 1/3, d, J=15Hz), 4.61 (IH x 2/3, d, J=15Hz) , 5.11-5.24 (IH, m) , 6.77-7.28 (9H, m) , 8.08 (IH x 1/3, d, J=8Hz), 8.15 (IH x 2/3, d, J=8Hz) (20) MASS (ESI) (m/z) : 480 (M+H) NMR (CDC1 3 , δ) : 2.29 (3H, s) , 2.30 (3H, s) , 2.23-2.48 (6H, m) , 2.63 (3 x 2/3H, s), 2.70-2.80 (IH, m) , 2.84 (3 x 1/3H, s) , 2.89-3.13 (2H, ) , 3.38-3.47 (2H, m) , 3.50-3.72 (2H, m) , 4.23-4.31 (2 x 2/3H, m) , 4.62 (2 x 1/3H, d, J=15Hz) , 5.10-5.22 (IH, m) , 6.87 (2 x 1/3H, d, J=8Hz) , 6.94 (2 x 2/3H, d, J=8Hz), 7.07 (2H, d, J=8Hz) , 7.12-7.29 (5H, m) , 8.08 (1 x 1/3H, d, J=8Hz), 8.15 (1 x 2/3H, d, J=8Hz) (21) NMR (CDC1 3 , δ) : 2.29 (3K, s), 2.36 (4H, m) , 2.66-2.77 (IH, m) , 2.87-3.09 (IH, m) , 2.95 (3H x 1/3, s) , 3.02 (3H x 2/3, s) , 3.42-3.69 (5H, m) , 3.76-3.93 (3H, m) , 4.57 (IH x 2/3, d, J=15Hz) , 4.66 (2H x 1/3, s), 4.67 (IH x 2/3, d, J=15Hz) , 5.03 (IH, m) , 7.16-7.36 (5H, ) , 8.42 (IH x 1/3, d, J=8Hz) , 8.50 (IH x 2/3, d, J=8Hz) (22) NMR (CDCl 3 , δ) : 0.81 (3H x 1/3, d, J=7Hz) , 0.84 (3H x 1/3, d, J=7Hz), 0.94 (3H x 2/3, d, J=7Hz) , 0.98 (3H x 2/3, d, J=7Hz), 1.42-1.72 (3H, m) , 2.29 (3H, s), 2.33-2.42 (4H, m) , 2.51-2.62 (IH, m) , 2.86-2.97 (IH, m), 2.93 (3H x 1/3, s) , 3.01 (3H x 2/3, s) , 3.46-3.77 (5H, m) , 4.43 (IH x 2/3, d, J=15Hz) , 4.61 (IH x 1/3, d, J=16Hz), 4.73 (IH x 1/3, d, J=16Hz) , 4.74 (IH x 2/3, d, J=15Hz) , 4.98 (IH, dt, J=4, 8Hz), 7.18-7.37 (5H, m) , 7.97 (IH x 1/3, d, J=8Hz) , 8.04 (IH x 2/3, d, J=8Hz) (23) NMR (CDC1 3 , δ) : 2.30 (3H, s) , 2.35-2.44 (4H, m) , 2.52 (IH, dd, J=8, 16Hz), 2.71 (3H x 2/3, s), 2.77 (IH, dd, J=3, 16Hz), 2.85 (3H x 1/3, s) , 2.93-3.17 (2H, ) , 3.41-3.47 (2H, m) , 3.54-3.74 (3H, m) , 4.35 (IH x 1/3, d, J=15Hz), 4.37 (IH x 2/3, d, J=15Hz) , 4.50 (IH x 1/3, d, J=l5Hz), 4.72 (IH x 2/3, d, J=15Hz) , 5.07 (IH x 1/3, q, J=7Hz) , 5.18 (IH x 2/3, q, J=7Hz), 7.01 (IH x 2/3, d, J=8Hz) , 7.13 (2H, d, J=8Hz), 7.20-7.25 (3 x 1/3H, ) , 7.50 (2H, t, J=8Hz) (24) NMR (CDC1 3 , δ) : 2.30 (3H, s) , 2.36 (4H, m) , 2.50 (IH, dd, J=7, 16Hz), 2.67 (3H x 3/5, s) , 2.81 (IH x 2/5, dd, J*4, 16Hz), 2.88 (3H x 2/5, s) , 2.90 (IH x 3/5, dd, J=4, 16Hz), 2.97-3.12 (2H, ) , 3.39-3.46 (2H, ), 3.56-3.77 (3H, ) , 4.32 (IH x 3/5, d, J=15Hz) , 4.32 (IH x 2/5, d, J=15Hz) , 4.44 (IH x 2/5, d, J=15Hz), 4.70 (IH x 3/5, d, J=15Hz) , 5.15 (IH, m) , 7.00-7.28 (10H, ) , 8.02 (IH x 2/5, d, J=8Hz) , 8.13 (IH x 3/5, d, J=8Hz) (25) NMR (CDC1 3 , δ) : 2.29 (3H, s), 2.25-2.50 (5H, m) , 2.66 (3H x 2/3, s), 2.73 (IH x 1/3, dd, J=3, 16Hz) , 2.82 (IH x 2/3, dd, J=3, 16Hz), 2.87 (3H x 1/3, s) , 2.92-3.13 (2H, ) , 3.38-3.47 (2H, ) , 3.54-3.73 (3H, m), 4.33 (IH x 2/3, d, J=15Hz) , 4.34 (IH x 1/3, d, J=15Hz), 4.41 (IH x 1/3, d, J=15Hz) , 4.67 (IH x 2/3, d, J=15Hz), 5.17 (IH, m) , 6.97-7.15 (3H, m), 7.21 (3H, s), 7.22-7.27 (4H, m) , 8.06 (IH x 1/3, d, J=7Hz), 8.16 (IH x 2/3, d, J=7Hz) (26) NMR (CDCL 3 , δ) : 2.30 (3H, s) , 2.36 (4H, m) , 2.50 (IH, dd, J=7, 16Hz), 2.67 (3H x 3/5, s) , 2.81 (IH x 2/5, dd, J=4, 16Hz), 2.88 (3H x 2/5, s) , 2.90 (IH x 3/5, dd ' J=4, 16Hz), 2.97-3.12 (2H, m) , 3.39-3.46 (2H, m), 3.56-3.77 (3H, m) , 4.32 (IH x 3/5, J=15Hz) , 4.32 (IH x 2/5, J=15Hz) , 4.44 (IH x 2/5, J=15Hz) , 4.70 (IH x 3/5, J=15Hz), 5.15 (IH, m) , 7.00-7.28 (10H, m), 8.02 (IH x 2/5, d, J=8Hz) , 8.13 (IH x 3/5, d, J=8Hz) (27) MASS (FAB) (m/z) : 538 (M+H) + NMR (CDC1 3 , δ) : 1.28 (3H, t, J=8Hz) , 2.25-2.33 (1 x 1/3H, m), 2.41-2.49 (1 x 2/3H, ) , 2.51-2.62 (4H, m >' 2 . 63 (3 x 2/3H, s) , 2.70-2.85 (IH, m) , 2.86 (3 x 1/3H, s), 2.92-3.13 (2H, m) , 3.23 (2H, s) , 3.42- 3.51 (2H, m), 3.57-3.77 (3H, ) , 4.19 (2H, q, J=8Hz), 4.31-4.42 (2 x 2/3H, m) , 4.68 (2 x 1/3H, d, J=15Hz), 5.11-5.20 (IH, ) , 6.98 (2 x 1/3H, d, J=8Hz), 7.05 (2 x 2/3H, d, J=8Hz) , 7.12-7.31 (8H, m), 8.07 (1 x 1/3H, d, J=8Hz) , 8.15 (1 x 2/3H, d, J=8Hz) (28) MASS : 524 (M+l) NMR (CDC1 3 , δ) : 2.29 (3H, s), 2.33-2.45 (4H, m) , 2.48-2.57 (IH, m) , 2.63 (3 x 2/3H, s) , 2.71-2.81 (IH, m), 2.83 (3 x 1/3H, s) , 2.92-3.14 (2H, m) , 3.39-3.47 (2H, ) , 3.52-3.73 (3H, m) , 3.88 (3H, s) , 4.33-4.49 (2 x 2/3H, m) , 4.72 (2 x 1/3H, d, J=15Hz), 5.07-5.22 (IH, ) , 6.98 (2 x 1/3H, d. J=8Hz), 7.08 (2 x 2/3H, d, J=8Hz), 7.13-7.30 (5H, m) , 7.92 (2H, t, J=8Hz), 8.10 (1 x 1/3H, d, J=8Hz) , 8.17 (1 x 2/3H, d, J=8Hz) (29) MASS (FAB) (m/z) : 596 (M+H) + NMR (CDC1 3 , δ) : 1.22 (3H, t, J=8Hz) , 2.33-2.42 (IH, m) , 2.48-2.62 (4H, ) , 2.63 (3 x 2/3H, s) , 2.69- 2.78 (IH, m) , 2.80 (3 x 1/3H, s), 2.92-3.13 (2H, m) , 3.20 (2H, s) , 3.42-3.51 (2H, ) , 3.57-3.72 (3H, m) , 3.90 (3H, s), 4.19 (2H, q, J=8Hz), 4.31-4.50 (2 x 2/3H, m) , 4.72 (2 x 1/3H, d, J=15Hz) , 5.07-5.12 (IH, m) , 6.98 (2 x 1/3H, d, J=8Hz) , 7.08 (2 x 2/3H, d, J=8Hz), 7.12-7.17 (IH, m) , 7.20-7.28 (4H, m) , 7.92 (2H, t, J=8Hz), 8.10 (1 x 1/3H, d, J=8Hz) , 8.17 (1 x 2/3H, d, J=8Hz) Preparation 52 To a solution of Starting compound (53.06 g) in dichloromethane (400 ml) were added N-methyl-N-(3- pyridylmethyl) amine (25.65 g) and 1-hydroxybenzotriazole (27.02 g) and the mixture was cooled with ice. l-Ethyl-3- (3- dimethylaminopropyl)carbodiimide hydrochloride (42.18 g) was added to the mixture in small portions, then the whole was stirred at room temperature for 8 hours. After the mixture was concentrated, IN sodium hydroxide (300 ml) was added thereto, and the mixture was extracted three times with ethyl acetate. The organic layer was washed once with brine and dried over magnesium sulfate. Evaporation of the solvent followed by silica gel column chromatography (chloroform- methanol) gave Object compound (81.37 g) as a colorless oil. MASS : m/z 370 (M+H) + NMR (CDC1 3 , δ) : 1.40 (1/5 x 9H, s) , 1.42 (4/5 x 9H, s), 2.63 (4/5 x 3H, s) , 2.79 (1/5 x 3H, s), 2.92- 3.06 (2H, m) , 4.08 (1/5 x IH, d, J=17Hz) , 4.35 (1/5 x IH, d, J=17Hz), 4.49 (4/5 x 2H, ABq, Δ=0.09, J=15Hz), 4.79-4.98 (IH, m) , 5.28-5.42 (IH, ) , 7.10-7.35 (7H, ) , 8.28 (1/5 x IH, s), 8.42 (4/5 x IH, s), 8.50-8.55 (IH, ) Preparation 53 Object compounds were obtained according to a similar manner to that of Preparation 1, 6, 11 or 52. (1) MASS : m/z 404 (M+H) + NMR (CDC1 3 , δ) : 1.42 (9H, s) , 2.63 (5/6 x 3H, s), 2.76 (1/6 x 3H, s), 2.88-3.09 (2H, m) , 4.04 (1/6 x IH, d, J=17Hz), 4.30 (1/6 x IH, d, J=17Hz), 4.44 (5/6 x 2H, ABq, J=15Hz) , 4.76-4.92 (IH, m) , 5.22-5.38 (IH, m) , 7.03-7.40 (7H, m) , 8.05 (1/6 x IH, d, J=2Hz), 8.18 (5/6 x IH, d, J=2Hz) (2) MASS : m/z 370 (M+H) + NMR (CDC1 3 , δ) : 1.39 (1/4 x 9H, s) , 1.42 (3/4 x 9H, s), 2.69 (3/4 x 3H, s), 2.82 (1/4 x 3H, s), 2.90- 3.12 (2H, m) , 4.28 (1/4 x 2H, s) , 4.48 (3/4 x 2H, ABq, J=15Hz), 4.68-4.98 (IH, m) , 5.20-5.40 (IH, m) , 6.73-7.35 (7H, m) , 8.40-8.52 (2H, ) Preparation 54 Trifluoroacetic acid (150 ml) was slowly added to ice- cooled Starting compound (72.82 g) , and the mixture was stirred at room temperature for 2.5 hours. The trifluoroacetic acid was evaporated and the residue was cooled with ice. 15" Aqueous sodium hydroxide (about 400 ml) was added to the residue, and the mixture was extracted three times with chloroform. The organic layer was dried over magnesium sulfate. Evaporation of the solvent gave Object compound (62.01 g) as a colorless oil. MASS : m/z 270 (M+H) + NMR (CDCI3, δ) : 2.71 (3/4 x 3H, s) , 2.76-3.10 (2H, m) , 2.88 (1/4 x 3H, s), 3.82-4.02 (IH, m) , 4.28 (1/4 x 2H, ABq, Δ=0.20, J=17HZ) , 4.55 (3/4 x 2H, ABq, Δ=0.21, J=15Hz), 7.11-7.55 (7H, m) , 8.32-8.58 (2H, m) Preparation 55 Object compound was obtained according to a similar manner to that of Preparation 3, 4, 8, 41 or 54. MASS : m/z 303 (M+H) + NMR (CDC1 3 , δ) : 2.49 (5/6 x 3H, s), 2.72 (1/6 x 3H, s), 2.98-3.23 (2H, m) , 3.70 (1/6 x IH, d, J=17Hz) , 4.23 (1/6 x IH, d, J=17HZ), 4.40 (IH, t, J=7Hz) , 4.42 (5/6 x 2H, ABq, Δ=0.07, J=15Hz) , 7.08-7.52 (7H, ), 8.06 (1/6 x IH, d, J=2Hz) , 8.20 (5/6 x IH, d, J=2Hz) Preparation 56 To a stirred solution of (2S)-3- (2-pyridyl)-2-(tert- butoxycarbonylamino)propionic acid (1.19 g) and Starting Compound (1.20 g) in N,N-dimethylformamide (3 ml) was added dropwise diphenylphosphoryl azide (1.25 g) followed by triethylamine (1.36 ml) at 0 β C. The mixture was stirred at room temperature for 3 hours. The reaction mixture was diluted with water and extracted with chloroform. The extract was dried and evaporated. The residue was purified by column chromatography on silica gel in chloroform - 2% methanol-chloroform. Recrystallization from ethyl acetate - n-hexane gave Object Compound (1.69 g) . MASS : m/z 518 (M + +l) NMR (CDC1 3 , δ) : 1.44 (9H, s) , 2.52 (3H x 3/4, s) , 2.74 (3H x 1/4, s) , 2.80 (2H x 3/4, d, J=7Hz) , 2.93 (2H x 1/4, m) , 3.19 (IH, m) , 3.35 (IH, m) , 4.08 (IH X 1/4, d, J=16Hz), 4.21 (IH x 1/4, d, J=16Hz) , 4.27 (IH x 3/4, d, J=15Hz), 4.56 (IH x 3/4, d, J=15Hz) , 4.57 (IH, m) , 5.06 (IH, q, J=7Hz) , 6.43 (IH, m) , 7.05-7.35 (9H, m) , 7.60 (2H, m) , 8.21 (IH x 1/4, d, J=2Hz), 8.35 (IH x 3/4, d, J=2Hz) , 8.51 (2H, m) Preparation 57 Object compounds were obtained according to a similar manners to that of Preparation 1, 6, 11, 38, 52 or 56. (1) MASS : m/z 555 (M + +l) NMR (CDC1 3 , δ) : 1.42 (9H, s), 2.47 (3H x 2/3, s), 2.75 (3H x 1/3, s) , 2.85 (2H, m) , 3.12-3.32 (2H, m) , 4.11 (IH x 1/3, d, J=16Hz) , 4.18 (IH x 1/3, d, J=16Hz), 4.22 (IH x 2/3, d, J=15Hz) , 4.52 (IH x 2/3, d, J=15Hz), 5.02 (IH, m) , 5.13 (IH, m) , 6.68 (IH, t, J=8Hz), 6.87-7.35 (15H, m) , 7.62 (IH, m) , 8.13 (IH x 2/3, s), 8.16 (IH x 1/3, s) (2) MASS : m/z 506 (M + +l) NMR (CDC1 3 , δ) : 1.43 (9H, s), 2.63 (3H x 2/3, s) , 2.83 (3H x 1/3, s), 2.91-3.02 (3H, m) , 3.12 (IH, m) , 4.16 (IH x 1/3, d, J=16Hz), 4.34-4.54 (2 x 2/3H, m) , 5.05 (IH, m) , 6.81 (IH, s), 6.99-7.13 (4H, m) , 7.21-7.28 (7H, m) , 7.47 (IH, d, J=8Hz) (3) MASS : m/z 552 (M + ) NMR (CDC1 3 , δ) : 1.44 (9H, s), 2.53 (3H x 2/3, s) , 2.71 (3H x 1/3, s), 2.79 (2H, d, J=8Hz) , 3.19 (IH, m) , 3.33 (IH, ) , 4.23 (IH x 2/3, d, J=15Hz) , 4.26 (IH x 1/3, d, J=16Hz), 4.48 (IH x 1/3, d, J=16Hz) , 4.51 (IH x 2/3, d, J=15Hz) , 4.57 (IH, m) , 5.05 (IH, m) , 6.43 (IH, m) , 7.06-7.25 (10H, m) , 7.60 (IH, m) , 8.12 (IH, m) , 8.51 (IH, m) (4) MASS : m/z 518 (M + +l) NMR (CDC1 3 , δ) : 1.45 (9H, s) , 2.62 (3H x 3/4, s) . 16981 - 433 - 2.77 (3H x 1/4, s), 2.82-2.98 (2H, m) , 3.12-3.33 (2H, ) , 4.02-4.54 (3K, m) , 4.93 (IH x 1/4, ) , 5.12 (IH x 3/4, ) , 6.63-6.68 (2H x 1/4, ) , 6.82-6.84 (2H x 3/4, m) , 7.06-7.24 (7H, m) , 7.54-7.62 (2H, m) , 8.37-8.52 (3H, ) (5) MASS : m/z 517 (M + +l) NMR (CDC1 3 , δ) : 1.44 (9H, s) , 2.49 (3H x 3/4, s) , 2.76 (3H x 1/4, s), 2.72-2.95 (2K, m) , 3.08-3.37 (2H, m) , 4.17 (IH x 1/4, d, J=15Hz) , 4.30 (IH x 3/4, d, J=15Hz), 4.34 (IK x 1/4, d, J=15Hz), 4.53 (IH x 3/4, d, J=15Hz), 4.57 (IH, m) , 5.08 (IH, m) , 6.84-7.26 (13H, m) , 7.53-7.62 (2H, m) , 8.49-8.52 (IK, ) Preparation 58 Object compounds were obtained according to a similar manner to that of Preparation 3, 4, 8, 41 cr 54. (1) NMR (CDCI3, δ) : 2.77 (3H x 3/4, s) , 2.86 (3H x 1/4, s), 2.67-3.08 (3K, m) , 3.17-3.35 (IH, m) , 3.74-3.8c (IH, m) , 4.32 (IH x 3/4, d, J=15Hz), 4.37 (IH x 1/4, d, J=15Hz), 4.58 (IK x 1/4, d, J=15Hz), 4.62 (IH x 3/4, d, J=15Hz), 4.97-5.06 (IH x 1/4, ) , 5.15-5.25 (IH x 3/4, m) , 6.75-6.79 (2H x 1/4, m) , 6.87-6.89 (2H x 3/4, m) , 7.14-7.27 (7H, ) , 7.56- 7.64 (IH, ) , 8.08-8.23 (IH, mi, 8.44-8.52 (3H, ) (2) NMR (CDCI3, δ) : 2.67 (3H x 2/3, s), 2.85 (3H x 1/3, s), 2.88-3.07 (3K, m) , 3.1 *7 -3.31 (IE, ) , 3.72-3.87 (IH, m) , 4.32 (IH x 2/3, d, J=15Hz), 4.33 (IH x 1/3, d, J=15Hz), 4.63 (IH x 1/3, d, J=15Hz), 4.65 (IH x 2/3, d, J=15Hz), 6.96-7.29 (12H, m) , 7.55- 7.63 (IH, m) , 8.17-8.28 (IK, m) , 8.48-8.52 (IH, m) - 434 - (3) NMR (CDC1 3 , δ) : 2.67 (3H x 2/3, s), 2.75 (3H x 1/3, s), 2.92 (3H, πt) , 3.18-3.31 (IH, m) , 3.74 (IH, m) , 4.23 (IH x 1/3, d, J=16Hz), 4.25 (IH x 2/3, d, J=15Hz), 4.53 (IH x 1/3, d, J=16Hz), 4.56 (IH x 2/3, d, J=15Hz), 7.10-7.30 (10H, m) , 7.56 (IH, m) , 8.00-8.20 (2H, m) , 8.49 (IH, ) (4) NMR (CDCI3, δ) : 2.72 (3H x 2/3, s), 2.79-3.06 (4H, m) , 2.8" (3H x 1/3, s) , 3.49 (IH x 1/3, dd, J=4, 7Hz), 3.58 (IH x 2/3, t, J=6Hz) , 4.32 (IH x 1/3, d, J=16Hz) , 4.37 (IH, x 2/3, d, J=15Hz) , 4.44 (IH x 1/3, d, J=16H∑) , 4.65 (IH x 2/3, d, J=15Hz) , 5.15 (IH, q, J=7Hz), 6.78 (IH, d, J=10Hz) , 7.01-7.28 (10H, ) , 7.47 (IH, d, J=2Hz), 8.03 (IH x 1/3, d, J=8Hz), 8.07 (IH x 2/3, d, J=8Hz) (5) NMR (CDCI3, δ) : 2.71 (3H x 2/3, s), 2.86 (3H x 1/3, s), 2.85-3.04 (3K, ) , 3.23 (IH x 1/3, dd, J=3, 15Hz) , 3.30 (IH x 2/3, dd, J=3, 15Hz), 3.61 (IH x 1/3, dd, J=4, 15Hz), 3.69 (IH x 2/3, dd, J=4, 15Hz) , 4.29 (IK x 2/3, d, J=15Hz) , 4.41 (2H x 1/3, s), 4.68 (IH x 2/3, d, J=15Hz), 5.21 (IH, ) , 6.96- 7.37 (14H, ir.) , 7.57 (IH, ) , 7.94-8.16 (2H, m) (6) NMR (CDCI3, δ) : 2.69 (3H x 3/4, s), 2.82 (3H x 1/4, s) , 2.85-3.03 (3K, rc.) , 3.16-3.30 (IH, ) , 3.69 (IK x 1/4, dd, J=3, 7Hz) , 3.77 (IH x 3/4, dd, J=3, 7Hz) , 4.30 (IH x 1/4, d, J=16Hz), 4.32 (IH x 3/4, d, J=15Hz) , 4.38 (IH x 1/4, d, J=16H∑) , 4.65 (IH x 3/4, d, J=15Hz), 5.15 (IH, m) , 7.14-7.27 (8H, ) , 7.37 (IH, rc.) , 7.61 (IH, m) , 8.21-8.53 (4H, ) Preparation 59 The following object compound was obtained according to a similar manner to that of Preparation 1, 6, 11, 38, 52 or - 435 - 58. MASS : 486 (M+l) NMR (CDC1 3 , δ) : 1.43 (9H, s) , 2.09 (3 x 1/3H, s), 2.11 (3 x 2/3H, s), 2.57 (3 x 2/3H, s), 2.82 (3 x 1/3H, s), 2.79-2.88 (2H, m) , 2.99-3.04 (2H, m) , 4.08 (2 x 1/6H, d, J=16Hz) , 4.31 (2 x 1/6H, d, J=16Hz), 4.39 (2 x 1/3H, d, J=15Hz) , 4.59 (2 x 1/3H, d, J=15Hz), 4.20-4.32 (IH, ) , 5.11-5.20 (IH, m) , 5.22-5.37 (IH, m) , 6.93-7.32 (11H, m) Preparation 60 The following object compounds were obtained according to a similar manner to that of Preparation 1, 6, 11, 38, 52 or 56. (1) MASS : 491 (M+l) NMR (CDC1 3 , δ) : 1.43 (9H, s) , 2.69 (3 x 4/5H, s), 2.77 (3 x 1/5H, s), 2.92-3.13 (2H, m) , 3.35 (IH, t, J=8Hz), 3.57-3.63 (IH, m) , 3.90-4.03 (IH, m) , 4.12- 4.25 (IH, ) , 4.35 (2 x 1/lOH, d, J=16Hz) , 4.40 (2 x 1/10H, d, J=16Hz), 4.39 (2 x 2/5H, d, J=15Hz) , 4.50 (2 x 2/5H, d, J=15Hz), 5.10 (IH, q, J=8Hz) , 5.43 (IH, d, J=8Hz), 7.09-7.19 (2H, m) , 7.20-7.32 (5H, m), 7.39 (IH, d, J=8Hz) , 8.10 (1 x 1/5H, s) , 8.19 (1 x 4/5H, s) (2) MASS : 714 (M+l) NMR (CDC1 3 , δ) : 1.42 (9H, s), 1.48-1.53 (IH, m) , 1.54 (3 x 2/3H, s), 2.64-2.73 (IH, m) , 2.77 (3 x 1/3H, s), 2.89-3.03 (2H, ) , 3.85-3.95 (IH, m) , 4.17-4.34 (2 x 2/3H, m) , 4.54 (2 x 1/3H, d, J=15Hz) , 4.67- 4.77 (IH, m) , 5.04-5.13 (IH, m) , 6.72-7.31 (20H, m), 7.39-7.43 (6H, ) (3) MASS : 507 (M+l) NMR (CDC1 3 , δ) : 1.45 (9H, s), 2.73 (3 x 3/4H, s) , 2.88 (3 x 1/4H, s), 2.93-3.12 (2H, m) , 3.24-3.33 (IH, m) , 3.52-3.64 (IH, m) , 3.92-4.08 (IH, m) , 4.13-4.24 (IH, m) , 4.60 (2 x 1/2H, d, J=15Hz), 4.78 (2 x 1/2H, d, J=15Hz), 5.10-5.20 (IH, m) , 5.38-5.47 (IH, m) , 7.10-7.20 (6H, m) , 7.58 (IH, t, J=8Hz) , 7.71 (IH, t, J=8Hz), 7.80 (IH, d, J=8Hz), 7.82 (1 x 1/4H, s), 7.92 (1 x 3/4H, s) , 8.10 (IH, dd, J=8, 2Hz), 8.70 (1 x 1/4H, d, J=2Hz) , 8.76 (1 x 3/4H, d, J=2Hz) (4) MASS (m/z) : 516 (M + +l) NMR (CDC1 3 , δ) : 2.52 (3H x 2/3, s) , 2.79 (3H x 1/3, s), 2.97 (2H, m) , 3.04 (2H, m) , 4.02 (IH x 1/3, d, J=15Hz), 4.25 (IH x 1/3, d, J=15Hz) , 4.34 (IH x 2/3, d, J=15Hz), 4.37 (IH, m) , 4.54 (IH x 2/3, d, J=15Hz), 4.92 (IH, m) , 5.11 (IH, m) , 6.68 (IH x 1/3, d, J=8Hz), 6.79 (IH x 2/3, d, J=8Hz) , 6.91 (IH, m) , 7.04-7.30 (14H, m) (5) MASS (m/z) : 457 (M + +l) NMR (CDC1 3 , δ) : 1.46 (9H, s) , 2.75 (3H x 3/4, s) , 2.86 (3H x 1/4, s) , 2.91-3.12 (2H, m) , 3.57-3.65 (IH, m) , 3.97 (IH, m) , 4.20 (IH, m) , 4.28 (IH x 1/4, d, J=15Hz), 4.33 (IH x 1/4, d, J=15Hz) , 4.44 (IH x 3/4, d, J=15Hz), 4.54 (IH x 3/4, d, J=15Hz) , 4.98-5.07 (IH x 1/4, m) , 5.13-5.21 (IH x 3/4, m) , 5.46 (IH, t, J=7Hz), 6.88 (IH x 1/4, d, J=7Hz) , 6.94 (IH x 3/4, d, J=7Hz) , 7.10-7.28 (5H, m) , 8.49 (2H, d, J=7Hz) (6) MASS (m/z) : 457 (M + +l) NMR (CDC1 3 , δ) : 1.46 (9H, s) , 2.70 (3H x 3/4, s) , 2.82 (3H x 1/4, s), 3.02 (2H, m) , 3.38 (IH, m) , 3.61 (IH, m) , 3.97 (IH, m) , 4.07 (IH x 1/4, d, J=15Hz), 4.21 (IH, m) , 4.42 (lH x 1/4, d, J=15Hz) , 4.44 (IH x 3/4, d, J=15Hz) , 4.57 (IH x 3/4, d, J=15Hz), 5.12 (IH, m) , 5.44 (IH, m) , 7.13-7.29 (7H, m) , 7.44 (IH, m) , 8.34 (IH x 1/4, d, J=2Hz) , 8.42 (IH x 3/4, d, J=2Hz), 8.53 (IH, dd, J=2, 6Hz) (7) MASS (m/z) : 546 (M + +l) NMR (CDC1 3 , δ) : 1.44 (9H, s) , 2.60 (3H x 2/3, s) , 2.82 (3H x 1/3, s) , 2.91-3.07 (2H, ) , 3.58 (IH, dd, J=7, 16Hz), 3.89 (IH, m) , 4.11-4.37 (2H, m) , 4.48-4.61 (2H, m) , 5.15 (IH, q, J=7Hz) , 5.33 (IH, m) , 6.94 (IH, m) , 7.07-7.34 (16H, m) (8) MASS (m/z) : 482 (M + +l) NMR (CDC1 3 , δ) : 0.96 (6H, m) , 1.45 (9H, s) , 1.55-1.71 (3H, m) , 2.60 (3H x 2/3, s) , 2.83 (3H x 1/3, s), 2.98-3.03 (2H, ) , 4.09 (lH x 1/3, d, J=15Hz) , 4.31 (IH x 1/3, d, J=15Hz), 4.39 (IH x 2/3, d, J=15Hz) , 4.56 (IH x 2/3, d, J=15Hz) , 4.82 (IH, m) , 5.15 (IH, m) , 6.82-6.96 (2H, m) , 7.07-7.28 (10H, m) (9) MASS (m/z) : 547 (M + +l) NMR (CDC1 3 , δ) : 1.45 (9H, s) , 2.85 (3H x 1/3, s) , 2.93 (3H x 2/3, s) , 3.08 (IH, m) , 3.26 (IH, m) , 3.56 (IH, m) , 3.87 (IH, m) , 4.26-4.32 (2H, m) , 4.46-4.67 (3H, m) , 4.75 (IH, m) , 5.38 (2H, m) , 6.87-7.16 (4H, m) , 7.24-7.53 (9H, m) , 8.47 (IH, m) (10) MASS (m/z) : 500 (M+H) NMR (CDC1 3 , δ) : 1.41 (9H, s) , 1.81-1.97 (IH, m) , 1.98-2.07 (IH, m) , 2.10 (3H, s) , 2.46-2.55 (2H, m) , 2.61 (3 x 2/3H, s) , 2.84 (3 x 1/3H, s) , 2.98-3.07 (2H, m) , 4.09-4.43 (2 x 2/3H, m) , 4.20-4.30 (IH, m) , 4.58 (2 x 1/3H, d, J=15Hz) , 5.12 (2H, q, J=8Hz), 6.93-7.32 (11H, m) (11) MASS (m/z) : 532 (M+H) + NMR (CDC1 3 , δ) : 1.42 (9H, s), 2.53 (2/3 x 3H, z), 2.79 (1/3 x 3H, s), 2.85-3.04 (4H, ) , 4.13 (1/3 x 2H, ABq, , 4.22-4.38 (IH, m) , 4.32 > (2/3 x IH, d, J=15Hz), 4.58 (2/3 x IH, d, J=15Hz), 4.90-5.18 (IH, ) , 6.22 (IH, br s), 6.60-7.32 (16H, ) (12) MASS (m/z) : 471 (M + +l) NMR (CDC1 3 , δ) : 1.46 (9H, s) , 2.52 (3H x 1/4, s), 2.54 (3H x 3/4, s) , 2.68 (3H x 3/4, s), 2.81 (3H x 1/4, s), 2.93-3.07 (2H, m) , 3.41 (IH, m) , 3.61 (IH, ), 4.00 (IH, m) , 4.21 (IH, m) , 4.41 (IH, d, J=15Hz) , 4.52 (IH, d, J=15Hz), 5.11 (IH x 3/4, m) , 5.17 (IH x 1/4, m) , 5.43 (IH, d, J=6Hz) , 7.08-7.37 (7H, m) , 8.24 (IH x 1/4, br s) , 8.31 (IH x 3/4, br s) (13) MASS (m/z) : 470 (M + +l) NMR (CDC1 3 , δ) : 1.11 (3H x 1/3, d, J=7Hz) , 1.14 (3H x 2/3, d, J=7Hz), 1.46 (9H, s) , 2.68 (3H x 2/3, s) , 2.86 (3H x 1/3, s), 2.93-3.10 (2H, m) , 4.03 (IH x 1/3, d, J=8Hz), 4.12 (IH x 2/3, d, J=8Hz), 4.22 (IH x 1/3, d, J=16Hz), 4.25 (IH, br s), 4.41 (IH x 2/3, d, J=15Hz), 4.42 (IH x 1/3, d, J=16Hz) , 4.61 (IH x 2/3, d, J=15Hz), 5.15 (IH, m) , 5.34 (IH, m) , 7.02- 7.29 (12H, m) (14) MASS : 566 (M+l) NMR (CDC1 3 , δ) : 1.37 (9H, s) , 2.47 (3 x 2/3H, s) , 2.69 (3 x 1/3H, s), 2.88-3.02 (2H, m) , 3.13-3.27 (2H, m) , 3.09 (2 x 1/6H, d, J=16Hz), 4.09 (2 x 1/3H, d, J=15Hz), 4.13 (2 x 1/6H, d, J=16Hz), 4.40- 4.52 (IH, ) , 4.51 (2 x 1/3H, d, J=15Hz), 4.92-5.01 (IH, m) , 5.02-5.13 (IH, m) , 6.68 (1 x 1/3H, d, J=8Hz), 6.78 (1 x 2/3H, d, J=8Hz) , 6.81-6.90 (IH, m) , 6.98-7.20 (6H, m) , 7.21-7.30 (3H, m) , 7.31 (IH, t, J=8Hz), 7.40-7.48 (2H, m) , 7.62 (IH, s), 7.70- 7.82 (3H, m) (15) MASS : 521 (M+l) NMR (CDC1 3 , δ) : 1.47 (9H, s), 2.53 (3H, s) , 2.58 (3 x 3/4H, s), 2.72 (3 x 1/4H, s), 2.78-3.01 (3H, m) , 3.03-3.20 (IH, m) , 3.95 (2 x 1/8H, d, J=16Hz) , 4.30 (2 x 1/8H, d, J=16Hz), 4.32 (2 x 3/8H, d, J=15Hz) , 4.48 (2 x 3/8H, d, J=15Hz), 4.32-4.50 (IH, m) , 4.97-5.12 (IH, m) , 5.70-5.90 (IH, m) , 6.80 (IH, s) , 7.02-7.40 (8H, m) , 7.50 (1 x 4/5K, s), 7.52 (1 x 1/5H, s), 8.17 (1 x 1/5H, s), 8.27 (1 x 4/5K, s) (16) MASS : 530 (M+l) NMR (CDC1 3 , δ) : 1.33 (9 x 1/2H, s), 1.37 (9 x 1/2H, s), 2.43-2.70 (5H, m) , 2.77-3.10 (4H, m) , 3.17-3.37 (IH, m) , 4.29 (2 x 1/6H, d, J=16Hz) , 4.31 (2 x 1/3H, d, J»15Hz), 4.36 (2 x 1/6H, d, J=16Hz) , 4.62 (2 x 1/3H, d, J=15Hz), 4.69-4.80 (1 x 1/2H, m) , 4.81-4.99 (1 x 1/2H, m) , 5.12-5.23 (IH, m) , 6.50- 6.90 (IH, m) , 6.93-7.37 (15H, m) (17) MASS : 568 (M+l) NMR (CDC1 3 , δ) : 1.42 (9H, s) , 2.59 (3 x 3/4H, s) , 2.83 (3 x 1/4H, s) , 2.71-2.88 (2H, m) , 3.15-3.40 (2H, m) , 4.30 (2 x 1/6H, d, J=16Hz) , 4.41 (2 x 1/6H, d, J=16Hz), 4.43 (2 x 1/3H, d, J=15Hz] , 4.78 (2 x 1/3H, d, J=15Hz), 4.52-4.63 (IH, m) , 5.03-5.20 (IH, m) , 6.37-6.46 (IH, m) , 7.02-7.22 (7H, ) , 7.51-7.80 (5H, m) , 7.87 (IH, s), 8.06 (1 x 1/4H, d, J=8Hz), 8.10 (1 x 3/4H, d, J=8Hz) , 8.51 (1 x 3/4H, d, J=2Hz), 8.54 (1 x 1/4H, d, J=2Hz) , 8.70 (IH, d, J=8Hz) (18) MASS : 508 (M+l) NMR (CDC1 3 , δ) : 1.45 (9H, s) , 2.92 (3 x 3/4H, s), 2.98 (3 x 1/4H, s), 3.00-3.22 (2H, n) , 3.30 (IH, t, J=5Hz), 3.52-3.64 (IH, ) , 3.87-4.02 (IK, m) , 4.12- 4.25 (IH, m) , 4.68 (2 x 1/6H, d, J=16Hz), 4.71 (2 x 1/3H, d, J=15Hz), 4.73 (2 x 1/6H, d, J=I6Hz) , 4.98 (2 x 1/3H, d, J=15Hz), 5.14-5.32 (IK, m) , 5.38-5.48 (IH, m) , 7.12-7.22 (6H, m) , 7.73-7.80 (2H, ra, , 7.99-8.06 (IH, m) , 8.10-8.14 (IH, ) , 8.78 (1 x 1/6H, s), 8.80 (1 x 5/6H, s) (19) MASS : 569 (M+l) NMR (CDC1 3 , δ) : 1.43 (9H, s), 2.73 (3 x 4/5H, s), 2.80-3.10 (2H, m) , 2.91 (3 x 1/5H, s) , 3.12-3.40 (2H, m) , 4.50-4.70 (IH, m) , 4.59 (2 x 1/2H, d, J=15Hz), 4.91 (2 x 1/2H, d, J=15Hz) , 5.03-5.28 (IH, m) , 6.23-6.41 (IH, m) , 7.00-7.23 (7E, m) , 7.59 (IH, t, J=8Hz), 7.67-7.80 (3H, m) , 7.92-6.03 (IH, m) , 8.04-8.14 (IH, m) , 8.48-8.52 (IH, m) , 8.58 (1 x 1/5H, s), 8.71 (1 x 4/5H, s) (20) MASS : 558 (M+l) NMR (CDC1 3 , δ) : 1.47 (9H, s) , 2.83 (3 x 4/5H, s), 2.90-3.20 (5H, m) , 2.98 (3 x 1/5H, s), 4.33-4.45 (IH, m) , 4.63 (2 x 1/5H, s), 4.74 (2 x 2/5H, d, J=15Hz), 4.83 (2 x 2/5H, d, J=15Hz) , 5.02-5.12 (1 x 4/5H, m), 5.13-5.22 (1 x 1/5H, m) , 6.81 (IH, s), 7.08-7.30 (6H, m) , 7.51 (IH, s) , 7.73-7.80 (2H, m) , 7.98-8.03 (IH, m) , 8.10-8.17 (IH, m) , 8.72 (1 x 1/5H, s) , 8.77 (1 x 4/5H, s) (21) MASS : 534 (M+l) NMR (CDC1 3 , δ) : 1.48 (9H, s), 2.83 (3 x 3/4H, s), 2.87 (3 x 1/4H, s) , 2.95-3.12 (2H, m) , 3.55-3.63 (IH, m) , 3.95-4.02 (IH, m) , 4.15-4.25 (IH, m) , 4.42 - 441 - (2 x 1/6H, d, J=16Hz), 4.43 (2 x 1/3H, d, J=15Hz) , 4.47 (2 x 1/6H, d, J=16Hz) , 4.70 (2 x 1/3H, d, J=15Hz), 5.10-5.22 (IH, m) , 5.38-5.48 (IH, m) , 7.08-7.32 (7H, m) , 7.45 (1 x 1/4H, dd, J=8, 2Hz), 7.58 (1 x 3/4H, dd, J=8, 2Hz) , 7.81 (IH, dd, J=8, 5Hz), 8.31-8.40 (2H, m) , 8.41 (1 x 1/4H, s) , 8.50 (1 x 3/4H, s), 8.67-8.71 (IH, m; (22) MASS : 595 (M+l) NMR (CDC1 3 , δ) : 1.44 (9H, s), 2.59 (3 x 4/5H, s), 2.70-3.02 (2H, m) , 2.68 (3 x 1/5H, s), 3.13-3.40 (2H, m) , 4.16 (2 x 1/6H, d, J=16Hz) , 4.30 (2 x 1/6H, d, J=16Hz), 4.37 (2 x I/3H, d, J=15Hz), 4.53 (2 x 1/3H, d, J=15Hz) , 4.54-4.63 (IH, m) , 5.01-5.13 (IH, m) , 6.35-6.48 (IH, m) , 7.03-7.28 (7H, m) , 7.37-7.47 (2H, m) , 7.53-7.70 (3H, m) , 8.23-8.33 (IH, m) , 8.47 (IH, s) , 8.51 (IH, d, J=3Hz), 8.67 (IH, d, J=8Hz) , 9.18 (IH, s) (23) MASS : 534 (M+l) NMR (CDC1 3 , δ) : 1.47 (9H, s) , 2.73 (3 x 4/5H, s), 2.83 (3 x 1/5H, s), 2.97-3.17 (2H, m) , 3.23-3.32 (IH, m) , 3.58-3.66 (IH, m) , 3.94-4.07 (IH, m) , 4.11 (2 x 1/6H, d, J=16Hz), 4.17-4.25 (IH, ) , 4.48 (2 x 1/6H, d, J=16Hz) , 4.50 (2 x 1/3H, d, J=15Hz), 4.59 (2 x 1/3H, d, J=15Hz) , 5.10-5.22 (IH, m) , 5.33-5.45 (IH, m) , 7.12-7.32 (6H, m) , 7.38-7.48 (IH, m) , 7.55 (IH, dd, J=8, 2Hz) , 7.68 (IH, dd, J=8, 2Hz), 8.27-8.32 (IH, ) , 8.43 (1 x 1/5H, s), 8.52 (1 x 4/5H, s), 8.67 (IH, d, J=2Hz), 9.19 (IH, s) (24) MASS (m/z) : 737 (M + +l) NMR (CDC1 3 , δ) : 1.42 (9H, s) , 1.44 (2K, m) , 1.32 (2H, m) , 2.14 (3H, s) , 2.66 (3H, s) , 2.73 (3H, s), 2.75 (2H, m) , 2.78 (3H, s), 3.12 (2H, m) , 3.82 (3H, s), 4.14 (IH, d, J=16Hz), 4.41 (IH, d, J=16Hz) , 4.54 (IH, m) , 4.92 (IH, m) , 4.52 (IH, m) , 6.55 (IH, s), 7.00-7.24 (10H, m) (25) MASS (m/z) : 517 (M + +l) NMR (CDC1 3 , δ) : 1.43 (9H, s) , 2.55 (3H x 3/4, s), 2.77 (3H x 1/4, s), 2.97 (2H, m) , 3.06 (2H, m) , 4.03 (IH x 1/4, d, J=16Hz) 4.24 (IH x 1/4, d, J=16Hz) , 4.32 (IH x 3/4, d, J=15Hz), 4.37 (IH, m) , 4.57 (IH x 3/4, d, J=15Hz), 4.92 (IH, m) , 5.10 (IH, m) , 6.72 (IH, m) , 7.10-7.39 (12H, m) , 8.26 (IH x 1/4, br s) , 8.40 (IH x 3/4, br s), 8.53 (IH, m) (26) MASS (m/z) : 518 (M + +l) NMR (CDC1 3 , δ) : 1.41 (9H, s), 2.59 (3H x 3/4, s) , 2.78 (3H x 1/4, s), 2.92-3.03 (3H, m) , 3.12 (IH, m) , 3.99 (IH x 1/4, d, J=16Hz) , 4.27 (IH x 1/4, d, J=16Hz), 4.33 (IH x 3/4, d, J=15Hz) , 4.43 (IH, m) , 4.61 (IH x 3/4, d, J=l5Hz) , 4.95 (IH, d, J=7Hz) , 5.09 (IH, m) , 6.90 (IH, d, J=7Hz) , 7.09-7.40 (9H, m) , 8.27 (IH x 1/5, br s) , 8.41 (IH x 4/5, br s), 8.50 (2H, d, J=5Hz), 8.53 (IH, d, J=5Hz) (27) MASS (m/z) : 523 (M + +l) NMR (CDC1 3 , δ) : 1.46 (9H, s) , 2.73 (3H x 3/4, s) , 2.85 (3H x 1/4, s), 2.93-3.11 (2K, m) , 3.59 (IH, m) , 3.98 (IH, m) , 4.17 (IH x 1/4, d, J=15Hz) , 4.20 (IH, m) , 4.47 (IH x 1/4, d, J=15Hz) , 4.52 (IH x 3/4, d, J=15Hz), 4.58 (IH x 3/4, d, J=15Hz) , 5.14 (IH, m) , 5.40 (IH, m) , 7.17-7.27 (7H, m) , 7.61 (2H, d, J=8Hz), 8.10 (IH, s), 8.54 (IH, s) (28) MASS (m/z) : 515 (M+l) ÷ NMR (CDC1 3 , δ) : 1.46 (9H, s), 1.90 (IH, m) , 2.03 (IH, m) , 2.10 (3H, s), 2.47-2.57 (2H, m) , 2.54 (3H, m) , 2.60 (3H x 4/5, s) , 2.79 (3H x 1/5, s) , 3.01 (2H, d, J=7.5Hz), 4.27 (IH, m) , 4.36 (IH, d, J=14.5Hz), 4.52 (IH, d, J=14.5Hz), 5.07-5.23 (2H, m) , 6.90-7.01 (IH, m) , 7.05-7.23 (6H, m) , 7.25-7.34 (IH, m) , 8.20 (1/5H, d, J=2.5Hz), 8.31 (4/5H, d, J=2.5Hz) (29) MASS (m/z) : 501 (M+l) + NMR (CDC1 3 , δ) : 1.47 (9H, s) , 1.91 (IH, m) , 2.04 (IH, m), 2.10 (3H, s), 2.47-2.57 (2H, m) , 2.63 (3H x 4/5, s), 2.80 (3H x 1/5, s) , 3.02 (2H, d, J=8.5Hz), 4.26 (IH, m) , 4.37 (IH, d, J=14.5Hz), 4.59 (IH, d, J=14.5Hz), 5.09-5.20 (2H, m) , 6.92-7.02 (IH, m) , 7.10-7.30 (6H, m) , 7.39-7.45 (IH, m) , 8.29 (IH x 1/5, d, J=1.5Hz), 8.41 (IH x 4/5, d, J=1.5Hz), 8.53 (IH, d, J=5.5Hz) (30) MASS (m/z) : 551 (M+l) + NMR (CDC1 3 , δ) : 1.46 (9H, s) , 1.92 (IH, ) , 2.05 (IH, m), 2.09 (3H, s) , 2.46-2.58 (2H, m) , 2.69 (3H x 4/5, s), 2.88 (3H x 1/5, s) , 3.03 (2H, d, J=7.5Hz), 4.21-4.35 (IH, m) , 4.28 (IH x 1/5, d, J=14.5Hz), 4.51 (IH x 1/5, d, J=14.5Hz), 4.56 (IH x 4/5, d, J=14.5Hz), 4.78 (IH x 4/5, d, J=8.0Hz), 5.07-5.29 (2H, m) , 6.93-7.04 (IH, ) , 7.10-7.20 (5H, m) , 7.51-7.60 (IH, m), 7.68-7.78 (IH, ) , 7.80 (IH, d, J=7.5Hz), 7.93 (IH x 4/5, d, J=0.75Hz), 8.06 (IH x 1/5, d, J=0.75Hz), 8.11 (IH, d, J=7.5Hz), 8.61 (IH x 1/5, d, J=1.5Hz), 8.77 (IH x 4/5, d, J=1.5Hz) (31) MASS (m/z) : 552 (M+l) + NMR (CDC1 3 , δ) : 1.46 (9H, s) , 1.83-2.11 (2H, m) , 2.08 (3H, s), 2.41-2.57 (IH, m) , 2.52 (IH, t, J=7.5Hz), 2.87 (3H x 4/5, s) , 2.96 (3H x 1/5, s) , 3.01-3.10 (2H, ) , 4.20-4.32 (IH, m) , 4.61 (2H x 1/5, s) , 4.69 (IH x 4/5, d, J=14.5Hz), 4.93 (IH x 4/5, d, J=14.5Hz), 5.08-5.29 (2H, m) , 6.97 (IH, m) , 7.11-7.24 (5H, m) , 7.73-7.80 (2H, m) , 7.97-8.04 (IH, m) , 8.07-8.15 (IH, m) , 8.66 (IH x 1/5, s) , 8.79 (IH x 4/5, s) (32) MASS (m/z) : 578 (M+l) + NMR (CDC1 3 , δ) : 1.47 (9H, s) , 1.86-1.97 (IH, m) , 2.00-2.12 (IH, m) , 2.10 (3H, s), 2.52 (2H, t, J=7.5Hz), 2.69 (3H x 4/5, s), 2.83 (3H x 1/5, s) , 3.03 (2H, d, J=7.5Hz), 4.13 (IH x 1/5, d, J=14.5Hz), 4.39 (IH x 1/5, d, J=14.5Hz), 4.48 (IH x 4/5, d, J=14.5Hz), 4.59 (IH x 4/5, d, J=14.5Hz), 5.08-5.23 (2H, m) , 6.92-7.01 (IH, m) , 7.13-7.33 (6H, m) , 7.40 (IH, dd, J=7.5, 5.5Hz), 7.52 (IH, dd, J=8.5, 1.5Hz), 7.65 (IH x 1/5, d, J=7.5Hz), 7.69 (IH x 4/5, d, J=7.5Hz), 8.31 (IH, dd, J=8.5, 1.5Hz), 8.40 (IH x 1/5, d, J=1.5Hz), 8.52 (IH x 4/5, d, J=1.5Hz), 8.65 (IH, d, J=5.5Hz), 9.17 (IH x 1/5, d, J=1.5Hz), 9.19 (IH x 4/5, d, J=1.5Hz) (33) MASS (m/z) : 522 (M+l) + NMR (CDC1 3 , δ) : 1.43 (9H, s) , 2.53 (3H x 2/3, s) , 2.80 (3H x 1/3, s) , 2.91-3.06 (2H, m) , 3.18-3.39 (2H, m) , 4.00 (IH x 1/3, d, J=14.5Hz), 4.26 (IH x 1/3, d, J=14.5Hz), 4.30-4.45 (IH, br s) , 4.38 (IH x 2/3, d, J=14.5Hz), 4.53 (IH x 2/3, d, J=14.5Hz), 5.00 (IH, br s), 5.14 (IH, m) , 6.81 (IH, dd, J=8.5, 1.5Hz), 6.87-6.95 (2H, m) , 7.07 (IH, dd, J=7.0, 1.5Hz), 7.09-7.32 (10H, m) (34) MASS : 500 (M+H) + NMR (CDC1 3 , δ) : 1.45 (9H, s) , 2.66 (2/3 x 3H, s) , 2.78 (1/3 x 3H, s) , 2.87-3.07 (2H, m) , 3.05 (1/3 x 6H, s), 3.07 (2/3 x 6H, z) , 3.52-3.65 (IH, mi, 3.82 (1/3 x IH, d, J=17Hz), 3.90-4.05 (IH, m) , 4.11-4.26 (IH, m) , 4.34 (1/3 x IH, d, J=17Hz) , 4.35 (2/3 x 2H, ABq, Δ=0.11, J=15Hz) , 5.01-5.32 (IH, m) , 5.32- 5.48 (IH, m) , 6.47 (IH, d, J=9Hz) , 7.05-7.35 (7H, m) , 7.90 (1/3 x IH, d, J=2Hz), 7.98 (2/3 x IH, d, J=2Hz) (35) MASS (m/z) : 597 (M+H) ÷ NMR (CDC1 3 , δ) : 1.46 (9H, s) , 2.68 (3/4 x 3H, s), 2.86 (1/4 x 3H, s), 2.92-3.16 (2H, ) , 3.53-3.66 (IH, m) , 3.81-4.00 (IH, m) , 4.21-4.62 ( (2+l/4)H, m) , 4.56 (2H, s), 4.81 (3/4 x IH, d, J=15Hz) , 5.10-5.45 (2H, m) , 7.03-8.16 (16H, m) , 8.61 (1/4 x IH, d, J=2Hz), 8.75 (3/4 x IH, d, J=2Hz) (36) MASS (m/z) : 506 (M+H) + NMR (CDCI3, δ) : 1.43 (9K, s) , 2.56 (2/3 x 3H, s), 2.80-3.06 (4H, m) , 2.82 (1/3 x 3K, s) , 4.15 (1/3 x 2H, ABq, Δ=0.24, J=17HZ) , 4.20-4.39 (IK, m) , 4.46 (2/3 x 2H, ABq, Δ=0.15, J=15Hz) , 4.91 (IH, br s) , 5.05-5.20 (IH, ) , 6.21 (1/3 x IH, s) , 6.26 (2/3 x IH, s), 6.70-7.40 (13H, m) (37) MASS (m/z) : 506 (M+H) + NMR (CDC1 3 , δ) : 1.44 (9H, s) , 2.52 (2/3 x 3H, s), 2.78 (1/3 x 3H, s) , 2.87-3.22 (4H, m) , 4.13 (1/3 x 2H, ABq, Δ=0.24, J=17Hz) , 4.34-4.48 (IH, ) , 4.43 (2/3 x 2H, ABq, J=15Hz) , 5.00-5.23 (2H, m) , 6.02-6.13 (IH, m) , 6.27 (IH, m) , 6.80-7.37 (12H, m) (38) MASS : 487 (M+l) NMR (CDC1 3 , δ) : 1.43 (9H, s), 2.64 (3 x 3/4H, s), 2.78 (3 x 1/4H, s) , 2.90-3.11 (2H, ) , 3.25-3.43 (IK, m) , 3.52-3.63 (IH, m) , 3.90 (3H, s), 3.84-4.02 (IH, m), 4.12-4.23 (IH, m) , 4.23 (2 x 1/6H, d, J=16Hz), 4.30 (2 x 1/3H, d, J=15Hz) , 4.35 (2 x 1/6H, d, J=16Hz), 4.50 (2 x 1/3H, d, J=15Hz) , 5.02- 5.25 (IH, m), 5.37-5.48 (IH, m) , 6.68 (IH, d, J=8Hz), 7.07-7.40 (7H, m) , 7.88 (1 x 1/5H, s) , 7.95 (1 x 4/5H, s) (39) MASS : 557 (M+l) NMR (CDC1 3 , δ) : 1.40 (9H, s), 2.63 (3 x 4/5H, s) , 2.84 (3 x 1/5H, s) , 2.88-3.20 (4H, m) , 4.22 (2 x 1/6H, d, J=16Hz), 4.33-4.50 (IH, m) , 4.53 (2 x 1/6H, d, J=16Hz), 4.60 (2 x 1/3H, d, J=15Hz) , 4.68 (2 x 1/3H, d, J=15Hz) , 5.00-5.18 (IH, m) , 5.71-5.90 (IH, m) , 6.80 (IH, s) , 7.04-7.22 (5H, m) , 7.44-7.60 (3H, m) , 7.68-7.80 (2H, m) , 7.90 (IH, s) , 8.04-8.11 (IH, m) , 8.61 (1 x 1/5H, s) , 8.71 (1 x 4/5H, s) (40) MASS : 584 (M+l) NMR (CDC1 3 , δ) : 1.43 (9H, s) , 2.68 (3 x 4/5H, s) , 2.81 (3 x 1/5H, s) , 2.87-3.02 (3H, m) , 3.08-3.20 (IH, m) , 4.11 (2 x 1/6H, d, J=16Hz) , 4.32-4.45 (IH, m) , 4.48 (2 x 1/3H, d, J=15Hz) , 4.51 (2 x 1/3H, d, J=15Hz), 4.58 (2 x 1/6H, d, J=16Hz) , 5.00-5.13 (IH, m) , 6.82 (IH, s), 7.08-7.16 (2H, m) , 7.18-7.28 (4H, m) , 7.30-7.43 (2H, m) , 7.46-7.53 (2H, m) , 7.62-7.70 (IH, m) , 8.29 (IH, d, J=8Hz) , 8.39 (1 x 1/5H, s) , 8.50 (1 x 4/5H, s), 8.63 (IH, d, J=5Hz) , 9.18 (IH, s) (41) MASS : 546 (M+l) NMR (CDC1 3 , δ) : 1.42 (9H, s) , 2.54 (3 x 2/3H, s) , 2.79 (3 x 1/3H, s) , 2.90-3.03 (4H, m) , 3.77 (3H, s), 4.02 (2 x 1/6H, d, J=16Hz) , 4.23 (2 x 1/6H, d, J=16Hz), 4.31 (2 x 1/3H, d, J=15Hz) , 4.58 (2 x 1/3H, d, J-15HZ), 4.25-4.40 (IH, m) , 4.87-4.98 (IH, m) , 5.03-5.18 (IH, m) , 6.63-6.93 (4H, m) , 7.01-7.17 (5H, m), 7.17-7.21 (2H, m) , 7.22-7.32 (4H, ) (42) MASS : 569 (M+l) NMR (CDC1 3 , δ) : 1.48 (9H, s) , 2.60 (3 x 2/3H, s) , 2.82 (3 x 1/3H, s) , 2.73-2.90 (2H, m) , 3.17-3.42 (2H, m) , 4.40 (2 x 1/6H, d, J=16Hz) , 4.55 (2 x 1/6H, d, J=16Hz), 4.56 (2 x 1/3H, d, J=15Hz) , 4.56- 4.67 (IH, m) , 4.75 (2 x 1/3H, d, J=15Hz) , 5.08-5.19 (IH, m) , 6.30-6.50 (IH, m) , 7.07-7.23 (7H, ) , 7.38 (IH, d, J=8HZ), 7.60 (IH, t, J=8Hz) , 7.62-7.75 (IH, m) , 7.81 (1 x 2/3H, s), 8.01 (1 x 1/3H, s) , 7.99 (IH, d, J=8Hz), 8.51 (IH, d, J=3Hz), 8.82 (2H, s) (43) MASS : 566 (M+l) NMR (CDC1 3 , δ) : 1.38 (9H, s) , 2.43 (3 x 3/4H, s) , 2.71 (3 x 1/4H, s), 2.80-2.98 (2H, m) , 3.35-3.67 (2H, m) , 4.03 (2 x 1/8H, d, J=16Hz) , 4.16 (2 x 1/8H, d, J=16Hz), 4.18 (2 x 3/8H, d, J=15Hz) , 4.54 (2 x 3/8H, d, J=15Hz), 4.42-4.53 (IK, m) , 4.90-5.18 (2H, m) , 6.50-6.65 (IH, m) , 6.83-7.40 (12H, m) , 7.42-7.60 (2H, m) , 7.74 (IH, d, J=8Hz) , 7.83 (IH, t, J=8Hz) , 8.12 (IH, d, J=8Hz) (44) MASS : 507 (M+l) NMR (CDC1 3 , δ) : 1.44 (9H, s) , 2.60 (3 x 3/4H, s) , 2.71 (3 x 1/4H, s), 2.74-3.03 (3H, m) , 3.04-3.19 (IH, m) , 4.32-4.40 (IH, m) , 4.41 (2 x 3/8H, d, J=15Hz), 4.47 (2 x 3/8H, d, J=15Hz) , 4.50 (2 x 1/8H, d, J=16Hz), 4.63 (2 x 1/8H, d, J=16Hz), 4.99- 5.12 (IH, m) , 5.72-5.90 (IH, m) , 6.81 (IH, s) , 7.08-7.32 (7H, m) , 7.32-7.43 (IH, m) , 7.47-7.53 (IH, m) , 8.27 (1 x 1/4H, s) , 8.38 (1 x 3/4H, s), 8.49-8.53 (IH, m) (45) MASS : 532 (M+l) NMR (CDCI3, δ) : 1.41 (9H, s) , 2.49 (3H, s), 2.52 (3 x 3/4H, s), 2.71 (3 x 1/4H, s) , 2.87-3.00 (2H, m) , 3.14-3.41 (2H, m) , 3.98 (2 x 1/8H, d, J=16Hz) , 4.20 (2 x 1/8H, d, J=16Hz), 4.23 (2 x 3/8H, d, J=15Hz) , 4.50 (2 x 3/8H, d, J=15Hz) , 4.52-4.63 (IH, m) , 5.00-5.17 (IH, m) , 6.30-6.47 (IH, n) , 6.92-7.30 (9H, m) , 7.53-7.68 (2H, m) , 8.12 (1 x 1/4H, s) , 8.25 (1 x 3/4H, s) , 8.48-8.52 (IH, m) (46) MASS : 517 (M+l) NMR (CDC1 3 , δ) : 1.40 (9H, s), 2.58 (3 x 2/3H, s), 2.82 (3 x 1/3H, s), 2.83-3.19 (4H, m) , 4.09 (2 x 1/6H, d, J=15Hz), 4.30 (2 x 1/6H, d, J=15Hz) , 4.33 (2 x 1/3H, d, J=16Hz), 4.33-4.50 (IH, m) , 4.60 (2 x 1/3H, d, J=16Hz), 5.00-5.20 (2H, m) , 6.90-7.40 (12H, m) , 7.50 (IH, t, J=8Hz) , 8.40 (IH, s), 8.48 (IH, s) (47) MASS : 550 (M+l) NMR (CDC1 3 , δ) : 1.41 (9H, s) , 2.57 (3 x 2/3H, s), 2.81 (3 x 1/3H, s), 2.87-3.10 (4H, m) , 3.99 (2 x 1/6H, d, J=16Hz), 4.27 (2 x 1/6H, d, J=16Hz) , 4.32 (2 x 1/3H, d, J=15Hz), 4.60 (2 x 1/3H, d, J=15Hz) , 4.28-4.43 (IH, m) , 4.85-5.00 (IH, m) , 5.02-5.18 (IH, m) , 6.69-6.99 (2H, m) , 7.02-7.15 (5H, ) , 7.16-7.40 (8H, m) (48) MASS : 528 (M+l) NMR (CDC1 3 , δ) : 1.46 (9 x 2/3H, s) , 1.50 (9 x 1/3H, s), 2.48-2.73 (2H, m) , 2.51 (3 x 2/3H, s) , 2.78 (3 x 1/3H, s), 2.90-3.37 (2H, m) , 4.26-4.70 (4H, m) , 4.82-5.10 (2H, m) , 6.52-6.73 (IH, m) , 6.83-7.08 (5H, m) , 7.09-7.40 (9H, m) Preparation 61 The following object compounds were obtained according a similar manner to that of Preparation 3, 4, 8, 41 or 54. (1) NMR (CDC1 3 , δ) : 1.99 (3 x 1/3H, s) , 2.03 (3 x 2/3H, s), 2.38-2.58 (IH, m) , 2.72 (3 x 2/3H, s) , 2.82- 3.12 (3H, m), 2.90 (3 x 1/3H, s), 3.38 (1 x 1/3H, dd, J=12, 4Hz), 3.49 (1 x 2/3H, dd, J=12, 4Hz) , 4.35 (2 x 2/3H, d, J=15Hz) , 4.36 (2 x 1/6H, d, J=16Hz), 4.43 (2 x 1/6H, d, J=16Hz) , 4.68 (2 x 1/3H, d, J=15Hz), 5.19 (IH, q, J=12Hz) , 7.00-7.32 (10H, m) , 8.04 (1 x 1/3H, d, J=8Hz) , 8.13 (1 x 2/3H, d, J=8Hz) (2) MASS : 391 (M+l) NMR (CDC1 3 , δ) : 2.71 (3 x 3/4H, s), 2.79 (3 x 1/4H, s), 2.93-3.17 (2H, m) , 3.35-3.49 (IH, m) , 3.58-3.68 (IH, ), 3.70-3.81 (IH, m) , 4.20 (2 x 1/8H, d, J=16Hz), 4.39 (2 x 1/8H, d, J=16Hz) , 4.35 (2 x 3/8H, d, J=15Hz), 4.58 (2 x 3/8H, d, J=15Hz) , 5.12 (IH, q, J=8Hz), 7.10-7.18 (2H, m) , 7.20-7.30 (4H, m) , 7.38 (IH, d, J=8Hz) , 7.97 (IH, d, J=8Hz) , 8.09 (1 x 1/4H, s), 8.19 (1 x 3/4H, s) (3) MASS : 614 (M+l) NMR (CDC1 3 , δ) : 2.31-2.50 (IH, m) , 2.57-2.68 (IH, m) , 2.63 (3 x 2/3H, s) , 2.81 (3 x 1/3H, s) , 2.88-3.04 (3H, m) , 4.28 (2 x 2/3H, d, J=15Hz), 4.63 (2 x 1/3H, d, J=15Hz), 5.09 (IH, q, J=8Hz) , 6.93-7.31 (19H, m), 7.40-7.45 (6H, m) , 7.70 (1 x 1/3H, d, J=8Hz), 7.80 (1 x 2/3H, d, J=8Hz) (4) MASS : 407 (M+l) NMR (CDC1 3 , δ) : 2.73 (3 x 3/4H, s), 2.89 (3 x 1/4H, s), 2.94-3.18 (2H, m) , 3.38-3.86 (3H, m) , 4.39 (2 x 1/6H, d, J=16Hz), 4.59 (2 x 1/6H, d, J=16Hz) , 4.60 (2 x 1/3H, d, J=15Hz), 4.73 (2 x 1/3H, d, J=15Hz) , 5.11-5.31 (IH, m), 7.08-7.28 (5H, m) , 7.56 (IH, t, J=8Hz), 7.69 (IH, t, J=8Hz), 7.77 (IH, d, J=8Hz) , 7.90 (IH, s), 8.00-8.12 (2H, m) , 8.68 (1 x 1/4H, d, J=2Hz), 8.74 (1 x 3/4H, d, J=2Hz) (5) NMR (CDC1 3 , δ) : 2.55 (3H x 2/3, s), 2.73 (3H x 1/3, s), 3.00 (2H, t, J=7Hz), 3.88 (2H, m) , 4.06-4.61 (5H, m) , 5.12 (IH, d, J=7Hz) , 6.84-7.25 (15H, m) , 8.14 (IH, d, J=7Hz) (6) NMR (CDC1 3 , δ) : 0.88 (6H, m) , 1.57-1.85 (3H, m) , 2.62 (3H x 2/3, s), 2.80 (3H x 1/3, s), 2.95-3.14 (2H, m) , 4.15 (IH, m) , 4.18 (IH x 1/3, d, J=15Hz), 4.27 (IH x 2/3, d, J=15Hz), 4.32 (IH x 1/3, d, J=15Hz) , 4.58 (IH x 2/3, d, J=15Hz) , 5.18 (IH, t, J=7Hz) , 6.90-6.99 (3H, m) , 7.11-7.23 (7H, m) , 8.14 (IH x 2/3, d, J=8Hz), 8.22 (IH x 1/3, d, J=8Hz) (7) NMR (CD 3 OD, δ) : 2.90 (3H x 2/3, s) , 3.04 (3H x 1/3, s), 3.41 (IH, m) , 3.56 (IH, m) , 3.65-3.73 (2H, m) , 3.80 (IH, m) , 4.13 (IH, m) , 4.37-4.67 (4H, m) , 5.47 (IH, m) , 7.18-7.37 (8H, m) , 7.76 (IH, m) , 7.89-8.02 (2H, m) , 8.26 (IH, m) , 8.48 (IH, m) , 8.73 (IH, m) (8) NMR (CDC1 3 , δ) : 2.81 (3H x 3/4, s), 2.89 (3H x 1/4, s), 2.92-3.14 (2H, m) , 3.29 (IH x 1/4, t, J=5Hz), 3.44 (IH x 3/4, t, J=5Hz) , 3.52-3.64 (IH, m) , 3.72- 3.83 (IH, m) , 4.37 (IH x 1/4, d, J=15Hz) , 4.41 (IH x 3/4, d, J=15Hz), 4.47 (IH x 1/4, d, J=15Hz) , 4.62 (IH x 3/4, d, J=15Hz), 5.04 (IH x 1/4, q, J=5Hz) , 5.21 (IH x 3/4, q, J=5Hz) , 6.88 (2H x 1/4, d, J=7Hz), 6.94 (2H x 3/4, d, J=7Hz) , 7.11-7.28 (5H, m) , 7.92 (IH, d, J=5Hz) , 8.51 (2H, d, J=7Hz) (9) NMR (CDC1 3 , δ) : 2.45 (IH x 1/3, dd, J=8, 15Hz) , 2.60 (IH x 2/3, dd, J=8, 15Hz), 2.70 (3H x 2/3, s) , 2.85 (3H x 1/3, s), 2.91-3.22 (3H, m) , 3.50 (IH x 1/3, dd, J=4, 8Hz), 3.59 (IH x 2/3, dd, J=4, 8Hz) , 4.32 (IH x 2/3, d, J=15Hz), 4.33 (IH x 1/3, d, J=15Hz) , 4.42 (IH x 1/3, d, J=15Hz) , 4.67 (IH x 2/3, d, J=15Hz), 5.22 (IH, m) , 6.97-7.34 (15H, m) , 7.92 (IH x 1/3, d, J=8Hz), 8.00 (IH x 2/3, d, J=8Hz) (10) NMR (CD 3 OD, δ) : 2.93 (3H x 3/4, s) , 3.07 (2H, d, J=7Hz), 3.34 (3H x 1/4, s) , 3.85 (IH, dd, J=7, 12Hz), 3.93-4.01 (2H, m) , 4.41 (IH x 1/4, d, J=15Hz), 4.53 (IH x 3/4, d, J=15Hz) , 4.75 (IH x 1/4, d, J=15Hz), 4.81 (IH x 3/4, d, J=15Hz) , 5.11 (IH, t, J=7Hz), 7.24-7.31 (5H, m) , 8.02 (IH, dd, J=6, 8Hz), 8.30 (IH, d, J=8Hz) , 8.67 (IH, d, J=2Hz), 8.77 (IH, d, J=6Hz) (11) MASS (m/z) : 400 (M+H) NMR (CDC1 3 , δ) : 1.62-1.78 (IH, m) , 1.90-2.02 (IH, m) , 2.05 (3 x 1/3H, s), 2.09 (3 x 2/3H, s) , 2.42 (IH, t, J=8Hz), 2.51 (IH, t, J=8Hz), 2.70 (3 x 2/3H, s) , 2.90 (3 x 1/3H, s), 2.97-3.11 (2H, m) , 3.38-3.41 (1 x 1/3H, m), 3.47-3.51 (1 x 2/3H, m) , 4.31-4.39 (2 x 2/3H, m) , 4.69 (2 x 1/3H, d, J=15Hz) , 5.19 (IH, q, J=8Hz), 7.01-7.32 (10H, m) , 7.83 (1 x 1/3H, d, J=8Hz), 7.91 (1 x 2/3H, d, J=8Hz) (12) MASS (m/z) : 356 (M+l) NMR (CDC1 3 , δ) : 2.73 (3 x 2/3H, s) , 2.89 (3 x 1/3H, s), 2.92-3.12 (2H, m) , 3.30 (1 x 1/3H, t, J=8Hz) , 3.42 (IH x 2/3H, t, J=8Hz) , 3.48-3.62 (IH, m) , 3.67-3.81 (IH, m) , 4.31-4.51 (2 x 2/3H, m) , 4.69 (2 x 1/3H, d, J=15Hz), 5.19 (IH, q, J=8Hz) , 7.06 (2 x 1/3H, d, J=8Hz), 7.11 (2 x 2/3H, d, J=8Hz) , 7.13-7.33 (8H, m) , 7.82-7.93 (IH, ) (13) NMR (CDC1 3 , δ) : 2.52 (3H x 1/4, s) , 2,54 (3H x 3/4, s), 2.72 (3H x 3/4, s) , 2.82 (3H x 1/4, s) , 2.93- 3.09 (2H, m) , 3.36 (IH x 1/4, t, J=6Hz) , 3.42 (IH 3/4, t, J=6Kz), 3.61 (IH, m) , 3.77 (IH, m) , 4.15 (IH x 1/4, d, J=16Kz), 4.37 (IH x 3/4, d, J=15Hz) , 4.42 (IH x 1/4, d, J=16Hz) , 4.56 (IH x 3/4, d, J=15Hz), 5.15 (IH x 3/4, q, J=7Hz), 5.20 (IK x 1/4 q, J=7Hz), 7.05-7.35 (7H, m) , 7.93 (IH, d, J=7Hz) , 8.23 (IH x 1/4, d, J=2Hz) , 8.31 (IH x 3/4, d, J=2Hz) (14) NMR (CDC1 3 , δ) : 1.05 (3H x 1/3, d, J=7Hz) , 1.12 (3H 2/3, d, J=7Hz), 2.77 (3H x 2/3, s), 2.92 (3H x 1/3 s), 2.94-3.12 (2H, m) , 4.12 (IK, m) , 4.37 (IH x 1/3, d, J=16Hz), 4.39 (IH x 2/3, d, J=15Hz) , 4.45 (IH, m) , 4.60 (IH x 1/3, d, J=16Hz) , 4.67 (IH x 2/3, d, J=15Hz), 5.13 (IH x 1/3, q, J=7Hz) , 5.22 (IH x 2/3, q, J=7Hz) , 7.05-7.31 (10H, m) , 7.97 (IH m) (15) MASS : 466 (M+l) NMR (CDC1 3 , δ) : 2.58-2.83 (IH, m) , 2.68 (3 x 2/3H, s), 2.81 (3 x 1/3H, s) , 2.90-3.10 (2K, m) , 3.28 (1 x 1/3H, dd, J=15, 5Hz), 3.33 (1 x 2/3H, dd, J=15, 5Hz), 3.60 (1 x 1/3H, dd, J=12, 5Hz) , 3.70 (1 x 2/3H, dd, J=12, 5Hz), 4.28 (2 x 1/3K, d, J=I5Hz) , 4.32 (2 x 1/6H, d, J=16Hz) , 4.41 (2 x 1/6H, d, J=16Hz), 4.68 (2 x 1/3H, d, J=15Hz) , 5.18-5.28 (IH m) , 7.00 (2 x 1/3H, d, J=7Hz) , 7.07 (2 x 2/3H, d, J=7Hz), 7.10-7.39 (9H, m) , 7.41-7.51 (2H, m) , 7.61 (1 x 1/3H, s), 7.64 (1 x 2/3H, s) , 7.73-7.85 (3H, m) , 7.92 (1 x 1/3H, d, J=8Hz) , 8.01 (1 x 2/3H, d, J=8Hz) (16) MASS : 421 (M+l) NMR (CDC1 3 , δ) : 2.50 J3H, s) , 2.63 (3 x 3/4K, s) , 2.80 (3 x 1/4H, s), 2.82-3.10 (4H, m) , 3.50-3.62 (IK, m) , 4.11 (2 x 1/8H, d, J=16Hz) , 4.39 (2 x 1/8H, d, J=16Hz), 4.41 (2 x 3/8H, d, J=15Hz) , 4.49 (2 x 3/SH, d, J=15Hz), 5.07-5.23 (IH, m) , 6.81 (IH, s), 7.03-7.37 (7H, m) , 7.53 (IH, s) , 7.95-8.08 (IH, m) , 8.22 (1 x 1/4H, s) , 6.30 (1 x 3/4H, s) (17) MASS : 430 (M+l) NMR (CDC1 3 , δ) : 2.26 (3H, s) , 2.43-2.61 (IH, m) , 2.71 (3 x 2/3H, s), 2.86 (3 x 1/3H, s) , 2.90-3.21 (4H, m) , 4.37 (2 x 1/6H, d, J=16Hz), 4.40 (2 x 1/3H, d, J=15Hz), 4.41 (2 x 1/6H, d, J=16Hz) , 4.61 (2 x 1/3H, d, J=15Hz), 5.18-5.28 (IH, m) , 7.00-7.38 (15H, m) , 7.80 (1 x 1/3H, d, J=8Hz) , 7.88 (1 x 2/3H, d, J=8Hz) (18) MASS : 468 (M+l) NMR (CDC1 3 , δ) : 2.72 (3 x 2/3H, s), 2.82-3.12 (3H, m) , 2.88 (3 x 1/3H, s) , 3.19-3.32 (IH, m) , 3.69 (1 x 1/4H, dd, J=8, 2Hz), 3.80 (1 x 3/4H, dd, J=8, 2Hz), 4.51 (2 x 1/3H, d, J=15H∑) , 4.52 (2 x 1/6H, d, J=16Hz), 4.59 (2 x 1/6H, d, J=16Hz), 4.81 (2 x 1/3H, d, J=15Hz), 5.12-5.30 (IH, m) , 7.10-7.23 (7H, m) , 7.51-7.80 (4H, m) , 7.92 (IH, s), 8.09 (1 x 1/4H, d, J=8Hz), 8.11 (1 x 3/4H, d, J=8Kz) , 8.22 (1 x 1/4H, d, J=8Hz), 8.24 (1 x 3/4H, d, J=8Hz) , 8.49- 8.56 (IH, m) , 8.63 (1 x 1/4H, d, J=2Hz) , 8.74 (1 x 3/4H, d, J=2Hz) (19) mp : 165-167 β C MASS : 408 (M+l) NMR (CDC1 3 , δ) : 2.96 (3H, s) , 2.98-3.35 (2H, m) , 3.42-3.82 (3H, m) , 4.72 (2 x 1/6H, d, J=16Hz) , 4.73 (2 x 1/3H, d, J=15Hz), 4.82 (2 x 1/6H, d, J=16Hz) , 4.93 (2 x 1/3H, d, J=15Hz), 5.15-5.32 (IH, m) , 7.10-7.23 (5H, m) , 7.72-7.80 (2H, m) , 7.90-8.03 <2H, m) , 8.06-8.13 (IH, m) , 8.73 (1 x 1/5H, s) , 8.80 (1 x 4/5H, s) (20) MASS : 469 (M+l) NMR (CDC1 3 , δ) : 2.73-3.09 (2H, m) , 2.91 (3 x 4/5H, s), 2.97 (3 x 1/5H, s) , 3.11-3.30 (2H, m) , 3.67 (1 x 1/5H, dd, J=8, 4Hz) , 3.79 (1 x 4/5H, dd, J=8, 4Hz), 4.67 (2 x 1/3H, d, J=15Hz) , 4.68 (2 x 1/6H, d, J=16Hz), 4.89 (2 x 1/6H, d, J=16Hz) , 4.93 (2 x 1/3H, d, J=15Hz), 5.16-5.31 (IH, m) , 7.08-7.22 (7H, m) , 7.52-7.63 (IH, m) , 7.72-7.80 (2H, m) , 7.97-8.03 (IH, m) , 8.08-8.14 (IH, m) , 8.17-8.26 (IH, m) , 8.48-8.53 (IH, m) , 8.68 (1 x 1/5H, s) , 8.76 (1 x 4/5H, s) (21) MASS : 458 (M+l) NMR (CDC1 3 , δ) : 2.70-3.20 (3H, m) , 2.91 (3 x 3/4H, s), 2.98 (3 x 1/4H, s) , 3.45-3.65 (2H, m) , 4.70 (2 x 1/6H, d, J=16Hz), 4.73 (2 x 1/3H, d, J=15Hz) , 4.83 (2 x 1/6H, d, J=16Hz) , 4.89 (2 x 1/3H, d, J=15Hz), 5.12-5.32 (IH, m) , 4.72 (1 x 1/4H, s) , 4.89 (1 x 3/4H, s) , 6.72 (1 x 1/4H, s) , 6.80 (1 x 3/4H, s), 7.05-7.23 (5H, m) , 7.49 (1 x 1/4H, s), 7.52 (1 x 3/4H, s), 7.71-7.80 (2H, m) , 7.96-8.07 (IH, m) , 8.08-8.13 (IH, m) , 8.72 (1 x 1/4H, s) , 8.78 (1 x 3/4H, s) (22) MASS : 434 (M+l) NMR (CDC1 3 , δ) : 2.78 (3 x 2/3H, s) , 2.89 (3 x 1/3H, s), 2.96-3.18 (2H, m) , 3.33 (1 x 1/3H, t, J=8Hz) , 3.42 (1 x 2/3H, t, J=8Hz) , 3.52-3.67 (IH, m) , 3.71- 3.81 (IH, m) , 4.35 (2 x 1/6H, d, J=16Hz) , 4.42 (2 x 1/3H, d, J=15Hz), 4.51 (2 x 1/6H, d, J=16Hz) , 4.71 (2 x 1/3H, d, J=15Hz), 5.11-5.19 (IH, m) , 7.11-7.33 (6H, m) , 7.56 (IH, dd, J=8, 2Hz), 7.81 (IH, t, J=8Hz), 7.94 (IH, d, J=8Hz) , 8.29-8.42 (2H, m) , 8.49 (IH, s), 8.63-8.70 (IH, m) (23) MASS : 495 (M+l) NMR (CDC1 3 , δ) : 2.77 (3 x 4/5H, s), 2.81 (3 x 1/5H, s), 2.86-3.14 (3H, m) , 3.20-3.32 (IH, m) , 3.70-3.82 (IH, m), 4.35 (2 x 1/6H, d, J=16Hz) , 4.40 (2 x 1/3H, d, J=15Hz), 4.43 (2 x 1/6H, d, J=16Hz) , 4.63 (2 x 1/3H, d, J=15Hz), 5.11-5.23 (IH, m) , 7.10-7.32 (7H, m), 7.40 (IH, dd, J=8, 4Hz) , 7.48 (IH, dd, J=8, 2Hz), 7.56-7.70 (2H, m) , 8.18-8.32 (2H, m) , 8.40 (1 x 1/5H, s) , 8.49 (1 x 4/5H, s) , 8.51 (IH, d, J=2Hz), 8.63 (IH, d, J=8Hz) , 8.19 (IH, s) (24) MASS : 434 (M+l) NMR (CDC1 3 , δ) : 2.79 (3 x 3/4H, s) , 2.88 (3 x 1/4H, s), 2.96-3.18 (2H, m) , 3.33-3.45 (IH, m) , 3.52-3.67 (IH, m) , 3.74-3.83 (IH, m) , 4.30 (2 x 1/6H, d, J=16Hz), 4.48 (2 x 1/3H, d, J=15Hz) , 4.49 (2 x 1/6H, d, J=16Hz), 4.66 (2 x 1/3H, d, J=15Hz) , 5.12- 5.25 (IH, m) , 7.12-7.30 (4H, ) , 7.38-7.43 (2H, m) , 7.55 (IH, dd, J=8, 2Hz) , 7.68 (IH, t, J=8Hz) , 7.92 (IH, d, J=8Hz), 8.29-8.33 (IH, m) , 8.44 (1 x 1/4H, s), 8.53 (1 x 3/4H, s) , 8.67 (IH, d, J=5Hz) , 9.16- 9.20 (IH, m) (25) MASS (m/z) : 637 (M + +l) (26) NMR (CDC1 3 , δ) : 2.52 (IH x 1/4, dd, J=8, 14Hz), 2.65 (IH x 3/4, dd, J=8, 14Hz) , 2.70 (3H x 3/4, s) , 2.82 (3H x 1/4, s), 3.01 (2H, m) , 3.15 (IH x 1/4, dd, J=4, 14Hz), 3.21 (IH x 3/4, dd, J=4, 14Hz) , 3.53 (IH x 1/4, dd, J=4, 8Hz) , 3.60 (IH x 3/4, dd, J=4, 8Hz), 4.29 (IH x 1/4, d, J=16Hz) , 4.32 (IH x 3/4, d, J=15Hz), 4.40 (IH x 1/4, d, J=16Hz), 4.66 (IH x 3/4, d, J=15Hz), 5.17 (IH, q, J=7Hz) , 7.13-7.40 (12H, m) , 7.98 (IH, m) , 8.30 (IH x 1/4, d, J=2Hz), 8.41 (IH x 3/4, d, J=2Hz) , 8.52 (IH, m) (27) NMR (CDC1 3 , δ) : 2.53-2.67 (IH, m) , 2.71 (3H x 3/4, s), 2.83 (3H x 1/4, s) , 2.94-3.21 (3H, ) , 3.56 (IH x 1/3, dd, J=4, 9Hz), 3.64 (IH x 2/3, dd, J=4, 12Hz), 4.25 (IH x 1/4, d, J=16Hz), 4.34 (IH x 3/4, d, J=15Hz), 4.42 (IH x 1/4, d, J=16Hz) , 4.64 (IH x 3/4, d, J=15Hz), 5.17 (IH, m) , 7.08-7.42 (9H, m) , 7.97 (IH, d, J=8Hz), 8.31 (IH x 1/4, br s) , 8.43 (IH x 3/4, br s), 8.53 (2H, d, J=5Hz) (28) NMR (CDC1 3 , δ) : 2.78 (3H x 3/4, s), 2.88 (3H x 1/4, s), 2.99 (IH, m) , 3.11 (IH, m) , 3.36 (IH x 1/4, t, J=5Hz), 3.43 (IH x 3/4, t, J=5Hz) , 3.58 (IH, m) , 3.78 (IH, ) , 4.35 (IH x 1/4, d, J=15Hz) , 4.47 (IH x 3/4, d, J=15Hz), 4.48 (IH x 1/4, d, J=15Hz) , 4.66 (IH x 3/4, d, J=15Hz), 7.13-7.28 (7H, m) , 7.60 (2H, d, J=8Hz), 7.93 (IH, d, J=8Hz) , 8.11 (IH, s) , 8.53 (IH, s) (29) mp : 96-99 β C MASS (m/z) : 415 (M+l) + NMR (CDC1 3 , δ) : 1.70 (IH, m) , 2.05 (IH, m) , 2.07 (3H x 1/4, s), 2.09 (3H x 3/4, s), 2.43-2.58 (2H, m) , 2.52 (3H x 1/4, s) , 2.55 (3H x 3/4, s) , 2.70 (3H x 3/4, s), 2.81 (3H x 1/4, s) , 2.92-3.15 (2H, m) , 3.38-3.52 (IH, m) , 4.21 (IH x 1/4, d, J=14.5Hz), 4.32 (IH x 3/4, d, J=14.5Hz), 4.39 (IH x 1/4, d, J=14.5Hz), 4.60 (IH x 3/4, d, J=14.5Hz), 5.10-5.27 (IH, m) , 7.01-7.10 (IH, m) , 7.11-7.34 (6H, m) , 7.90 (IH, d, J=9.0Hz), 8.21 (IH x 1/4, d, J=1.5Hz), 8.30 (IH x 3/4, d, J=1.5Hz) (30) MASS (m/z) : 401 (M+l) ÷ NMR (CDC1 3 , δ) : 1.73 (IH, m) , 2.07 (3H x 1/4, s) , 2.10 (3H x 3/4, s), 1.99-2.16 (IH, m) , 2.48 (2H x 1/4, t, J=7.5Hz), 2.53 (2H x 3/4, t, J=7.5Hz), 2.72 (3H x 3/4, s), 2.84 (3H x 1/4, s), 2.94-3.12 (2H, m) , 3.38-3.44 (IH x 1/4, m) , 3.46-3.52 (IH x 3/4, m) , 4.31 (IH x 1/4, d, J=14.5Hz), 4.35 (IH x 3/4, d, J=14.5Hz), 4.41 (IH x 1/4, d, J=14.5Hz), 4.65 (IH x 3/4, d, J=14.5Hz), 5.12-5.23 (IH, m) , 7.12-7.30 (8H, m) , 7.38-7.44 (IH, m) , 7.93 (IH, d, J=8.5Hz), 8.31 (IH x 1/4, d, J=1.5Hz), 8.43 (IH x 3/4, d, J=1.5Hz), 8.49-8.56 (IH, m) (31) MASS (m/z) : 451 (M+l) τ NMR (CDC1 3 , δ) : 1.65-1.79 (IK, m) , 1.98-2.14 (IH, ) , 2.05 (3H x 1/4, s), 2.10 (3H x 3/4, s) , 2.47 (2H x 1/4, t, J=7.5Hz), 2.53 (2H x 3/4, t, J=7.5Hz), 2.78 (3H x 3/4, s), 2.92 (3H x 1/4, s) , 2.96-3.17 (2H, m) , 3.39 (IH x 1/4, dd, J=7.5, 4.5Hz), 3.50 (IH x 3/4, dd, J=7.5, 4.5Hz), 4.52 (IH x 1/4, d, J=14.5Hz), 4.53 (IH x 3/4, d, J=14.5Hz), 4.62 (IH x 1/4, d, J=14.5Hz), 4.82 (IH x 3/4, d, J=14.5Hz), 5.13-5.32 (IH, ) , 7.11-7.25 (5H, m) , 7.51-7.60 (IH, ) , 7.67-7.98 (4H, m) , 8.09 (IH x 1/4, d, J=7.5Hz), 8.11 (IH x 3/4, d, J=7.5Hz), 8.66 (IH x 1/4, d, J=I.5Hz), 8.78 (IH x 3/4, α, J=1.5Hz) (32) mp : 110-lil"C MASS (m/z) : 452 (M+lA NMR (CDC1 3 , δ) : 1.63-1.78 (IH, m) , 1.99-2.12 (IH, ) , 2.02 (3H x 1/5, s), 2.08 (3H x 4/5, s) , 2.39 (2H x 1/5, t, J=7.5Hz), 2.52 (2H x 4/5, t, J=7.5Hz), 2.94 (3H x 4/5, s), 2.97-3.28 (2H, m) , 3.01 (3H x 1/5, s), 3.38 (IH x 1/5, dd, J=7.5, 5.5Hz), 3.50 (IH x 4/5, dd, J=7.5, 5.5Hz), 4.69 (IH, d, J=14.5Hz), 4.95 (IH x 1/5, d, J=14.5Hz), 4.98 (IH x 4/5, d, J=14.5Hz), 5.17-5.33 (IH, m) , 7.11-7.23 (5H, m) , 7.74-7.81 (2H, m) , 7.87-7.96 (IH, m) , 7.99-8.04 (IH, m) , 8.08-8.15 (IH, m) , 8.70 (IH x 1/5, s), 8.80 (IH x 4/5, s) (33) MASS (m/z) : 478 (M+l) + NMR (CDC1 3 , δ) : 1.63-1.80 (IH, m) , 1.99-2.14 (IH, m) , 2.08 (3H x 1/4, s), 2.10 (3H x 3/4, s) , 2.49 (2H x 1/4, t, J=7.5Hz), 2.53 (2H x 3/4, t, J=7.5Hz), 2.78 (3H x 3/4, s), 2.88 (3H x 1/4, s) , 2.93-3.20 (2H, m) , 3.44 (IH x 1/4, dd, J=7.5, 4.5Hz), 3.51 (IH x 3/4, dd, J=7.5, 4.5Hz), 4.37 (IH x 1/4, d, J=14.5Hz), 4.43 (IH x 1/4, d, J=14.5Hz), 4.47 (IH x 3/4, d, J=14.5Hz), 4.67 (IH x 3/4, d, J=14.5Hz), 5.13-5.27 (IH, ) , 7.14-7.38 (21/4H, m) , 7.41 (IH, dd, J=8.5, 5.5Hz), 7.51 (IH x 3/4, dd, J=8.5, 1.5Hz), 7.65 (IH x 1/4, d, J=7.5Hz), 7.68 (IH x 3/4, d, J=7.5Hz), 7.88-8.01 (IH, m) , 8.31 (IH, dd, J=8.5, 1.5Hz), 8.42 (IH x 1/4, d, J=1.5Hz), 8.53 (IH x 3/4, d, J=1.5Hz), 8.67 (IH, d, J=5.5Hz), 9.17 (IH x 1/4, d, J=1.5Hz), 9.20 (IH x 3/4, d, J=1.5Hz) (34) MASS (m/z) : 422 (M+l) + NMR (CDC1 3 , δ) : 2.69 (3H x 2/3, s) , 2.87 (3H x 1/3, s), 2.93-3.09 (3H, m) , 3.26 (IH x 1/3, dd, J=14.5, 4.5Hz), 3.31 (IH x 2/3, dd, J=14.5, 4.5Hz), 3.49 (IH x 1/3, dd, J=8.5, 4.5Hz), 3.59 (IH x 2/3, dd, J=8.5, 4.5Hz), 4.29 (IH x 1/3, d, J=14.5Hz), 4.33 (IH x 2/3, d, J=14.5Hz), 4.40 (IH x 1/3, d. J=14.5Hz), 4.67 (IH x 2/3, d, J=14.5Hz), 5.20 (IH, q, J=7.5Hz), 6.78-7.02 (3H, m) , 7.05-7.33 (10H, m) , 7.94 (IH x 1/3, br d, J=8.5Hz), 8.C2 (IH x 2/3, br d, J=8.5Hz) (35) MASS (m/z) : 400 (M+H) + NMR (CDC1 3 , δ) : 2.69 (2/3 x 3H, s), 2.81 (1/3 x 3H, s), 2.86-3.10 (2H, m) , 3.06 (1/3 x 6H, s), 3.08 (2/3 x 6H, s), 3.34-3.82 (3H, m) , 3.92 (1/3 x IH, d, J=17Hz), 4.35 (2/3 x 2K, ABq, J=15Hz) , 4.36 (1/3 x IH, d, J=17Hz), 5.02-5.35 (IH, m) , 6.44 (1/3 x IH, d, J=9Hz), 6.47 (2/3 x IH, d, J=9Hz), 7.06-7.36 (6H, m) , 7.80-8.04 (2H, ) (36) MASS (m/z) : 497 (M+H) + NMR (CDC1 3 , δ) : 2.74 (3/4 x 3H, s) , 2.90 (1/4 x 3H, s), 2.92-3.20 (2H, m) , 3.44-3.75 (3K, m) , 4.42-4.88 (4H, m) , 5.10-5.30 (IH, m) , 7.03-8.23 (16H, m) , 8.62 (1/4 x IH, d, J=2Hz) , 8.77 (3/4 x IH, d, J=2Hz) (37) MASS (m/z) : 406 (M+H) + NMR (CDC1 3 , δ) : 2.46-2.69 (IH, m) , 2.68 (2/3 x 3H, s), 2.77-3.10 (3H, ) , 2.87 (1/3 x 3H, s), 3.38- 3.58 (IH, m) , 4.33 (2/3 x IH, d, J=15Hz) , 4.36 (1/3 x 2H, ABq, , 4.67 (2/3 x IH, d, J=15Hz), 5.12-5.26 (IH, m) , 6.21 (1/3 x IH, s) , 6.27 (2/3 x IH, s), 6.95-7.40 (12H, m) , 7.86-8.05 (IH, m) (38) MASS (m/z) : 406 (M+H) + NMR (CDC1 3 , δ) : 2.61-2.84 (IH, m) , 2.66 (2/3 x 3H, s), 2.86 (1/3 x 3H, s), 2.89-3.20 (3H, m) , 3.50- 3.68 (IH, m) , 4.32 (2/3 x IH, d, J=15Hz) , 4.34 (1/3 x 2H, ABq, Δ=0.22, J=17HZ) , 4.67 (2/3 x IH, d, J=15Hz), 5.12-5.26 (IH, m) , 6.04 (1/3 x IH, d, J=2Hz), 6.10 (2/3 x IH, d, J=2Hz), 6.24-6.32 (IH, m) , 6.93-7.38 (11H, m) , 7.98 (1/3 x IH, d, J=8Hz), 8.05 (2/3 x IH, d, J=8Hz) (39) MASS : 387 (M+l) NMR (CDC1 3 , δ) : 2.71 (3 x 3/4H, s) , 2.81 (3 x 1/4H, s), 2.90-3.13 (2H, m) , 3.33-3.43 (IH, ) , 3.51-3. (IH, m) , 3.70-3.81 (IH, m) , 3.89 (3H, s), 4.09 (2 1/6H, d, J=16Hz), 4.29 (2 x 1/3H, d, J=15Hz), 4.3 (2 x 1/3H, d, J=15Hz), 4.53 (2 x 1/6K, d, J=16Hz), 5.08-5.29 (IH, ) , 6.68 (1 x 1/4K, d, J=8Hz), 6.6 (1 x 3/4H, d, J=8Hz), 7.10-7.30 (5H, m) , 7.38 (IH, d, J=8Hz), 7.90 (IH, s), 7.91 (1 x 1/4H, s) , 7.98 (1 x 3/4H, s) (40) MASS : 457 (M+l) NMR (CDC1 3 , δ) : 2.72 (3 x 3/4H, s), 2.87 (3 x 1/4H, s), 2.89-3.12 (4H, m) , 3.50-3.70 (IH, m) , 4.40 (2 1/6H, d, J=16Hz), 4.60 (2 x 1/6H, d, J=16Hz), 4.6 (2 x 1/3H, d, J=15Hz), 4.68 (2 x I/3H, d, J=15Hz), 5.05-5.30 (IH, m) , 6.81 (IH, s), 7.03-7.23 (5H, m) 7.48-7.60 (2H, m) , 7.67-7.81 (2H, m) , 7.91 (IH, s) 8.00-8.20 (2H, m) , 8.68 (1 x 1/4H, s) , 8.72 (1 x 3/4H, s) (41) MASS : 484 (M+l) NMR (CDC1 3 , δ) : 2.77 (3 x 2/3H, s) , 2.87 (3 x 1/3H, s), 2.81-3.20 (4H, m) , 3.58-3.70 (IH, ) , 4.30 (2 1/6H, d, J=16Hz), 4.48 (2 x 1/6H, d, J=16Hz) , 4.5 (2 x 1/3H, d, J=15Hz), 4.58 (2 x 1/3H, d, J=15Hz), 5.08-5.22 (IH, m) , 6.78-6.88 (IH, ) , 7.10-7.31 (5H, m) , 7.33-7.46 (IH, ) , 7.49-7.60 (2K, ) , 7.61-7.70 (IH, m) , 8.00-8.10 (IH, ) , 8.23-8.33 (IH, m) , 8.41 (1 x 1/4H, s), 8.51 (1 x 3/4H, s), 8 . 65 ( IH, s ) , 9 . 17 ( IH, s ) ( 42 ) MASS : 446 (M+l ) NMR (CDC1 3 , δ) : 2.38-2.60 (IH, m) , 2.69 (3 x 2/3H, s), 2.83 (3 x 1/3H, s ) , 2.90-3.15 (3H, m) , 3.40- 3.60 (IH, ) , 3.78 (3H, s) , 4.31 (2 x 1/6H, d, J=16Hz), 4.32 (2 x 1/3H, d, J=15Hz) , 4.41 (2 x 1/6H, d, J=16H∑), 4.69 (2 x 1/3H, d, J=15Hz) , 5.13- 5.26 (IH, m) , 6.80-6.90 (2H, m) , 6.95-7.32 (12K, m) , 7.90 (1 x 1/3H, d, J=8Hz) , 7.99 (1 x 2/3H, d, J=8Hz) (43) MASS : 469 (M+l) NMR (CDC1 3 , δ) : 2.77 (3 x 2/3H, s) , 2.90 (3 x 1/3H, s), 2.82-3.12 (3H, m) , 3.14-3.31 (IK, m) , 3.65-3.72 (1 x 1/3H, m), 3.78-3.85 (1 x 2/3H, m) , 4.52 (2 x 1/6H, d, J=16Hz), 4.61 (2 x 1/6H, d, J=16Hz), 4.62 (2 x 1/3H, d, J=15Hz), 4.80 (2 x 1/3H, d, J=15Hz) , 5.16-5.28 (IH, m) , 7.10-7.33 (7H, m) , 7.43 (IH, d, J=8Hz), 7.53-7.65 (IH, m) , 7.77 (1 x 1/3H, s), 7.83 (1 x 2/3H, s), 8.01 (IH, d, J=8Hz) , 8.23 (IH, t, J=8Hz), 8.49-8.58 (IH, m) , 8.83 (2H, s) (44) MASS : 466 (M+l) NMR (CDC1 3 , δ) : 2.53-2.81 (IH, m) , 2.78 (3 x 2/3H, s), 2.89 (3 x 1/3H, s) , 2.93-3.13 (2K, m) , 3.62- 3.90 (2H, m) , 4.30 (2 x 1/3H, d, J=15Hz) , 4.41 (2 x 1/3H, s), 4.71 (2 x 1/3H, d, J=15Hz) , 5.20-5.29 (IH, m) , 7.00-7.10 (2H, ) , 7.12-7.33 (9H, m) , 7.36-7.43 (IH, m) , 7.45-7.60 (2H, m) , 7.77 (IH, d, J=8Hz), 7.85 (IH, d, J=8Hz) , 7.98-8.22 (2H, ) (45) MASS : 407 (M+l) NMR (CDC1 3 , δ) : 2.70 (3 x 3/4H, s), 2.81 (3 x 1/4H, s), 2.78-3.10 (4H, m) , 3.47-3.65 (IH, m) , 4.22 (2 x 1/8H, d, J=16Hz), 4.41 (2 x 3/8H, d, J=15Hz) , 4.52 (2 x 3/8H, d, J=15Hz), 4.63 (2 x 1/8H, d, J=16Hz) , 5.07-5.20 (IH, m) , 6.72-6.85 (IH, m) , 7.09-7.31 (6H, m) , 7.41 (IH, d, J=7Hz), 7.47-7.60 (IH, m) , 7.97-8.05 (IH, m) , 8.31 (1 x 1/4H, s) , 8.39 (1 x 3/4H, s), 8.43 (1 x 1/4H, s), 8.51 (1 x 3/4H, s) (46) MASS : 432 (M+l) NMR (CDC1 3 , δ) : 2.52 (3H, s) , 2.67 (3 x 3/4H, s), 2.78 (3 x 1/4H, s) , 2.80-3.10 (3H, m) , 3.18-3.30 (IH, m) , 3.68-3.80 (IH, m) , 4.19 (2 x 1/8H, d, J=16Hz), 4.28 (2 x 3/8H, d, J=15Hz), 4.33 (2 x 1/8H, d, J=16Hz), 4.58 (2 x 3/8H, d, J=15Hz), 5.09- 5.22 (IH, m) , 6.99-7.30 (9H, m) , 7.61 (IH, t, J=8Hz), 8.19 (IH, s), 8.21 (1 x 1/4H, s), 8.29 (1 x 3/4H, s), 8.49-8.53 (IH, m) (47) MASS : 417 (M+l) NMR (CDCI3, δ) : 2.49-2.73 (IH, m) , 2.70 (3 x 2/3H, s), 2.89 (3 x 1/3H, s), 2.91-3.22 (3H, m) , 3.48- 3.53 (1 x 1/3H, m) , 3.55-3.63 (1 x 2/3H, m) , 4.31 (2 x 1/6H, d, J=16Hz), 4.33 (2 x 1/3H, d, J=15Hz) , 4.41 (2 x 1/6H, d, J=16Hz), 4.68 (2 x 1/3H, d, J=15Hz), 5.12-5.26 (IH, m) , 6.98-7.35 (11H, m) , 7.48 (1 x 1/3H, d, J=8Hz) , 7.52 (1 x 2/3H, d, J=8Hz), 7.88 (1 x 1/3H, d, J=8Hz) , 7.92 (1 x 2/3H, d, J=8Hz), 8.42 (1 x 1/3H, s), 8.48 (1 x 2/3H, s), 8.50 (IH, s) (43) MASS : 450 (M+l) NMR (CDCI3, δ) : 2.43-2.68 (IK, m) , 2.69 (3 x 2/3H, s), 2.88 (3 x 1/3H, s) , 2.90-3.18 (3H, ) , 3.42- 3.50 (1 x 1/3H, m) , 3.52-3.60 (1 x 2/3H, ) , 4.31 (2 x 1/6H, d, J=16Hz), 4.32 (2 x 1/3H, d, J=15Hz), 4.41 (2 x 1/6H, d, J=16Hz) , 4.69 (2 x 1/3H, d, J=15Hz) , 5.12-5.23 (IH, m) , 6.97-7.43 (14H, m) , 7.87 (1 x 1/3H, d, J=8Hz) , 7.94 (1 x 2/3H, d, J=8Hz) (49) MASS : 428 (M+l) NMR (CDC1 3 , δ) : 2.52-2.78 (IH, ) , 2.69 (3 x 2/3H, s) , 2.70-3.12 (3H, m) , 2.89 (3 x 1/3H, s) , 3.38- 3.49 (1 x 1/3H, m) , 4.49-3.58 (1 x 2/3H, m) , 3.80- 4.04 (2H, m) , 4.33 (2 x 1/3H, d, J=15Hz) , 4.41 (2 x 1/3H, s) , 4.69 (2 x 1/3H, d, J=15Hz) , 5.14-5.27 (IH, m) , 6.93-7.33 (14K, m) , 7.87 (1 x I/3H, d, J=8Hz) , 7.93 (1 x 2/3H, d, J=8Hz) Preparation 62 The following object compounds were obtained by reacting each Starting compound with di-tert-butyl-dicarbonate in a conventional manner. (1) MASS : 236 (M+l) NMR (CDC1 3 , δ) : 1.45 (9H, s) , 2.14 (3H, s), 2.93-3.03 (2H, m) , 4.48-4.58 (IH, m) , 5.41 (IH, br s) (2) mp : 50-53°C MASS : 222 (M+l) NMR (CDC1 3 , δ) : 1.46 (9H, s), 2.32 (3H, s), 4.31 (2H, d, J=6Hz), 4.68 (IK, br s), 7.12-7.27 (4K, m) (3) MASS : 222 (M+l) NMR (CDCI3, δ) : 1.42 (9H, s) , 2.33 (3H, s) , 4.28 (2K, d, J=8Hz), 4.72 (IH, br s) , 7.07 (2K, d, J=8Hz) , 7.09 (IH, s), 7.23 (IK, dd, J=15, 8Hz) Preparation 63 The following object compounds were obtained according to a similar manner to that of Preparation 1, 6, 11, 33, 52 or 56. (1) MASS : 419 (M+l) NMR (CDC1 3 , δ) : 1.38 (9 x 1/3H, s), 1.42 (9 x 2/3H, s), 2.60 (3 x 2/3H, s), 2.81 (3 x 1/3H, s), 3.07- 3.22 (2H, m) , 4.14 (2 x 1/6H, d, J=16Hz) , 4.32 (2 1/6H, d, J=16Hz), 4.36 (2 x 1/3H, d, J=15Hz), 4.59 (2 x 1/3H, d, J=15Hz), 4.92-5.06 (IH, m) , 5.37 (1 1/3H, d, J=10Hz), 5.45 (1 x 2/3H, d, J=10Hz), 6.82 (2 x 1/3H, d, J=8Hz), 6.92 (2 x 2/3H, d, J=8Hz) , 7.02-7.21 (3H, m) , 7.27 (1 x 1/3H, d, J=8Hz), 7.32 (1 x 2/3H, d, J=8Hz) , 7.40-7.50 (2H, m) , 7.60 (1 x 1/3H, s), 7.63 (1 x 2/3H, s), 7.69-7.82 (3H, m) (2) MASS : 383 (M+l) NMR (CDCI3, δ) : 1.08 (9 x 2/9H, s), 1.19 { 9 x 4/9H, s), 1.32 (9 x 3/9H, s), 2.79-2.93 (6H, m) , 2.93- 3.29 (2H, m) , 4.37-4.75 (2H, m) , 4.97-5.08 (1 x 1/2H, m) , 5.30-5.45 (1 x 1/2H, m) , 6.90-7.00 (IH, m) , 7.03-7.40 (9H, m) (3) MASS : 399 (M+l) NMR (CDCI3, δ) : 1.38 (9 x 1/4H, s) , 1.40 (9 x 3/4H, s), 2.61 (3 x 3/4H, s), 2.81 (3 x 1/4H, s), 2.92 (IH, d, J=8Hz), 3.77 (3 x 3/4H, s) , 3.79 (3 x 1/4H s) , 4.17 (2 x 1/6H, d, J=16Hz) , 4.37 (2 x I/6H, d, J=16Hz), 4.40 (2 x 1/3H, d, J=15Hz) , 4.59 [ 2 x 1/3H, d, J=15Hz), 4.78-4.90 (IH, m) , 5.31 ;i x 1/4H, d, J=8Hz), 5.40 (1 x 3/4H, d, J=8Hz) , 6.70- 6.82 (2H, ) , 6.92-7.13 (4H, m) , 7.20-7.32 (3H, m) (4) MASS : 383 (M+l) NMR (CDCI3, δ) : 1.39 (9 x 1/3H, s) , 1.41 (9 x 2/3H, s), 2.30 (3 x 1/3H, s), 2.32 (3 x 2/3H, s) , 2.59 ( x 1/3H, s) , 2.82 (3 x 2/3H, s) , 2.97-3.03 (2H, m) , 4.00 (2 x 1/6H, d, J=16Hz), 4.37 (2 x 1/6H, d, J-16HZ), 4.42 (2 x 1/3H, d, J=15Hz) , 4.49 (2 x 1/3H, d, J=15Hz), 4.82-4.97 (IK, m) , 5.32-5.43 (IH, m) , 6.77-7.30 (9H, m) (5) MASS : 383 (M+l) NMR (CDC1 3 , δ) : 1.38 (9 x 1/3H, s) , 1.41 (9 x 2/3H, s), 2.13 (3 x 1/3H, s), 2.22 (3 x 2/3H, s), 2.63 (3 x 2/3H, s), 2.87 (3 x 1/3H, s), 2.97-3.08 (2H, m) , 3.99 (2 x 1/6H, d, J=16Hz) , 4.22 (2 x 1/6H, d, J=16Hz) , 4.41 (2 x 1/3H, d, J=15Hz) , 4.62 (2 x 1/3H, d, J=15Hz), 4.70-4.79 (1 x 1/3H, m) , 4.88- 4.96 (1 x 2/3H, m) , 5.38 (IH, t, J=8Hz) , 6.78 (1 x 1/3H, d, J=8Hz), 6.82 (1 x 2/3H, d, J=8Hz) , 7.05- 7.18 (4H, m) , 7.22-7.32 (4H, m) (6) MASS : 371 (M+l) NMR (CDCI3, δ) : 1.38 (9 x 1/3H, s) , 1.40 (9 x 2/3H, s), 2.83 (3 x 4/5H, s), 2.90 (3 x 1/5H, s) , 2.93- 3.12 (2H, m) , 4.52 (2 x 1/2H, d, J=15Hz), 4.61 (2 x 1/2H, d, J=15Hz), 4.89-4.97 (IH, ) , 5.29-5.33 (IH, m) , 6.80 (1 x 1/5H, d, J=5Hz) , 6.92 (1 x 4/5H, d, J=5Hz), 7.12-7.31 (5H, m) , 8.57 (1 x 1/5H, d, J=5Hz) , 8.59 (1 x 4/5H, d, J=5Hz) , 9.10 (IH, s) (7) MASS : 421 (M+l) NMR (CDCI3, δ) : 1.31 (9 x 1/3H, s) , 1.40 (9 x 2/3H, S), 2.85 (3 x 5/6H, s), 2.94 (3 x 1/6H, s) , 2.98- 3.15 (2H, m) , 4.55 (2 x 1/6H, d, J=16H∑) , 4.68 (2 x 1/6H, d, J=16Hz), 4.73 (2 x 1/3H, d, J=15Hz) , 4.88 (2 x 1/3H, d, J=15Hz), 4.88-5.02 (IH, m) , 5.32-5.42 (IH, m) , 7.10-7.23 (5H, m) , 7.70-7.80 (2H, ) , 7.97-8.03 (IH, m) , 8.07-8.13 (IH, ) , 8.61 (1 x 1/4H, s) , 8.78 (1 x 3/4H, s) (8) MASS : 420 (M+l) NMR (CDC1 3 , δ) : 1.34 (9 x 1/3H, s), 1.39 (9 x 2/3H, s), 2.80 (3 x 3/4H, s) , 2.92 (3 x 1/4H, s) , 2.98- 3.18 (2H, m), 4.51 (2 x 1/6H, d, J=16Hz) , 4.63 (2 x 1/6H, d, J=16Hz), 4.81 (2 x 2/3H, s) , 4.90-5.04 (IH, m) , 5.34-5.43 (IH, m) , 7.09-7.29 (6H, m) , 7.51 (IH, t, J=8Hz), 7.69 (IH, t, J=8Hz) , 7.79 (IH, d, J=8Hz), 8.01 (IH, d, J=8Hz), 8.07 (IH, d, J=8Hz) (9) MASS : 420 (M+l) NMR (CDC1 3 , δ) : 1.39 (9 x 1/4H, s) , 1.45 (9 x 3/4H, s), 2.68 (3 x 3/4H, s) , 2.88 (3 x 1/4H, s) , 2.97- 3.05 (2H, m) , 4.25 (2 x 1/6H, d, J=16Hz) , 4.58 (2 x 1/6H, d, J=16Hz), 4.68 (2 x 1/3H, d, J=15Hz) , 4.72 (2 x 1/3H, d, J=15Hz), 4.82-5.00 (IH, m) , 5.33-5.47 (IH, ) , 7.08-7.32 (6H, ) , 7.37-7.42 (IH, m) , 7.70-7.80 (IH, m) , 7.88 (IH, s) , 8.13 (IH, d, J=8Hz), 8.88-8.92 (IH, m) (10) MASS : 371 (M+l) NMR (CDC1 3 , δ) : 1.40 (9 x 1/3H, s) , 1.42 (9 x 2/3H, S), 2.81 (3 x 5/6H, s) , 2.90 (3 x 1/6H, s) , 2.93- 3.08 (2H, m) , 4.38 (2 x 1/6H, d, J=16Hz) , 4.44 (2 x 1/6H, d, J=16Hz), 4.58 (2 x 1/3H, d, J=15Hz) , 4.68 (2 x 1/3H, d, J=15Hz) , 4.83-4.93 (IH, m) , 5.29-5.40 (IH, m) , 7.13-7.28 (5H, m) , 8.43-8.50 (3H, m) (11) MASS : 447 (M+l) NMR (CDC1 3 , δ) : 1.40 (9 x 1/4H, s) , 1.41 (9 x 3/4H, s), 2.68 (3 x 3/4H, s) , 2.83 (3 x 1/4H, s) , 2.92- 3.12 (2H, m) , 4.16 (2 x 1/6H, d, J=16Hz) , 4.41 (2 x 1/6H, d, J=16Hz), 4.53 (2 x 2/3H, s) , 4.82-4.98 (IH, m) , 5.32-5.42 (IH, m) , 7.12-7.30 (5H, m) , 7.38-7.42 (IH, m) , 7.48-7.52 (IH, m) , 7.62 (1 x 1/4H, d, J=8Hz), 7.68 (1 x 3/4H, d, J=8Hz) , 8.25- 8.32 (IH, m) , 8.40 (1 x 1/4H, s) , 8.51 (1 x 3/4H, s), 8.63 (IH, d, J=5Hz), 9.12-9.20 (IH, m) (12) MASS : 447 (M+l) NMR (CDC1 3 , δ) : 1.40 (9 x 1/4H, s) , 1.42 (9 x 3/4H, s), 2.63 (3 x 1/4H, s), 2.80 (3 x 3/4H, s), 2.93- 3.10 (2H, m) , 4.13 (2 x 1/6H, d, J=16Hz) , 4.42 (2 x 1/6H, d, J=16Hz), 4.49 (2 x 1/3H, d, J=15Hz) , 4.62 (2 x 1/3H, d, J=15Hz), 4.82-4.99 (IH, m) , 5.32-5.41 (IH, m) , 7.15-7.23 (4H, m) , 7.27-7.32 (2H, m) , 7.52 (IH, d, J=8Hz), 7.70-7.76 (IH, m) , 8.25-8.40 (2H, m) , 8.49 (IH, s), 8.68 (IH, d, J=5Hz) (13) MASS (m/z) : 321(M + +1) NMR (CDC1 3 , δ) : 0.89-1.00 (6H, m) , 1.43 (9H, s) , 1.97 (IH, ) , 2.90 (3H x 1/3, s) , 3.02 (3H x 2/3, s) , 4.47 (IH x 2/3, d, J=15Hz), 4.50 (IH x 1/3, d, J=16Hz), 4.53 (IH, m) , 4.70 (IH x 1/3, d, J=16Hz) , 4.74 (IH x 2/3, d, J=15Hz) , 5.32 (IH, m) , 7.21-7.34 (5H, ) (14) MASS (m/z) : 375 (M + +l) NMR (CDC1 3 , δ) : 0.85-2.00 (13H, m) , 1.45 (9H, s) , 2.92 (3H x 1/3, s), 2.98 (3H x 2/3, s) , 4.48 (IH x 2/3, d, J=15Hz), 4.65 (IH x 2/3, d, J=15Hz) , 4.72 (2H x 1/3, s), 4.74 (IH, m) , 5.17 (IH x 1/3, d, J=7Hz), 5.24 (IH x 2/3, d, J=7Hz) , 7.20-7.37 (5H, m) (15) MASS (m/z) : 467 (M + +l) NMR (CDC1 3 , δ) : 1.41 (9H, s) , 2.34 (3H, s) , 2.55 (4H, m) , 2.58 (3H, s) , 2.97 (2H, d, J=7Hz) , 3.18 (4H, m) , 3.98 (IH x 1/3, d, J=16Hz) , 4.30 (IH x 1/3, d, J=16Hz), 4.36 (IH x 2/3, d, J=15Hz) , 4.45 (IH x 2/3, d, J=15Hz), 4.83 (IH x 2/3, q, J=7Hz) , 4.94 (IH x 1/3, q, J=7Hz), 5.37 (IH x 1/3, d, J=7Hz), 5.42 (IH x 2/3, d, J=7Hz) , 6.79-6.90 (3H, m) , 7.02 (IH, d, J=8Hz), 7.13-7.24 (5H, m) (16) MASS (m/z) : 370 (M + +l) NMR (CDC1 3 , δ) : 1.37 (9H x 1/3 s), 1.41 (9H x 2/3, s), 2.77 (3H x 2/3, s), 2.91 (3H x 1/3, sj , 2.88- 3.06 (2K, m) , 4.40 (IH x 4/5, , J=15Kz. , 4.42 (2H x 1/5, s), 4.63 (IH x 4/5, d, J=15Hz) , 4.90 (IH, ) , 5.28 (IH x 1/3, d, J=8Hz) , 5.39 (IH x 2/3, α, J=8Hz), 7.02-7.12 (4H, m) , 7.27-7.32 (3H, no, 8.45 (2H x 4/5, d, J=6Hz), 8.52 (2H x 1/5, d, J=6Hz) (17) MASS (m/z) : 420 (M+H) ~ NMR (CDCI3, δ) : 1.39 (1/5 x 9H, s), 1.45 (4/5 x 9H, s), 2.68 (4/5 x 3H, s), 2.86 (1/5 x 3H, s), 2.92- 3.08 (2H, m) , 4.22 (1/5 x IH, d, J=17Hz) , 4.58 (1/5 x IH, d, J=17Hz), 4.68 (4/5 x 2H, ABq, Δ=0.09, J=15Hz), 4.80-5.05 (IH, m) , 5.30-5.47 (IH, rr.) , 7.06-7.26 (5H, si), 7.50-8.15 (5H, n) , 6.62 (1/5 x IH, s) , 8.76 (4/5 x IK, s) (18) MASS (m/z) : 420 (M+H) + NMR (CDCI3, δ) : 1.38 (1/4 x 9H, s) , 1.43 (3/4 x 9H, s), 2.68 (3/4 x 3H, s), 2.83 (1/4 x 3H, s) , 2.92- 3.12 (2H, m) , 4.40 (1/4 x 2H, ABq, Δ=0.24, J=17Hz) , 4.68 (3/4 x 2H, ABq, J=15HZ) , 4.83-5.02 (IH, m) , 5.28-5.48 (IH, m) , 7.08-7.62 (8H, rc.) , 7.96-8.15 (2K, ) , 8.90 (IH, a, J=2Hz) (19) MASS (m/z) : 427 (M+H) " " NMR {CDCI3, δ) : 1.42 (9H, s), 2.21 (3H, s,, 2.62 (4/5 x 3H, s), 2.76 (1/5 x 3H, s), 2.89-3.08 (2H, ) , 3.99 (1/5 x IH, d, J=17Hz) , 4.32 (1/5 x IH, d, J=17Hz), 4.43 (4/5 x 2H, ABq, Δ=0.15, J=15Hz, , 4.77-5.00 (IH, m) , 5.51 (IH, br d, , 7.06-7.43 (6H, m) , 7.92-8.28 (3K, m) (20) MASS (m/z) : 449 (M+H) ~ NMR (CDC1 3 , δ) : 1.39 (1/3 x 9H, s), 1.43 (2/3 x 9H, s), 2.61 (2/3 x 3H, s), 2.62 (1/3 v. 3H, ≤), 2.90- 3.08 (2H, m) , 3.95 (3K, s) , 4.11 (1/3 x IH, d, =17Hz), 4.39 (1/3 x IH, d, J=17Hz), 4.51 (2/3 x 2H, ABq, J=15Hz), 4.78-5.02 (IK, ) , 5.30-5.50 (IH, m) , 6.51 (IH, m) , 6.93-7.32 (7H, ) , 7.38 (IH, S) , 7.62-7.78 (2H, m) (21) MASS (m/z) : 413 (M+H) + NMR (CDC1 3 , δ) : 1.41 (9H, s) , 2.56 (3/4 x 3H, s), 2.74 (1/4 x 3H, s), 2.88-3.C4 (2H, m) , 3.05 (1/4 x 6H, s), 3.07 (3/4 x 6H, ε), 3.79 (1/4 x IH, d, J=17Hz), 4.26 (1/4 x IK, d, J=17Hz), 4.32 (3/4 x 2H, ABq, J=15H∑) , 4.72-5.05 (IH, m) , 5.31- 5.45 (IH, m) , 6.40 (1/4 x IH, d, J=9Hz) , 6.45 (3/4 x IH, d, J=9Hz), 7.00-7.33 (6H, m) , 7.86 (1/4 x IH, d, J=2Hz), 7.97 (3/4 x IH, α, J=2Hz) (22) MASS (m/z) : 435 (M+H) + NMR (CDC1 3 , δ) : 1.38 (1/4 x 9H, s), 1.42 (3/4 x 9H, s), 2.67 (3/4 x 3K, s), 2.83 (1/4 x 3H, s), 2.91- 3.11 (2H, in) , 4.25 (1/4 x 2H, ABq, Δ=0.22, J=17HZ) , 4.52 (3/4 x 2H, ABς, J=15Hz), 4.31-4.96 (IH, m) , 5.28-5.44 (IH, m) , 6.98-7.35 (11H, ) , 7.80 (1/4 x IH, S), 7.82 (3/4 x IH, s) (23) MASS (m/z) : 437 (M+H) τ NMR (CDCI3, δ) : 1.39 (1/4 x 9H, s) , 1.42 (3/4 x 9K, s), 2.58 (3/4 X 3H, s), 2.60 (3H, s), 2.81 (1/4 x 3H, s), 2.88-3.07 (2H, m) , 3.71 (3H, s) , 4.12 (1/4 x IH, d, J=17HZ), 4.52 (1/4 x IH, d, J=17Hz), 4.60 (3/4 x 2H, s), 4.75-5.08 (IH, m) , 5.34-5.52 (IH, m) , 6.82-7.50 (8H, m) (24) MASS (m/z) : 359 (M+H'~ NMR (CDC1 3 , δ) : 1.4C [1/4 x 9H, ≤A 1.43 (3/4 x 9H, s), 2.68-2.95 (2H, , 2.86 ;3/4 x 3H, s), 2.90 (1/4 x 3H, s), 4.48 (1/4 x 2H, ABq, J=17Hz), 4.56 (3/4 x 2H, ABq, , 4.75-4.90 (IH, m) , 5.23-5.43 (IH, m) , 6.21 (1/4 x IK, s), 6.28 (3/4 x IH, s), A05-7.4C (7H, m (25) MASS (m/z) : 373 (M+H) ~ NMP (CDC1 3 , δ) : 1.41 (9H, s), 2.62 (3/4 x 3H, s 2.81 (1/4 x 3H, s), 2.88-3.10 (2H, m) , 3.80 (1/4 x 3H, s), 3.86 (3/4 x 3H, s) , 3.90 (1/4 x IH, d, J=17Hz), 4.17 (1/4 x IH, d, J=17Hz), 4.30 (3/4 x 2H, ABq, 4.70-5.02 (IH, m) , 5.28- 5.42 (IH, m) , 7.02-7.35 (7H, m) (26) MASS (m/z) : 403 (M+H) τ NMR (CDCI3, δ) : 1.38 (1/3 x 9H, s), 1.41 (2/3 κ 9H, s), 2.71 (2/3 x 3K, s , 2.81-3.17 >'2H, m) , 2.87 (1/3 x 3H, s), 4.36 (1/3 x 2H, ABq, Δ=0.02, J=17Hz), 4.50 (2/3 x 2K, ABq, J=15Hz) , 4.8 (IH, q, J=3Hz), 5.31 (1/3 x IH, d, J=8Hz), 5.42 (2/3 x IH, d, J=8Hz), 6.90-7.85 (9H, ir.) (27) MASS (m/z) : 359 (M+H) " NMR (CDCI3, δ) : 1.40 (1/4 X 9H, s) , 1.42 (3/4 x 9K, s), 2.80 (3/4 x 3H, s), 2.88 (1/4 x 3K, s > , 2.90- 3.12 (2K, m) , 4.41 (3/4 x IH, d, J=15Hz), 4.43 (1/ x 2H, ABq, ..=0.19, J=17Hz), 4.66 (3/4 x IH, d, J=15Hz), 4.87-5.06 (IH, n) , 5.30-5.51 (IH, m, , 6.0 (IK, s), 6.23 (3/4 x IH, s), 6.28 (1/4 x IH, s), 7.05-7.40 (6H, m) (28) MASS : 421 (M+l) NMR (CDC1 3 , δ) : 1.33 (9 x 1/3H, s) , 1.40 (9 x 2/3K, s), 2.69 (3 x 2/3H, s), 2.89 (3 x 1/3H, s), 3.02 (2H, d, J=8Hz), 4.31 (2 x 1/6K, d, J=16Hz) , 4.58 (2 x 1/6H, d, J=16Hz), 4.70 (2 x 2/3H, s) , 4.84-4.98 (IH, ) , 5.32-5.46 (IH, m) , 7.10-7.32 (5H, ) , 7.47 (IH, d, J=8Hz), 7.75 (1 x I/3H, s), 7.83 (1 x 2/3H, S), 7.97-8.07 (IH, n) , 3.82 (2K, s) (29) MASS : 419 (M+l) NMR (CDCI3, δ) : 1.41 (9 x 1/3K, s) , 1.43 (9 x 2/3H, s), 2.03 (3 x 2/3H, s), 2.65 (3 x 1/3H, s), 3.2 " ?- 3.41 (IH, m) , 3.57-3.72 (IH, m) , 3.92 (2 x 1/6H, d, J=16Hz), 4.24 (2 x 1/3K, d, J=15Hz), 4.31 (2 x 1/6H, d, J=16Hz), 4.37 (2 x 1/3H, d, J=15Hz) , 5.02- 5.16 (IK, m) , 5.51 (1 x 1/3H, d, J=8Hzj, 5.60 (1 x 2/3H, d, J=8Hz), 6.70-6.79 (2 x 1/3H, m) , 6.9C-7.00 (2 x 2/3H, m) , 7.10-7.40 (5H, m) , 7.41-7.63 (2H, m) , 7.68-7.90 (2H, m) , 3.11 (1 x 1/2H, d, J=8Hz), 8.30 (1 x 2/3H, d, J=8Hz) (30) MASS : 370 (M+l) NMR (CDC1 3 , δ) : 1.32 (9 x 1/3H, s;, 1.33 (9 x 2/3H, s), 2.78 (3 x 2/3H, s), 2.82-3.10 (2H, m) , 2.89 (3 x 1/3H, s), 4.38 (2 x 1/6H, d, J=16Hz), 4.46 (2 x 1/6H, d, J=16Hz), 4.49 (2 x 1/3H, d, J=15Hz), 4.52 (2 x 1/3H, d, J=15Hz), 4.81-4.92 (IH, m) , 5.32 (1 x 1/3H, d, J=8Hz), 5.42 (1 x 2/3H, d, J=8Hz) , 7.00- 7.20 (3H, ) , 7.21-7.34 (3H, m) , 7.39 (1 x 1/3K, d, J=8Hz), 7.44 (1 x 2/3H, d, J=8Hz) , 8.32 (1 x 1/3H, s), 8.48 (1 x 2/3H, s) , 8.41-8.50 (IH, m) (31) MASS : 335 (M+l) NMR (CDCI3, δ) : 0.78-0.98 (3H, m) , 1.18-1.40 (4H, ) , 1.41 (9 x 1/3H, s), 1.42 (9 x 2/3H, s), 1.49-1.78 (2H, m) , 2.91 (3 x 1/3H, s) , 2.98 (3 κ 2/3K, s) , 4.50 (2 x 1/3H, d, J=15Hz), 4.62 (2 x 1/3H, d, J=15Hz) , 4.68 (2 x 1/3K, d, J=17Hz) , 4.58-4.73 (IH, m) , 5.31 (1 x 1/3H, d, J=8Hz) , 5.39 (1 x 2/3H, d, J=8Hz), 7.13-7.40 (5H, m) Preparation 64 The following object compounds were obtained according to a similar manner to that of Preparation 3, 4, 8, 41 or 54. (1) MASS : 319 (MA) NMR (CDC1 3 , δ) : 2.72 (3 x 2/3H, s) , 2.91 (3 x 1/3H, s), 2.89-3.02 (IH, ) , 3.12-3.23 (IH, m) , 3.99 (1 x 1/3H, t, J=8Hz), 4.10 (1 κ 2/3H, t, J=8Hz) , 4.22 (2 x 1/6H, d, J=16Hz), 4.39 (2 x 1/6H, d, J=16Hz) , 4.42 (2 x 1/3H, d, J=15Kz) , 4.69 (2 x 1/3H, d, J=15Hz), 6.92-7.39 (6H, m) , 7.40-7.51 (2H, m) , 7.59 (1 x 1/3H, s), 7.68 (1 x 2/3H, s), 7.71-7.85 (3H, m) (2) MASS : 283 (M+l) NMR (CDCI3, δ) : 2.25 (3 x 1/3H, s), 2.37 (3 x 2/3H, s), 2.50 (3 x 2/3K, s), 2.90 (3 x 1/3H, s), 2.81- 2.91 (IK, ) , 2.91-3.05 (IH, ) , 3.62-3.78 (IK, m) , 3.79 (2 x 1/6H, d, J=16Hz), 4.21 (2 x 1/6H, d, J=16Hz), 4.49 (2 κ 1/3H, d, J=15Hz) , 4.59 (2 x 1/3K, d, J=15Hz), 6.96 (2 x 1/3H, d, J=8Hz) , 7.08 (2 x 2/3H, d, J=8Kz), 7.13-7.32 (8H, ) (3) MASS : 299 (M-rl) NMR (CDC1 3 , δ) : 2.68-2.80 (IH, m) , 2.71 (3 x 2/3H, s), 2.88-2.98 (IH, ) , 2.91 (3 x 1/3H, s), 2.76 (3 x 2/3H, s), 2.78 (3 x 1/3H, s), 3.81 (1 x 1/3H, t, J=8Hz), 3.91 (1 x 2/3H, t, J=8Hz) , 4.20 (2 x 1/6H, d, J=16Hz) , 4.39 (2 x 1/6H, d, J=16Hz) , 4.41 (2 κ 1/3H, d, J=15Hz), 4.67 (2 x 1/3H, d, 6.78 (2H, t, J=8Hz), 7.00 -7.18 (4H, m) , 7.22-7.37 (3K, m) (4) MASS : 283 (M+l) NMR (CDC1-,, δ) : 2.32 (3H, s), 2.69 (3 x 2/3H, ≤), 2.72-2.81 (IH, ) , 2.9C (3 x 1/3H, s] , 2.93-3.03 (IH, ) , 3.86-4.00 (IH, m; , 4.12 (2 x 1/4H, c, J=16Hz), 4.37 (2 x 1/4H, d, J=16Hz), 4.46 (2 κ 1/4H, d, J=15Hz), 4.59 (2 κ 1/4H, d, J=15Hz) , 6.82- 7.31 (9H, m) (5) MASS : 283 (M+i) NMR (CDC1 3 , δ) : 2.13 (3 κ 1/3K, s) , 2.27 (3 x 2/3H, s), 2.72 (3 x 2/3H, s) , 2.73-2.85 (IH, m) , 2.97 (3 x I/3H, s), 2.98-3.08 (IH, m) , 3.70 (i x 1/2H, t, J=8Hz) , 4.02 (1 κ 1/2H, t, J=8Hz) , 4.03 (2 x 1/4H, d, J=16Hz), 4.73 (2 x 1/4H, d, J=16Hz) , 4.55 (2 x 1/4H, d, J=15Hz), 4.63 (2 κ 1/4H, d, J=15Hz) , 6.88- 6.93 (IH, m) , 7.09-7.18 (4H, ) , 7.22-7.32 (4H, m) (6) MASS : 271 (M+I) NMR (CDCI3, δ) : 2.78-2.88 (IH, ) , 2.95 (3 κ 2/3K, s) , 2.96 (3 κ 1/3H, s), 3.00-3.09 (IH, ) , 3.80 (1 x 1/4H, t, J=7Hz), 4.05 (1 x 3/4H, t, J=7Hz) , 4.32 (2 κ 1/6H, d, J=17Hz), 4.42 (2 x 1/6K, d, J=17Hz), 4.53 (2 x 1/3H, d, J=15Hz) , 4.69 (2 κ 1/3H, d, ■J=15Hz) , 6.92 (1 x 1/4H, d, J=5Hz) , 7.01 (1 x 3/4H, d, J=5Hz) , 7.12-7.32 (5H, ml , 8.62 (IH, d, J=5Hz) , 9.11 (1 x 3/4H, s) , 9.13 (I x 1/4H, s) (7) MASS : 321 (M+l) NMR (CDCI3, δ) : 2.78-2.88 (IH, ) , 2.90 (3 x 3/4H, 5), 3. CO (3 x 1/4H, s), 2.98-3.15 (IK, m) , 4.02 (IH, t, , 4.70 (2 x 1/6H, d, J=16Hz), 4.78 (2 κ 1/3H, d.. J=15Hz , 4.98 (2 κ 1/3H, d, J=15Hz), 7.11-7. C (5H, m, , 7.71-7.80 (2H, m) , 7.98-8.04 (IH, IT.) , 8.08-8.15 (IH, m) , 8.66 (1 x I/4K, s . , a .82 1 κ 3/4H, s' (8) MASS : 320 (M+l) NMR (CDC1 3 , δ) : 2.79-2.88 (IH, m) , 1.65 (3 κ 2/3H, s) , 2.97 (3 κ 1/3K, s), 3.02-3.11 (IK, m) , 3.98- 4.07 (IH, si) , 4.51 (2 x 1/6H, d, J=16Hz), 4.70 (2 x 1/όH, d, J=16Hz), 4.60 (2 κ 1/3H, c, J=15Hz), 4.92 (2 κ 1/3H, d, J=15Hz) , 7.11- 7 .29 (6K, ) , 7.51-7.58 (IH, m) , 7.68-7.73 (IH, si) , 7.81 (IH, a, J=8Hz, , 8.01 (IH, d, J=8Hz), 3.10 (IK, t, J=8Hz) (9) MASS : 320 (M+l) NMR (CDC1 3 , δ) : 2.77 (3 κ 3/4H, s), 2.60-2.88 (IH, m) , 2.99 (3 κ 1/4H, s) , 3.00-3.09 (IH, m) , 3.92- 4.05 (IH, m) , 4.36 (2 κ 1/6H, d, J=16Hz) , 4.59 (2 κ 1/6H, d, J=16HZ), 4.73 (2 x 1/3H, d, J=15Hz), 4.80 (2 x 1/3H, d, J=15Hz), 7.11-7.31 (5K, ) , 7.33-7.42 (2H, m) , 7.79 (IH, dd, J=8, 2Hz) , 7.85 (1 κ 1/4H, s) , 7.89 (1 κ 3/4H, s), 8.15 (IK, d, J=8Hz), 6.90- (10) MASS : 271 (M+l) NMR (CDCI3, δ) : 2.77-2.84 (IH, m) , 2.88 (3 κ 3/4H, s), 2.92 (3 κ 1/4K, s) , 2.97-3.09 (IH, si), 4.00 (IK, t, J=8Hz), 4.29 (2 κ 1/6H, a, J=17Hz, , 4.51 (2 κ 1/6H, d, J=17Hz), 4.61 (2 x 1/3K, d, J=15Hz), 4.75 (2 κ 1/3H, d, J=15Hz), 7.16-7.32 (5H, m) , 8.38-8.53 (3K, m) (11) MASS : 347 (M+I) NMR (CDCI3, δ) : 2.79 (3 y. 4/5H, s), 2.68-2.87 (IH, m) , 2.91 (3 x 1/5H, s), 2.96-3.10 (IH, m) , 3.88- 4.03 (IH, m) , 4.26 (2 x 1/6H, d, J=16Hz) , 4.43 (2 x 1/6H, d, J=16Hz), 4.51 (2 x 1/3H, d, J=15Hz) , 4.69 (2 x 1/3H, d, J=15Hz), 7.13-7.32 (5H, m) , 7.40 (IH, dd, J=8, 5Hz), 7.61 (IH, dd, J=8, 5Hz) , 7.69 (IH, t, J=8Hz), 8.30 (IH, d, J=8Hz) , 8.47 (1 x 1/5H, s) , 8.53 (1 x 4/5H, s) , 8.63 (IH, d, J=5Hz) , 9.18 (IH, s) (12) MASS : 347 (M+l) NMR (CDC1 3 , δ) : 2.73 (3 x 4/5H, s) , 2.80-2.90 (IH, m), 2.92 (3 x 1/5H, s) , 2.97-3.09 (IH, ) , 3.92- 4.02 (IH, m) , 4.26 (2 x 1/6H, d, J=16Hz) , 4.45 (2 x 1/6H, d, J=16Hz), 4.50 (2 x 1/3H, d, J=15Hz) , 4.74 (2 x 1/3H, d, J=15Hz), 7.17-7.42 (6H, m) , 7.62 (IH, dd, J=8, 2HZ), 7.82 (IH, t, J=8Hz) , 8.32-8.42 (2H, ), 8.52 (IH, s), 8.70 (IH, d, J=5Hz) (13) NMR (CDC1 3 , δ) : 0.95 (6H x 2/3, d, J=7Hz) , 0.99 (6H x 1/3, d, J=7Hz), 1.91 (IH, m) , 2.94 (3H, s), 3.46 (IH x 1/3, d, J=7Hz), 3.53 (IH x 2/3, d, J=7Hz) , 4.43 (IH x 1/3, d, J=16Hz), 4.46 (IH x 2/3, d, J=15Hz), 4.72 (IH x 1/3, d, J=16Hz) , 4.77 (IH x 2/3, d, J=15Hz), 7.17-7.38 (5H, m) (14) NMR (CDC1 3 , δ) : 0.75-1.02 (2H, m) , 1.11-1.33 (3H, m) , 1.39 (2H, m) , 1.53-1.88 (6H, m) , 2.92 (3H x 2/3, s), 2.97 (3H x 1/3, s) , 3.73 (IH x 1/3, dd, J=4, 7Hz), 3.80 (IH x 2/3, dd, J=4, 7Hz) , 4.43 (IH x 1/3, d, J=16Hz), 4.48 (IH x 2/3, d, J=15Hz) , 4.65 (IH x 1/3, d, J=16Hz) , 4.73 (IH x 2/3, d, J=15Hz) , 7.16-7.39 (5H, m) (15) NMR (CDC1 3 , δ) : 2.35 (3H, s) , 2.56 (4H, m) , 2.69 (3H x 3/5, s), 2.77 (IH, dd, J=7, 12Hz) , 2.90 (3H x 2/5, s), 2.98 (IH, dd, J=7, 12Hz) , 3.19 (4H, m) , 3.92 (IH, q, J=7Hz) , 4.07 (IH x 2/5, d, J=16Hz) , 4.33 (IH x 2/5, d, J=16Hz) , 4.39 (IH x 3/5, d, J=15Hz), 4.52 (IH x 3/5, d, J=15Hz) , 6.85-6.96 (3H, m) , 7.08 (IH, d, J=8Hz) , 7.13-7.31 (5H, m) (16) NMR (CDC1 3 , δ) : 2.78 (IH, m) , 2.80 (3H x 3/5, s) , 2.97 (3H x 2/5, s), 3.00 (IH, m) , 3.86 (IH x 2/5, t, J=7Hz), 3.97 (IH x 3/5, t, J=7Hz) , 4.37 (IH x 2/5, d, J=16Hz), 4.43 (IH x 2/5, d, J=16Hz) , 4.43 (IH x 3/5, d, J=15Hz), 4.68 (IH x 3/5, d, J=15Hz) , 7.03 (2H, m) , 7.15 (2H, m) , 7.31 (3H, m) , 8.48 (2H, m) (17) MASS (m/z) : 320 (M+H) + NMR (CDC1 3 , δ) : 2.72-3.12 (2H, m) , 2.77 (3/4 x 3H, S), 2.97 (1/4 x 3H, s) , 3.90-4.07 (IH, m) , 4.49 (1/4 x 2H, ABq, Δ=0.18, J=17Hz) , 4.72 (3/4 x 2H, ABq, Δ=0.19, J=15Hz), 7.07-8.17 (10H, m) , 8.68 (1/4 x IH, s) , 8.80 (3/4 x IH, s) (18) MASS (m/z) : 320 (M+H) + NMR (CDC1 3 , δ) : 2.76 (3/4 x 3H, s) , 2.79-3.10 (2H, m) , 2.98 (1/4 x 3H, s) , 3.87-4.08 (IH, m) , 4.48 (1/4 x 2H, ABq, Δ=0.16, J=17HZ) , 4.73 (3/4 x 2H, ABq, Δ=0.18, J=15Hz) , 7.08-7.65 (8H, m) , 7.98-8.15 (2H, m) , 8.91 (IH, d, J=2Hz) (19) MASS (m/z) : 327 (M+H) + NMR (CDC1 3 , δ) : 2.21 (3H, s) , 2.70 (3/4 x 3H, s) , 2.75-3.10 (2H, m) , 2.86 (1/4 x 3H, s), 3.85-4.01 (IH, m) , 4.22 (1/4 x 2H, ABq, Δ=0.22, J=17Hz) , 4.49 (3/4 x 2H, ABq, J=15Hz) , 7.10-7.55 (6H, m) , 7.95-8.20 (3H, m) (20) MASS (m/z) : 275 (M+l) + NMR (CDC1 3 , δ) : 2.86 (3H x 2/3, s), 2.96 (3H x 1/3, s), 2.95-3.05 (IH, m) , 3.16-3.29 (IH, m) , 3.89 (IH x 1/3, t, J=7.0Hz), 3.97 (IH x 2/3, t, J=7.0Hz), 4.38 (IH x 1/3, d, J=14.5Hz), 4.51 (IH, d, J=14.5Hz), 4.69 (IH x 2/3, d, J=14.5Hz), 6.80 (IH x 1/3, d, J=1.5Hz), 6.84 (IH x 2/3, d, J=1.5Hz), 6.89-6.97 (IH, m) , 7.09 (IH x 2/3, d, J=7.5Hz), 7.13-7.19 (2H, m) , 7.23-7.38 (10/3H, m) (21) MASS (m/z) : 349 (M+H) + NMR (CDC1 3 , δ) : 2.71 (2/3 x 3H, s) , 2.73-2.87 (IH, m) , 2.92 (1/3 x 3H, s) , 2.95-3.06 (IH, m) , 3.84- 4.02 (IH, m) , 3.93 (3H, s) , 4.30 (1/3 x 2H, ABq, Δ=0.20, J=17Hz), 4.57 (2/3 x 2H, ABq, Δ=0.22, J=15Hz), 6.52 (IH, m) , 6.98-7.41 (8H, m) , 7.65-7.78 (2H, m) (22) MASS (m/z) : 313 (M + +H) NMR (CDC1 3 , δ) : 2.68 (3/4 x 3H, s) , 2.72-2.82 (IH, m) , 2.84 (1/4 x 3H, s) , 2.90-3.03 (IH, m) , 3.07 (6H, s), 3.88-4.04 (IH, m) , 3.99 (1/4 x IH, d, J=17Hz) , 4.30 (1/4 x IH, d, J=17Hz), 4.40 (3/4 x 2H, ABq, Δ=0.11, J=15Hz), 6.43 (1/4 x IH, d, J=9Hz) , 6.47 (3/4 x IH, d, J=9Hz), 7.06-7.40 (6H, m) , 7.92 (1/4 x IH, d, J=2Hz), 7.99 (3/4 x IH, d, J=2Hz) (23) MASS (m/z) : 335 (M+H) + NMR (CDC1 3 , δ) : 2.77 (2/3 x 3H, s) , 2.77-2.88 (IH, ) , 2.92 (1/3 x 3H, s) , 2.96-3.10 (IH, ) , 3.82- 4.05 (IH/ m) , 4.33 (1/3 x 2H, ABq, Δ » 0.18, J=17Hz) , 4.58 (2/3 x 2H, ABq, Δ=0.13, J=17Hz) , 7.06-7.37 (11H, m) , 7.82 (IH, s) (24) MASS (m/z) : 337 (M+H) + NMR (CDC1 3 , δ) : 2.60 (3H, s) , 2.72 (3/5 x 3H, s) , 2.73-2.35 (IH, m) , 2.92 (2/5 x 3H, s), 2.93-3.05 (IH, m) , 3.71 (3H, s), 3.88-4.05 (IH, m) , 4.26 (2/5 κ IH, d, J=17Hz), 4.54 (2/5 κ IK, d, J=I7Hz), 4.68 (3/5 κ 2K, ABq, 6.88-7.52 (8H, ) (25) MASS (m/z) : 259 (M+H) ÷ NMR (CDC1 3 , δ) : 2.62-2.83 (2K, si) , 2.91 (2/3 κ 3H, s), 2.97 (1/3 x 3H, s), 2.79-4.04 (IH, m) , 4.33- 4.73 (2H, m) , 6.19 (1/3 x IH, s, , 6.27 (2/3 x IH, s), 7.08-7.41 (7H, m) (26) MASS (m/z) : 273 (M+H) + NMR (CDCI3, δ) : 2.69-3.10 (2H, ) , 2.72 (2/3 κ 3H, s), 2.89 (1/3 κ 3H, s), 3.82 (1/3 κ 3H, s), 3.87 (2/3 κ 3H, s), 3.89-4.00 (IH, m) , 4.16 (1/3 κ 2H, ABq, Δ=0.15, J=17Hz), 4.35 (2/3 κ 2H, ABq, Δ=0.12, J=15Hz), 6.95-7.38 (7H, m) (27) MASS (m/z) : 303 (M+H) ÷ NMR (CDCI3, δ) : 2.68-3.04 (2H, m) , 2.76 (3/5 x 3H, s), 2.93 (2/5 x 3H, s), 3.76-4.05 (IH, m) , 4.36 (2/5 x 2H, ABq, Δ=0.1I, J=17HZ) , 4.42 (3/5 x IH, d, J=15Hz), 4.68 (3/5 κ IH, d, J=l5Hz) , 6.95-7.42 (9H, m) (28) MASS (m/z) : 259 (M+H) " NMR (CDCI3, δ) : 2.76-3.08 (2K, ) , 2.85 (2/3 κ 3H, s), 2.94 (1/3 κ 3H, s), 4.02 (1/3 κ IH, t, J=7Hz), 4.08 (2/3 κ IH, t, J=7Hz) , 4.45 (2/3 κ IH, d, J=17HZ) , 4.72 (2/3 κ IH, d, J=15Hz;, 6.09 (IH, m) , 6.28 (IH, m) , 7.08-7.40 (6H, ) (29) MASS : 321 (M+l) NMR (CDCI3, δ) : 2.80 (3 κ 3/4H, s), 2.81-2.91 (IH, si), 3.00 (3 x 1/4H, s), 3.01-3.11 (IK, m) , 3.91 (1 x 1/4H, t, J=8Hz), 4.03 (1 x 3/4H, t, J=8Hz), 4.40 (2 x 1/6H, d, J=16Hz), 4.60 (2 x 1/6H, d, J=16Hz), 4.72 (2 x 1/3H, d, J=15Hz), 4.83 (2 x 1/3H, d, J=15Hz), 7.10-7.45 (5H, m) , 7.57 (IH, d, J=8Hz) , 7.82 (1 x 1/4H, s), 7.83 (I x 3/4H, s), 8.C0-8.10 (IK, si) , 8.80-8.88 (2H, ) (30) MASS : 319 (M+l) NMR (CDC1 3 , δ) : 2.31 (3 x 2/3H, s) , 2.83 (3 x 1/3H, s), 3.28-3.47 (2H, m) , 3.81 (2 κ 1/6H, d, J=16Hz) , 4.02 (2 x 1/6H, d, J=16Hz) , 4.01-4.09 (1 x 1/3H, m) , 4.13-4.23 (1 x 2/3H, ) , 4.39 > 2 κ 1/3H, d, J=15Hz), 4.46 (2 κ 1/3H, d, J=15Hz), 6.90 (2 κ 1/3H, d, J=8Hz), 7.03 (2 x 2/3H, d, J=8Hz), 7.15- 7.60 (7H, m) , 7.69-7.80 (IH, m) , 7.84 (IK, d, J=8Hz), 7.84 (1 x 1/3H, d, J=8Hz) , 8.10 (1 κ 2/3H, d, J=8Hz) (31) MASS : 270 (M+l) NMR (CDCI3, δ) : 2.70-2.89 (IH, ) , 2.76 (3 x 2/3H, s), 2.90-3.03 (IH, m, , 2.99 (3 x 1/3H, s) , 3.82 (1 x 1/3H, t, J=8Hz), 3.92 (1 x 2/3H, t, J=8Hz) , 4.32 (2 x 1/6H, d, J=16Hz), 4.43 (2 x I/6H, d, J=16Hz), 4.49 (2 κ 1/3H, t, J=15Hz), 4.61 (2 κ 1/3H, d, J=15Hz), 7.02 (1 x 2/3H, d, J=7Hz) , 7.19 (1 x 1/3H, d, J=7Hz), 7.11-7.40 (5H, a), 7.47 (1 κ 1/3H, d, J=7Hz) , 7.51 (1 κ 2/3H, d, J=7Hz) , 8.37 (1 I/3H, s), 8.47 (1 κ 2/3H, s;, 8.48 (IH, s) (32) MASS : 235 (M+l) NMR (CDCI3, δ) : 0.82-0.95 (3H, ) , 1.20-1.55 (5H, m) , 1.56-1.73 (IH, m) , 2.91 (3 κ 2/3H, s) , 2.93 (3 κ 1/3K, s), 3.61-3.75 (IH, m) , 4.44 (2 x 1/6H, d, J=16Hz), 4.50 (2 x I/3H, d, J=15Hz) , 4.66 (2 κ 1 / 6H, d, J= 16Hz ) , 4 . 70 ( 2 κ 1 / 3H, a, J= 15Hz ) , 7 . 10- 7 . 40 ( 5H , m) Pre ara ion 65 The following object compounds were obtained according to a similar manner to that of Preparation 1, 6, 11, 36, 52 or 56. (1) MASS : 603 (M+l) NMR (CDC1 3 , δ) : 1.45 (9H, s), 2.47-3.60 (IH, ) , 2.51 (3 x 2/3K, s), 2.79 (3 κ 1/3H, s), 3.08-3.31 (3H, m) , 3.36-3.50 (2K, ) , 3.50-3.60 (2K, m) , 3.61-3.77 (4K, m) , 4.18 (2 x 1/3H, d, J=15Hz) , 4.21 (2 x 1/6K, d, J=16Hz), 4.28 (2 x 1/6H, d, J=16Hz) , 4.69 (2 κ 1/3H, d, J=15Hz) , 4.49-4.60 (IH, m) , 5.20-5.30 (IH, m) , 5.96-6.05 (IK, m) , 6.72 (2 x 1/3H, d, J=8Hz), 6.88 (2 x 2/3H, d, J=8Hz) , 6.99-7.19 (3H, m) , 7.28-7.55 (4H, m) , 7.61-7.82 (4H, m) (2) MASS : 567 (M+l) NMR (CDC1 3 , δ) : 1.43 (9H, s), 2.67-2.83 (IH, mi, 2.79 (3 κ 2/3H, s), 2.89 (3 x 1/3H, s) , 2.92-3.07 (IH, m) , 3.10 (3H, s), 3.14-3.27 (IH, m) , 3.28-3.50 (4H, m) , 3.50-3.70 (5H, m) , 4.13 (2 x 1/6H, d, J=16Hz) , 4.20-4.31 (IH, m) , 4.37 (2 κ 1/6H, d, J=16Hz), 4.40 (2 κ 1/3H, d, J=15HZ) , 4.71 (2 κ 1/3H, d, J=l5Hz), 4.80-5.00 (IH, m) , 5.64-5.80 (IH, ) , 6.92 (IH, d, J=5Hz), 7.10-7.32 (9H, m) (3) MASS : 533 (M+l) NMR (CDC1 3 , δ) : 1.48 (9H, s), 2.50-2.62 (IH, m) , 2.60 (3 κ 2/3H, s), 2.80 (3 κ 1/3H, s), 2.88-3.06 (2H, m) , 3.12-3.27 (IH, m) , 3.40-3.50 (2H, m) , 3.57-3.63 (2H, m) , 3.64-3.72 (4H, m) , 3.73 (3 κ 2/3H, s), 3.79 (3 κ 1/3H, s), 4.18 (2 κ 1/6K, d, J=16Hz) , 4.28 (2 x 1/3H, d, J=15Hz) , 4.31 (2 x 1/6H, d, J=16Hz), 4.50-4.70 (IH, m) , 4.68 (2 x 1/3K, d, J=15Hz), 5.00-5.14 (IH, m) , 5.95-6.07 (IH, m) , 6.72 (2 x 2/3H, d, J=8Hz), 6.80 (2 x 1/3H, d, J=8Hz) , 6.83-6.92 (IH, m) (4) MASS : 526 (M+l) NMR (CDC1 3 , δ) : 1.48 (9H, s) , 2.51-2.62 (IH, m) , 2.52 (3K, s), 2.53 (3 x 2/3H, s), 2.73 (3 x 1/3H, s) , 2.94 (3H, s), 2.98-3.03 (2H, m) , 3.01 (3K, s), 3.09-3.30 (IH, m) , 4.00 (2 κ 1/6H, d, J=17Hz) , 4.22 (2 κ 1/6H, d, J=17Hz) , 4.27 (2 κ 1/3H, d, J=15Hz) , 4.54 (2 κ 1/3H, d, J=15Hz) , 4.50-4.58 (IH, m) , 5.06-5.18 (IH, m) , 6.08-6.14 (IH, m) , 6.92-7.30 (7H, m) , 7.51 (IH, t, J=8Hz) , 8.14 (1 x 1/4H, s) , 8.28 (1 x 3/4H, s) (5) MASS : 580 (M+l) NMR (CDC1 3 , δ) : 1.43 (9H, s), 2.27 (3 x 1/3H, s) , 2.31 (3 x 2/3H, s) , 2.29 (3H, s) , 2.32-2.44 (4H, m) , 2.49-2.61 (IH, m) , 2.50 (3 x 2/3H, s) , 2.80 (3 x 1/3H, s), 2.97-3.11 (2H, m) , 3.17-3.28 (IH, m) , 3.40-3.50 (2H, m) , 3.57-3.65 (2H, m) , 4.02 (2 x 1/6K, d, J=16Hz), 4.23 (2 x 1/6H, d, J=16Hz) , 4.28 (2 x 1/3H, d, J=15Hz) , 4.58 (2 x 1/3H, d, J=15Hz) , 4.48-4.56 (IH, m) , 5.08-5.18 (IH, ) , 5.99-6.07 (IH, m) , 6.66-7.47 (10H, m) (6) MASS : 580 (M+l) NMR (CDC1 3 , δ) : 1.47 (9H, s) , 2.17 (3 x 2/3H, s), 2.28 (3 κ 1/3H, s) , 2.28 (3H, s) , 2.32-2.42 (4H, m) , 2.48-2.61 (IH, m) , 2.54 (3 x 2/3H, s) , 2.80 (3 x 1/3H, s), 2.95-3.28 (3H, m) , 3.40-3.50 (2H, m) , 3.55-3.65 (2H, m) , 4.00 (2 x 1/4H, d, J=16Hz), 4.13 (2 x 1/4H, d, J=16Hz) , 4.49 (2 x 1/2H, s) , 4.50- 4.59 (IH, m) , 4.93-5.02 (1 x 1/3H, m) , 5.13-5.21 (1 x 2/3H, m) , 6.00 (IH, d, J=8Hz) , 6.63 (1 x 1/3H, d, J=8Hz), 6.71 (1 x 2/3H, d, J=8Hz) , 7.02-7.18 (4H, m) , 7.20-7.30 (4H, m) , 7.38-7.45 (IK, m) (7) MASS : 555 (M+l) NMR (CDC1 3 , δ) : 1.47 (9 x 3/4H, s), 1.48 (9 x 1/4H, s), 2.51-2.62 (IH, m) , 2.81 (3 κ 3/4H, s), 2.88 (3 x 1/4H, s), 2.94-3.23 (3K, m) , 3.43-3.49 (2H, m) , 3.57-3.62 (2H, m) , 3.63-3.73 (4H, m) , 4.36 (2 x 1/6H, d, J=17Hz), 4.40 (2 x 1/6H, d, J=17Hz) , 4.47 (2 x 1/3H, d, J=15Hz), 4.51-4.60 (IH, m) , 4.61 (2 x 1/3H, d, J=15Hz), 4.92-5.00 (1 κ 1/4H, m) , 5.13- 5.22 (1 x 3/4H, m) , 5.97-6.05 (IH, m) , 6.72 (1 x 1/4H, d, J=5Hz), 6.82 (1 x 3/4H, d, J=5Hz) , 7.18- 7.30 (5H, m) , 7.33 (1 x 1/4H, d, J=8Hz), 7.40 (1 x 3/4H, d, J=8Hz), 8.54 (1 x 1/4K, d, J=5Hz) , 8.59 (1 x 3/4H, d, J=5Hz), 9.08 (1 x 1/4H, s) , 9.10 (1 x 3/4H, s) (8) MASS : 605 (M+l) NMR (CDCI3, δ) : 1.42 (9H, s), 2.49-2.62 (IH, m) , 2.79 (3 x 5/6H, s), 2.93 (3 x 1/6H, s) , 3.00-3.23 (3H, m) , 3.40-3.50 (2H, m) , 3.53-3.62 (2H, m) , 3.63-3.73 (6H, m) , 4.51 (2 x 1/6H, d, J=16Hz) , 4.58 (2 x 1/6H, d, J=16Hz), 4.62 (2 x 1/3H, d, J=15Hz) , 4.92 (2 x 1/3H, d, J=15Hz), 4.50-4.63 (IH, m) , 7.08-7.21 (5H, m) , 7.47-7.53 (IH, m) , 7.71-7.80 (2H, m) , 7.98-8.03 (IH, m) , 8.07-8.13 (IH, m) , 8.61 (1 x 1/6H, s), 8.74 (1 κ 5/6K, s) (9) MASS : 604 (M+l) NMR (CDC1 3 , δ) : 1.42 (9H, s) , 2.49-2.61 (IH, m) , 2.72 (3 x 2/3H, s), 2.89 (3 x 1/3H, s) , 3.00-3.25 (3K, m) , 3.40-3.50 (2H, m) , 3.56-3.62 (2H, m) , 3.63-3.73 (4H, m) , 4.48 (2 x 1/6H, a, J=17Hz), 4.58 (2 x 1/6H, d, J=17Hz), 4.50-4.61 (IH, m) , 4.69 (2 x 1/3H, d, J=15Hz), 4.85 (2 x 1/3H, d, J=15Hz), 5.17- 5.28 (IH, si) , 5.97-6.04 (IH, ) , 7.03 (1 x 1/4K, d, J=8Hz), 7.09 (1 κ 3/4H, d, J=8Hz) , 7.18-7.24 (5H, rv.) , 7.41-7.56 (2H, si), 7.70 (IH, t, J=8Kz) , 7.80 (IK, d, J=8Hz), 7.97-8.08 (2H, ) (10) MASS : 604 (M+l) NMR (CDC1 3 , δ) : 1.49 (9H, s) , 2.52-2.60 (IH, m) , 2.62 (3 x 2/3H, s), 2.83 (3 x 1/3H, s), 2.99-3.27 (3H, si) , 3.40-3.50 (2H, i) , 3.56-3.62 (2H, ) , 3.64-3.74 (4H, m) , 4.21 (2 x 1/6H, a, J=16Kz), 4.50 (2 x I/6H, a, J=16Hz), 4.53-4.62 (IH, m) , 4.60 (2 x 1/3H, d, J=15Hz), 4.73 (2 x 1/3H, d, J=15Hz) , 5.11- 5.27 (IH, ) , 5.97-6.08 (IH, m) , 7.02-7.30 (6H, m) , 7.40 (IH, dd, J=8, 5Hz), 7.44-7.53 (IH, ) , 7.70- 7.80 (IK, m) , 7.83 (IH, ε), 3.14 (IH, t, J=5Hz) , 8.89 (IH, t, J=5Hz) (II, MASS : 555 (M+l) NMR (CDCI3, δ) : 1.43 (9H, s), 2.52-2.60 (IH, j , 2.78 (3 κ 3/4H, s), 2.88 (3 κ 1/4H, s) , 3.02-3.22 (2H, ) , 3.41-3.50 (2H, m) , 2.57-3.72 (7H, m) , 4.36 (2 x 1/3H, s), 4.47 (2 κ 1/3H, a, J=15Hz), 4.48-4.60 (IH, ) , 4.70 (2 x I/3H, a, A15Hz), 5.06-5.16 (IH, , , 6.00 (IH, br s,, 7.13-7.26 (6H, m, , .47 (IH, br s) , 8. 1-8.50 (2H, ιr.j (12) MASS : 631 (MA) NMB (CDCI3, δ) : 1.43 (9H, s,\ 2.51-2.62 (IH, m ; , 2.62 (3 κ 3/4H, s), 2.80 !3 κ 1/4H, s,, 2.96-3.26 (3H, ; , 3.40-3.52 (2H, m, , 3.55-3.62 (2K, m, , 3.62-5.72 X ' X., TΛ 4.14 (2 x 1/6H, a, J=16Hz;, 4.32 [ 2 x 1/όH, d, =I6Hz; , 4.4 (2 x 1/3H, a, =15Kz) , 4.51-4.60 (IH, m) , 4.61 (2 κ 1/3H, a, J=15Hz) , 5.08-5.20 (IH, m) , 5.99-6.06 (IH, n) , 7.12-7.30 (5H, ) , 7.38-7.50 (3H, m) , 7.59 ; x ι/ 4 / d/ J=8Hz), 7.67 (1 κ 3/4H, a, J=8Hz) , 6.26-3.32 (IH, m) , 8.33 (1 x 1/4H, s), 8.48 (1 x 3/4K, s ) , 8.64 (IH, d, J=5Hz), 9.12-9.20 (IH, si) (13) MASS : 631 (M+l) NMR (CDCI3, δ) : 1.43 (9H, s) , 2.52-2.62 (IH, m) , 2.59 (3 κ 3/4H, s), 2.80 (3 κ 1/4H, s) , 2.99-3.22 (3H, m) , 3.42-3.50 (2H, ) , 3.58-3.62 (2H, m) , 3.67-3.77 (4H, m) , 4.18 (2 x 1/6H, d, J=I6Hz) , 4.32 (2 κ 1/6H, d, J=16H∑), 4.31 (2 x 1/3H, d, J=15Hz), 4.71 (2 κ 1/3H, d, J=15Hz) , 4.51-4.60 (IH, m! , 5.08-5.22 (IH, m) , 6.02 (IH, br s), 7.18-7.22 (5H, m) , 7.28- 7.33 (IH, m) , 7.41-7.51 (2H, ) , 7.79-7.88 (IH, m) , 8.22-8.46 (3K, m) , 8.66-8.70 (IH, m) (14) MASS : 505 (M + +l) NMR (CDCI3, δ) : 0.88-0.99 (6H, m) , 1.47 (9H, s), 2.07 (IH, m) , 2.57 (IH, ) , 2.91 (3H κ 1/3, s), 3.01 (3H κ 2/3, s), 3.21 (IH, dd, J=3, 15Hz) , 3.45 (2H, ) , 3.58 (2H, m) , 3.65 (4H, m) , 4.37 (IH κ 2/3, a, J=15HZ), 4.57 (IH, ) , 4.63 (2H κ 1/3, s) , 4.31 (IH, m) , 4.82 (IH κ 2/3, d, J=15Hz), 6.12 (IH, ) , 7.21-7.35 (5H, m) (15) MASS : 559 (M + +l) NMR (CDCI3, δ) : 0.80-1. CO (2H, si), 1.07-1.25 (3H, m), 1.45 (9H, s), 1.43-1.94 (8K, si), 2.55 (IH, si), 2.92 (3H κ 1/3, s), 2.98 (3H κ 2/3, s), 3.17 (IH, dd, J=4, 15Hz), 3.44 (2H, m) , 3.60 (2H, m) , 3.66 (4K, m) , 4.38 (IH κ 2/3, a, J=15Hz) , 4.56 (IH κ 1/3, d, J=16Hz), 4.55 (IH, m) , 4.67 (IH κ 1/3, a, J=16Hz), 4.75 (IH κ 2/3, d, J=15Hz) , 5.02 (IH, m. , 6.03 (IH, 81 - 485 - d, J=7Hz), 7.17-7.38 (5H, m ) (16) MASS : 651 (K~-l ) NMR (CDC1 3 , δ) : 1.47 (9K, s), 2.35 (3H, s) , 2.51 (3H x 2/3, s), 2.56 (5H, si), 2.74 (3H x 1/3, s) , 3.02 (2K, ) , 3.18 (5H, si), 3.45 (2E, ) , 3.60 (2H, si), 3.67 (4H, m) , 3.92 ( H x 1/3, a, J=16Hz), 4.22 (IH κ 1/3, d, J=16Hz), 4.23 (IH x 2/3, d, J=15Hz) , 4.52 (IH x 2/3, d, J=15Hz), 4.54 (IH, m) , 5.07 (IH x 2/3, m) , 5.17 (IH x 1/3, si), 6.00 (IH, d, J=7Hz) , 6.80 (4H x 1/3, s), 6.82 (2H x 2/3, s), 6.97 (2H x 2/3, s), 7.19 (4H, s} , 7. jiv, si) (17) MASS (m/z) : 554 (K~~l ) NMR (CDCI3, δ) : 1.45 (9H, s) , 2.46-2.58 (IH, si) , 2.72 (3H x 2/2, s), 2.88 (3K x 1/3, s), 2.90-2.99 (IH, si), 3.08 (IH, dd, J=7, 13Hz), 3.18 (IH, ) , 3.43 (2H, ) , 3.57 (2H, si; , 3.65 (4K, si), 4 .26 (IH κ 2/3, d, J=15Hz), 4.35 (IH κ 1/3, d, J=16Hz), 4.44 (IH x 1/5, a, J=16Hz), 4.52 (IH, si), 4.70 (IH x 2/3, a, J=15Hz;, 5.15 (IH, si:, 5.98 (IH, a, J=7Hz), 6.92-7.13 (4H, si) , 7.27-7.45 (3H, ) , 8.43 (2K, m> ;i8) MASS (m/z) : 620 (M'+I) NMR (CDCI3, δ) : 1.47 (9H, s, , 2.61 (3H x 3/4, s,, 2.80 (3H x 1/4, s) , 1 H, —\) , 3.45 (2H, TC. ) , 3.60 (2ή ' , si, , 3.6" ( , m) , 4.26 (IH x 1/4, a, J=16H∑), 4.30 (IH κ 1/4, d, J=16Hz), 4.36 (IH x 3/4, a, =15Hz), 4.54 (IH, X , 4.63 (IH x 3/4, a, =15Hz), 5.13 (IH, r.-, 6.02 (IH, m; , 6.97-7.1 " (2H, ir.) , 7.21-7.28 (4H, r.) , 7. ^-^.58 ;3H, m, , 6 1 - C. IH, s, , 8.52 (IH, s) 19) MASS (m/z) : 604 (MTH) NM?. (CDC1- 5 , δ' : 1.48 (9H, sj, 2.49-2.66 (IH, si; , 2. cl - 486 - (3/4 κ 3H, s), 2.83 (1/4 κ 3H, s), 2.94-3.23 (3H, si), 3.35-3.76 (8H, m) , 4.38 (1/4 x 2H, ABq, Δ=0.19, J=17Hz), 4.49 (3/4 x IH, d, J=15Hz), 4.50-4.65 (IH, m) , 4.80 (3/4 x IK d, J=15Hz) , 5.C2-5.25 (IH, ) , 5.93-6.10 (IH, br d) , 7.03-7.30 (5H, m) , 7.40-8.15 (6H, si), 8.58 (1/4 x IK, d, J=2Hz) , 6.72 (3/4 κ IK, a, J=2Hz) (20) MASS : 604 (M+H) + NMR (CDC1 3 , δ) : 1.48 (9H, s), 2.48-2.66 (IH, si), 2.62 (2/3 x 3H, s), 2.84 (1/3 x 3H, s) , 2.94-3.28 (3H, m) , 3.37-3.78 (8H, j , 4.38 (1/3 κ 2H, ABq, Δ=0.11, J=17Hz), 4.49 (2/3 x IH, d, J=15Hz), 4.50-4.64 (IH, m) , 4.80 (2/3 κ IH, a, J=15Hz), 5.10-5.24 (IH, si), 5.96-6.08 (IH, br d) , 7.10-7.55 (9H, ) , 7.93-8.15 (2H, m) , 8.86-8.92 (IK, m) (21) MASS (m/z) : 611 (M+H) ÷ NMR (CDCI3, δ) : 1.46 (9H, s) , 2.19 (1/4 x 3H, s), 2.21 (3/4 x 3H, s), 2.50-2.63 (IH, m) , 2.55 (3/4 κ 3H, s), 2.72 (1/4 x 3H, s), 2.93-3.28 (3H, m) , 3.37-3.78 (8H, si), 4.11 (1/4 κ 2H, ABq, Δ=0.22, J=17Hz), 4.21 (3/4 κ IH, d, J=15Hz) , 4.48-4.60 (IH, m) , 4.58 (3/4 κ IH, d, J=15Hz) , 5.02-5.22 (IH, ) , 5.95-6.10 (IH, br d), 7.05-7.52 (7H, m) , 7.86-8.15 (3H, ) (22) MASS (m/z) : 588 (M+H) ÷ NMR (CDCI3, δ) : 1.43 (9K, s.;, 1.8-2.2 (2H, si), 2.3- 23 (2H, m) , 2.60 (2/3 κ 3H, s), 2.82 (1/3 κ 3H, s), 3.0-3.1 (2H, m) , 4.10 (1/3 κ IH, a, J=15Hz) , 4.1- 4.2 (IH, m) , 4.32 (1/3 x IH, d, J=15Hz) , 4.38 (2/3 x IH, d, J=15Hz), 4.60 (2/3 x IH, d, J=15Hz) , 5.1- 5.2 (2H, si) , 5.13 (2K, s) , 6.9-7.3 (16H, ) (23) MASS (m/z) : 537 (M + +l) NMR (CDC1 3 , δ) : 1.47 (9H, s) , 2.52-3.28 ( 4ή ' , m) , 3.42-3.68 (8H, m) , 4.52-4.68 (2H, m) , 4.89-4.97 (IH, m) , 5.39-5.47 (IH, ) , 6.90 (IH, d, J=8Hz) , 7.01 (IH, t, J=8HZ), 7.13 (IH, t, J=8Hz) , 7.16-7.34 (6H, n) , 6.79-7.85 (IH, si) (24) MASS (m/z) : 559 (M+l) + NMR (CDCI3, δ) : 1.47 (9H, s), 2.49-2.62 (IH, ) , 2.76 (3H x 2/3, s), 2.84 (3H x 1/3, s), 3.11-3.26 (2H, m) , 3.32 (IH x 2/3, κ, J=δ.5Hz), 3.33 (IK κ 1/3, d, J=8.5Hz), 3.40-3.50 (2H, m) , 3.55-2.76 (6K, si), 4.33 (IH κ 1/3, d, J=14.5Hz), 4.37 (IH κ 2/3, d, J=14.5Hz), 4.41 (IH κ 1/3, d, J=14.5Hz), 4.47-4.60 (IH, m) , 4.64 (IH x 2/3, d, J=14.5Kz), 5.10-5.19 (IH, m) , 6.02 (IH, br d, J=7.5Kz), 6.83-7.33 (8K, m) , 7.40 (IH x 1/3, br d, =7.5Hz), 7.47 (IH x 2/3, br d, J=7.5Hz) (25) MASS (m/z) : 633 (M+H) ÷ NMR (CDCI3, δ) : 1.47 (9H, s), 2.47-2.62 (IH, si), 2.54 (2/3 x 3H, s), 2.79 (1/3 x 3H, s) , 2.93-3.11 (2H, m) , 3.11-3.28 (IH, m) , 3.35-3.75 (8H, m) , 3.94 (3H, s), 4.20 (1/3 κ 2H, ABq, Δ=0.21, J=17Hz) , 4.26 (2/3 x IH, d, J=15Hz), 4.49-4.62 (IH, m) , 4.68 (2/3 x IH, d, J=15Hz), 5.05-5.23 (IH, m) , 6.02 (IH, br d, J=3Hz), 6.50 (1/3 x IH, d, J=2Hz) , 6.52 (2/3 x IH, d, J=2Hz), 6.87-7.73 (11H, m) (26) MASS (m/z) : 597 (M+H) + NMR (CDCI3, δ) : 1.47 (9H, S) , 2.50 (2/3 x 3H, s) , 2.51-2.62 (IH, m) , 2.71 (1/3 κ 3H, s), 2.97-3.06 (2H, m) , 3.06 (1/3 x 6H, s) , 3.08 (2/3 x 6H, s) , 3.11-3.23 (IH, m) , 3.36-3.80 (8H + 1/3 x 2H, ) , 4.31 (2/3 x 2H, ABq, Δ=0.21, J=15Hz) , 4.4-7-4.61 (IH, m) , 4.98-5.32 ;1H, m) , 6.02 (IH, br a, J=3Hz), 6.39 (1/3 x IH, d, J=9Hz), 6.43 (2/3 x IH, a, J=9Hz), 7.12-7.52 (7K, m) , 7.82 (1/3 x IH, a, J=2Kz), 7.94 (2/3 κ IH, d, J=2Hz) (27) MASS (m/z) : 619 (M+H) + NMR (CDC1 3 , δ) : 1.47 (9H, s), 2.49-2.65 (IH, m) , 2.61 (2/3 x 3H, s), 2.79 (1/3 x 3H, s), 2.92-3.30 (3H, m) , 3.36-3.78 (8K, m) , 4.22 (1/3 x 2H, ABq, Δ=0.15, J=17Hz), 4.46-4.62 (IH, m) , 4.49 (2/3 x 2H, ABq, Δ=0.16, J=15Hz), 5.06-5.21 (IH, m) , 5.92-6.08 (IH, m) , 6.92-7.50 (12H, ) , 7.82 (IH, s) (28) MASS (m/z) : 621 (M+H) ÷ NMR (CDCI3, δ) : 1.47 (9H, s) , 2.48-2.65 (IH, ) , 2.52 (2/3 κ 3H, s), 2.58 (1/3 x 3H, s) , 2.60 (2/2 κ 3K, s), 2.76 (1/3 x 3H, s) , 2.93-3.27 (3H, m) , 3.36- 3.77 (8H, m) , 3.69 (1/3 x 3H, s) , 3.71 (2/3 x 3H, s), 4.02 (1/3 x IH, d, J=17Kz) , 4.47 (1/3 x IH, d, J=17Hz), 4.48-4.62 (IH, m) , 4.57 (2/3 κ 2H, ABq, Δ=0.16, J=15Hz), 5.02-5.34 (IH, m) , 6.02 (IH, br d) , 6.75-7.56 (9H, ) (29) MASS (m/z) : 543 (M+H) + NMR (CDCI3, δ) : 1.45 (9H, s), 2.46-2.62 (IH, m) , 2.70-3.02 (2H, m) , 2.35 (2/3 x 3H, s), 2.88 (1/3 x 3H, s), 3.11-3.30 (IH, m) , 3.37-3.76 (8H, a), 4.36 (2/3 x IH, d, J=15Hz), 4.45-4.60 (IK, m) , 4.48 (1/3 x 2H, s), 4.70 (2/3 x IH, d, J=15Hz) , 5.00-5.12 (IH, ) , 6.02 (IH, br d, J=8Hz) , 6.23 (1/3 x IH, s), 6.28 (2/3 x IK, s), 7.00-7.50 (8H, m; (30) MASS (m/z) : 557 (M+H) + NMR (CDCI3, δ) : 1.48 (9H, s), 2.50-2.62 (IH, m) , 2.56 (2/3 x 3H, s), 2.78 (1/3 x 3H, s) , 2.92-3.28 (3H, m) , 3.38-3.75 (8H, m) , 3.79 (1/3 x 3H, s), 3.85 (2/3 x 3H, s), 4.01 (1/3 x 2H, ABq, Δ=0.16, J=17Hz), 4.13 (2/3 x IH, d, J=15Hz), 4.40 (2/3 x IH, d, J=15Hz), 4.46-4.60 (IH, m) , 4.98-5.23 (IH, m) , 5.93-6.09 (IH, m) , 6.88-7.50 (8H, m) (31) MASS (m/z) : 587 (M+H) + NMR (CDC1 3 , δ) : 1.46 (9H, s) , 2.45-2.62 (IH, m) , 2.67 (2/3 x 3H, s), 2.83 (1/3 x 3H, s) , 2.85-3.27 (3H, m), 3.35-3.76 (8H, m) , 4.25 (2/3 x IH, d, J=15Hz) , 4.34 (1/3 x 2H, ABq, Δ=0.06, J=17Hz) , 4.45-4.60 (IH, m) , 4.71 (2/3 x IH, d, J=15Hz) , 5.04-5.16 (IH, m) , 6.00 (IH, d, J=8Hz) , 6.84-7.48 (10H, m) (32) MASS (m/z) : 543 (M+H) + NMR (CDC1 3 , δ) : 1.48 (9H, s) , 2.48-2.67 (IH, m) , 2.78 (2/3 x 3H, s), 2.86 (1/3 x 3H, s) , 2.94-3.28 (3H, m) , 3.35-3.79 (8H, m) , 4.31 (2/3 x IH, d, J=15Hz) , 4.41 (1/3 x 2H, ABq, Δ=0.13, J=17Hz) , 4.46-4.63 (IH, m) , 4.77 (2/3 x IH, d, J=15Hz) , 5.10-5.30 (IH, m) , 5.92- 6.10 (IH, br d, J=8Hz) , 6.11 (2/3 x IH, d, J=2Hz) , 6.13 (1/3 x IH, d, J=2Hz) , 6.24 (2/3 x IH, d, J=2Hz) , 6.30 (1/3 x IH, d, J=2Hz), 7.02-7.60 (7H, m) (33) MASS : 605 (M+l) NMR (CDC1 3 , δ) : 1.49 (9H, s), 2.50-2.70 (IH, m) , 2.63 (3 x 2/3H, S), 2.83 (3 x 1/3H, s) , 2.97-3.30 (3H, m), 3.40-3.50 (2H, m) , 3.58-3.64 (2H, m) , 3.65-3.80 (4H, m), 4.32 (2 x 1/6H, d, J=16Hz) , 4.49 (2 x 1/6H, d, J=16Hz), 4.51-4.63 (IH, m) , 4.59 (2 x 1/3H, d, J=15Hz), 4.80 (2 x 1/3H, d, J=15Hz) , 5.10- 5.21 (IH, m), 5.95-6.08 (IH, m) , 7.15-7.28 (5H, m) , 7.39-7.53 (2H, m) , 7.71 (1 x 1/3H, s) , 7.82 (1 x 2/3H, s), 7.98 (1 x 1/3H, d, J=8Hz) , 8.00 (1 x 2/3H, d, J=8Hz), 8.82 (2H, s) - 490 - 34) MASS : 603 (M+l) NMR (CDCl-,, δ) : 1.49 (9H, s) , 1.91 (3 x 2/3H, s), 2.61 (3 κ 1/3K, s), 3.20-3.53 (4H, m) , 3.54-3.86 (8H, m) , 4.22 (2 κ 1/2H, d, J=15Hz) , 4.36 (2 κ 1/2H, d, J=15Hz), 4.50-4.63 (IH, m) , 5.28-5.36 (I m) , 6.00-6.10 (IH, m) , 6.61-6.68 (2 κ 1/3H, m) , 6.88-7.00 (2 x 2/3H, m) , 7.07-7.30 (5H, m) , 7.31- 7.72 (4H, m) , 7.74-7.86 (IH, m) , 8.19 (1 x 1/3H, J=8Hz), 8.39 (1 x 2/3H, d, J=3Hz! (35) MASS : 554 (M+l) NMR (CDC1 3 , δ) : 1.41 (9H, s) , 2.48-2.61 (IH, m) , 2.7 (3 x 2/3H, s), 2.88 (3 x 1/3H, s) , 2.89-3.27 (3H, a), 3.35-3.49 (IH, ) , 3.52-3.75 (7H, si) , 4.38 (2 1/3H, s), 4.39 (2 κ 1/3H, d, J=15Hz), 4.59 (2 x 1/3H, d, J=15Hz), 4.44-4.58 (IH, m) , 5.07-5.18 (I m) , 5.96-6.06 (IH, m) , 6.91-6.98 (2 κ 1/3H, 31), 7.08-7.11 (2 κ 2/3H, a), 7.06-7.20 (IH, m) , 7.22- 7.33 (3H, m) , 7.38-7.57 (2H, a), 8.38 (1 κ 1/3H, s), 8.47 (1 κ 2/3H, s), 8.47 (iκ, s) (36) M7\SS : 584 (M+l) NMR (CDCI3, δ) : 1.48 (9H, s), 2.51 (3 x 3/4H, s), 2.71 (3 x 1/4H, s), 2.49-2.63 (IH, a), 2.95-3.05 (2H, m) , 3.06-3.25 (IH, m) , 3.38-3.50 (2K, a), 3.53-3.62 (2H, a), 3.62-3.77 (4H, a), 3.88 (3 κ 1/4H, s), 3.99 (3 x 3/4H, s) , 4.20 (2 x 1/2H, d, J=16Hz), 4.49 (2 κ I/2K, d, J=16Hz), 4.50-4.60 (I m) , 5.00-5.11 (IH, m) , 5.95-6.07 (IH, a), 6.60-6.7 (IH, m) , 7.00 (1 κ 1/4H, d, J=8Hz), 7.18 (1 x 3/4 d, J=8Hz), 7.10-7.30 (5K, a), 7.43 (IH, t, J=8Hz), 7.80 (1 x 1/4H, s), 7.92 (1 x 3/4H, s) (37) MASS : 519 (M+l) NMR (CDCI3, δ) : 0.78-1.00 (3K, m) , 1.15-1.41 (4H, m) , 1.47 (9H, s), 1.56-1.71 ' (2H, m) , 2.48-2.62 (IH, a), 2.91 (3 κ 1/3H, s), 2.97 (3 κ 2/3H, s) , 3.20 (IH, d, J=16Hz) , 3.35-3.50 (2H, m) , 3.52-3.60 (2H, m) , 3.61-3.78 (4H, m) , 4.41 (2 κ 1/3H, d, J=15Hz), 4.49-4.63 (IH, ) , 4.61 (2 x 1/3H, s), 4.77 (2 x 1/3H, d, J=15Hz), 4.87-5.00 (IH, m) , 6.08 (IH, d, J=8Hz) , 7.12-7.50 (6H, m) Preparation 66 The following object compounds were obtained according to a similar manner to that of Preparation 3, 4, 8, 41 or 54. (1) MASS : 503 (M+l) NMR (CDC1 3 , δ) : 1.97-2.03 (1 x 1/3H, m) , 2.20-2.30 (1 x 2/3H, m) , 2.47 (1 x 1/3H, dd, J=15, 2Hz) , 2.60 (1 x 2/3H, dd, J=15, 2Hz) , 2.72 (3 x 2/3H, s) , 2.90 (3 x 1/3H, s), 2.98-3.33 (4H, m) , 3.40-3.72 (7H, m) , 4.30 (2 x 1/3H, d, J=15Hz) , 4.42 (2 x 1/6H, d, J=16Hz) , 4.50 (2 x 1/6H, d, J=16Hz) , 4.71 (2 x 1/3H, d, J=15Hz), 5.26-5.38 (IH, a) , 6.92-7.02 (2H, a) , 7.10-7.23 (3H, m) , 7.34-7.48 (3H, m) , 7.59 (1 κ 1/3H, s), 7.69 (1 κ 2/3K, s) , 7.70-7.81 (3H, m) , 8.03 (1 κ 1/3H, d, J=8Hz) , 8.19 (1 κ 2/3H, d, J=8Hz) (2) MASS : 467 (M+l) NMR (CDCI3, δ) : 2.64 (1 κ 2/3H, d, J=8Hz), 2.71 (1 κ 1/3H, d, J=8Hz), 2.80 (3 κ 2/3H, s), 2.89 (3 κ 1/3H, s), 2.91-3.14 (2H, m) , 3.11 (3H, s), 3.15- 3.42 (3H, m) , 3.43-3.70 (8H, m) , 3.93 (1 κ 1/3H, t, J=8Hz), 4.08 (1 κ 2/3H, t, J=8Hz) , 4.36 (2 κ 1/6H, d, J=16Hz) , 4.47 (2 x 1/3H, d, J=15Hz), 4.62 (2 x 1/3H, d, J=15Hz), 4.68 (2 x 1/6H, d, J=16Hz) , 5.73- 5.83 (IH, m) , 6.97 (2 x 1/3H, d, J=7Hz) , 7.13 (2 x 2/3H, d, J=7Hz) , 7.18-7.33 (8H, m) 1 - 492 - ( 3 ) MASS : 483 (M+ l ) NMR (CDC1 3 , δ) : 2.27-2.39 (1 κ 1/3H, a) , 2.42-2.53 ( κ 2/3H, m) , 2.60-2.82 (IH, ) , 2.68 (3 κ 2/3H, s), 2.88 (3 κ 1/3H, s), 2.90-3.08 (2H, a), 3.33-3.46 (2H, m) , 3.50-3.72 (7H, m) , 3.73 (3 κ 2/3H, s), 3.76 (3 x 1/3H, s) , 4.30 (2 x 1/3H, d, J=15Hz) , 4.40 (2 x 1/3H, s), 4.71 (2 κ 1/3H, d, J=I5Hz), 5.08-5.19 (IH, a), 6.70-6.82 (2H, a), 6.93-7.15 (4H, a), 7.20-7.32 (3H, a), 8.01 (1 κ 1/3H, a, J=8Hz), 8.11 (1 κ 2/3K, d, J=8Hz) (4) MASS : 426 (M+l) NMR (CDCI3, δ) : 2.50-2.62 (IH, m) , 2.51 (3 x 1/3H, s), 2.52 (3 κ 2/3H, s) , 2.63 (3 κ 2/3H, s), 2.72- 2.85 (IH, m) , 2.79 (3 κ 1/3H, s), 2.91-3.22 (2H, m) , 2.99 (3H, s) , 3.00 (3H, s), 3.62-3.80 (IK, m) , 4.22 (2 κ 1/6H, d, J=17Hz) , 4.32 (2 κ 1/3H, d, J=15Hz), 4.38 (2 κ 1/6H, d, J=17Hz) , 4.60 (2 κ 1/3H, d, J=17Hz), 5.10-5.23 (IH, m) , 7.01-7.11 (I m) , 7.14-7.31 (6H, m) , 8.18 (IH, m) , 8.21 (1 κ 1/4H, s) , 8.30 (1 κ 3/4H, s) (5) MASS : 480 (M+l) NMR (CDCI3, δ) : 2.30 (3H, s) , 2.31 (3K, s), 2.22-2.4 (5H, a), 2.68 (3 κ 2/3K, s) , 2.72-2.85 (IH, a) , 2.89 (3 x 1/3H, s), 2.92-3.16 (2H, a), 3.39-3.48 (2H, a), 3.52-3.73 (3H, a), 4.30 (2 x 1/6H, d, J=l6Hz), 4.37 (2 κ 1/6H, d, J=16Hz) , 4.32 (2 κ 1/3H, d, J=15Hz), 4.62 (2 κ 1/3H, d, J=15Hz) , 5.1 5.22 (IH, m) , 6.78-7.27 (9H, a), 8.08 (1 κ 1/3H, J=8Hz), 8.17 (1 κ 2/3H, d, J=8Hz) ' (6) NMR (CDC1 3 , δ) : 2.19 (3 κ I/3H, s), 2.21 (3 κ 2/3H, s) , 2.28 (3H, s) , 2.31-2.47 (5H, m! , 2.62-2.85 (I m) , 2.72 (3 κ 2/3H, s), 2.92 (3 κ 1/3K, s) , 2.95- 3.18 (2H, m) , 3.33-3.72 (5H, m) , 4.30 X κ 1/3H, s), 4.48 (2 x 1/3H, d, J=15Hz), 4.59 (2 x 1/3H, d, J=15Hz), 5.02 (1 x 1/3H, q, J=8HZ), 5.12 (1 x 2/3H, q, J=8Hz), 6.78-6.80 (IH, a) , 7.07-7.17 (4H, a), 7.20-7.30 (4H, m) , 7.97 (1 x 1/3H, d, J=8Hz), 8.13 (1 x 2/3H, d, J=8Hz) (7) MASS : 455 (M+l) NMR (CDC1 3 , δ) : 2.39-2.61 (IH, m) , 2 0-2.82 (IH, a), 2.88 (3 x 3/4H, s), 2.89 (3 x 1/4H, s), 2.93-3.22 (2H, m) , 3.38-3.47 (2H, m) , 3.51-3.73 (7H, m) , 4.32 (2 x 1/6H, d, J=17Hz), 4.48 (2 κ 1/3H, d, J=15Hz), 4.62 (2 κ 1/6H, d, J=17Hz) , 4.64 (2 κ 1/3H, d, J=15Hz), 4.93-5.04 (1 κ 1/4H, m) , 5.17-5.22 (I x 3/4H, m) , 6.82 (1 κ 1/4H, d, J=5Hz) , 6.88 (1 κ 3/4H, d, J=5Hz), 7.17-7.31 (5K, a), 8.08-8.14 (IH, a), 8.58 (1 κ 1/4H, d, J=5Hz) , 8.60 (1 κ 3/4H, d, J=5Hz), 9.10 (IH, s) (8) MASS : 505 (M+l) NMR (CDC1 3 , δ) : 2.28-2.36 (1 x 1/4H, a), 2.48-2.57 (1 x 3/4H, a), 2.64-2.82 (IH, a), 2.86 (3 x 3/4H, s), 2.97 (3 κ 1/4H, s), 3.00-3.26 (2H, a), 3.35-3.48 (2H, a), 3.50-3.77 (7H, a), 4.68 (2 κ 1/6H, d, J=16Hz), 4.70 (2 κ 1/3H, d, J=15Hz), 4.81 (2 κ 1/6H, d, J=16Hz), 4.92 (2 x 1/3H, d, J=15Hz) , 5.13- 5.30 (IH, a), 7.09-7.22 (5H, a), 7.72-7.80 (2H, a), 7.97-8.03 (IH, a), 8.08-8.20 (2H, a), 3.69 (1 x 1/4H, s) , 8.78 (1 κ 3/4H, s) (9) MASS : 504 (M+l) NMR (CDC1 3 , δ) : 2.23-2.33 (1 κ 1/3H, a), 2.47-2.53 (1 x 2/3H, a), 2.69-2.83 (IH, a), 2.85 (3 x 3/4H, s), 2.95 (3 x 1/4H, s), 3.00-3.27 (2H, a), 3.37-3.47 (2H, a), 3.50-3.77 (7H, a), 4.65 (2 x 1/6H, d, 16981 - 494 - J=16Hz), 4.70 (2 κ 1/3H, " d, J=15Hz) , 4.72 (2 κ 1/6H, d, J=16Hz), 4.91 (2 x 1/3H, d, J=15Hz) , 5.20- 5.30 (IH, a), 7.11-7.23 (6H, a), 7.52 (IH, t, J=8Hz), 7.70 (IH, t, J=8Hz), 7.30 (IH, a, J=8Hz), 8.00-8.20 (3H, a) (10) MASS : 504 (M+l) NMR (CDC1 3 , δ) : 2.29-2.52 (IH, a), 2.69-2.83 (IH, a), 2.80 (3 x 3/4H, s), 2.91 (3 x 1/4H, s), 2.98-3.18 (2H, m) , 3.35-3.47 (2H, m) , 3.50-3.68 (7H, a), 4.42 (2 κ 1/6H, d, J=16Hz), 4.61 (2 κ 1/6H, d, J=16Hz) , 4.68 (2 x 1/3H, d, J=15Hz), 4.77 (2 x 1/3H, d, J=15Hz), 5.14-5.28 (IH, a), 7.11-7.30 (6H, a) , 7.40 (IH, dd, J=8, 5Hz), 7.72 (IH, dd, J=8, 2Hz), 7.78 (1 κ 1/4H, s) , 7.82 (1 κ 3/4H, s), 8.08-8.20 (2H, m) , 8.88-8.92 (IH, m) (11) MASS : 455 (M+l) NMR (CDCI3, δ) : 2.31-2.40 (1 κ 1/4H, m, , 2.48-2.56 (1 κ 3/4H, ) , 2.69-2.82 (IH, m) , 2.85 (3 κ 4/5H, s), 2.91 (3 κ 1/5H, s), 2.97-3.20 (2H, a), 3.36-3.42 (2H, a) , 3.50-3.72 (7H, a), 4.43 (2 κ 1/6H, d, J=16Hz), 4.51 (2 x 1/3H, d, J=15Hz) , 4.62 (2 x 1/6H, d, J=16Hz), 4.73 (2 κ 1/3H, d, J=15Hz) , 5.12- 5.22 (IH, a), 7.15-7.29 (5H, a), 8.08-8.16 (IH, a) , 8.33-8.50 (3H, a) (12) MASS : 531 (M+l) NMR (CDCI3, δ) : 2.47-2.60 (IH, a), 2.72 (3 κ 3/4H, s), 2.81 (IH, dd, J=15, 2Hz) 2.85 (3 x 1/4H, s), 2.97-3.11 (2H, a), 3.40-3.48 (2H, a), 3.51-3.77 (7H, a), 4.32 (2 x 1/6H, d, J=16Hz) , 4.41 (2 κ 1/6H, d, J=16Hz), 4.42 (2 κ 1/3H, d, J=15Hz) , 4.65 (2 κ 1/3H, d, J=15Hz), 5.11-5.22 (IH, a), 7.18-7.30 (5H, a) , 7.38-7.42 (IH, a), 7.49 (IH, d, J=8Hz) , 16981 - 495 - 7.61 (1 x 1/4H, d, J=8Hz) , 7.67 (1 κ 3/4H, d, J=8Hz), 8.18 (IH, d, J=8Hz), 8.27-8.32 (IH, ) , 8.40 (1 x 1/4H, s), 8.50 (1 x 3/4H, s), 8.67 (IH, d, J=5Hz), 9.16 (1 κ 1/4H, s) , 9.18 (1 κ 3/4H, s) (13) MASS : 531 (M+l) NMR (CDC1 3 , δ) : 2.42-2.58 (IH, a) , 2.67 (3 κ 5/6H, s), 2.72-2.82 (IH, a), 2.83 (3 x 1/6K, s), 2.99- 3.20 (2H, a), 3.41-3.48 (2H, a), 3.52-3.77 (7H, a), 4.36 (2 x 1/6H, d, J=17Hz), 4.38 (2 κ 1/3H, d, J=15Hz), 4.42 (2 x 1/6H, d, J=17Hz) , 4.71 (2 x 1/3H, d, J=15Hz), 5.12-5.23 (IH, a), 7.15-7.32 (6H, m) , 7.51 (IH, d, J=8Hz), 7.79-7.85 (IH, m) , 8.18 (IH, t, J=8Hz), 8.27-8.40 (2H, m) , 8.49 (IH, s), 8.70 (IH, d, J=5Hz) (14) NMR (CDCI3, δ) : 0.89-1.00 (6H, m) , 2.10 (IH, m) , 2.72 (IH, dd, J=7, 15Hz), 2.84 (IH, dd, J=3, 15Hz) , 2.93 (3H x 1/3, s), 3.04 (3H x 2/3, s), 3.47 (2H, m) , 3.58-3.76 (7H, m) , 4.38 (IH x 2/3, d, J=15Hz) , 4.66 (2H x 1/3, s), 4.79 (IH, t, J=7Hz) , 4.83 (IH x 2/3, d, J=15Hz), 7.22-7.37 (5H m), 8.12 (IH, m) (15) NMR (CDCI3, δ) : 0.84-1.23 (3H, m) , 1.51-1.94 (10H, m) , 2.56-2.67 (IH, m) , 2.82-2.90 (IH, m) , 2.94 (3H κ 1/3, s), 3.02 (3H κ 2/3, s) , 3.46 (2H, m) , 3.62- 3.76 (7H, m) , 4.41 (IH κ 2/3, d, J=15Hz), 4.58 (IH x 1/3, d, J=16Hz), 4.73 (IH x 1/3, d, J=16Hz), 4.77 (IH x 2/3, d, J=15Hz), 5.01 (IH, m) , 7.20-7.38 (5H, m) , 7.91 (IH x 1/3, d, J=7Hz) , 7.97 (IH κ 2/3, d, J=7Hz) (16) NMR (CDCI3, δ) : 2.34 (3H, s), 2.47 (IK, dd, J=7, 15Hz), 2.57 (4H, m) , 2.64 (3H x 2/3, s) , 2.76 (IH, dd, J=4, 7Hz), 2.83 (3H x 1/3, s) , 2.93-3.12 (2H, a), 3.19 (4K, m) , 3.42 (2H, a), 3.66 (7H, a) , 4.17 (IH κ 1/3, d, J=16Hz), 4.27 (IH κ 2/3, d, J=15Hz), 4.33 (IH κ 1/3, d, J=16Hz), 4.55 (IK κ 2/3, d, J=15Hz), 5.10-5.25 (IH, a), 6.81-7.03 (4H, a) , 7.15-7.25 (5H, a), 8.07 (IH 1/3, d, J=7Hz) , 8.13 (IH x 2/3, d, J=7Hz) (17) NMR (CDC1 3 , δ) : 2.34-2.77 (2K, a), 2.79 (3H x 2/3, s), 2.93 (3K κ 1/3, s) , 2.87-3.14 (2H, a) , 3.34- 3.42 (2H, a), 3.50-3.68 (6H, a), 4.29 (IH κ 2/3, d, J=15Hz), 4.42 (IH x 1/3, d, J=16Hz), 4.57 (IH x 1/3, d, J=16Hz), 4.72 (IH κ 2/3, d, =15Hz) , 5.18 (IH, a), 6.97-7.15 (4H, a), 7.26-7.31 (3H, a) , 8.08 (IH x 1/3, d, J=8Hz), 8.20 (IH x 2/3, d, J=8Hz) , 8.43 (2H, d, J=5Hz) (18) NMR (CDCI3, δ) : 2.42-2.57 (IH, a), 2.72 (3H κ 3/4, s), 2.77-2.83 (IH, a), 2.85 (3H κ 1/4, s), 2.95- 3.18 (2K, a), 3.43 (2H, a), 3.63 (6H, a), 3.72 (IH, m) , 4.38 (2H κ 1/4, s) , 4.40 (IH κ 3/4, s), 4.67 (IH κ 3/4, s), 5.17 (IH, a), 7.05-7.25 (7H, m) , 7.57 (2H, m) , 8.10 (IH, s) , 8.17 (IH, t, J=8Hz), 8.54 (IH, s) (19) MASS (m/z) : 504 (M+H) ~ NMR (CDCI3, δ) : 2.38-2.62 (IH, a), 2.69-2.86 (IH, a), 2.72 (3/4 κ 3H, s), 2.90 (1/4 κ 3H, s), 2.94-3.22 (2H, m) , 3.35-3.78 (9H, a) , 4.53 (1/4 x 2H, ABq, Δ=0.10, J=17Hz), 4.54 (3/4 κ IH, d, J=15Hz) , 4.80 (3/4 x IH, d, J=I5Hz), 5.10-5.29 (IK, a), 7.06-7.30 (5H, a), 7.50-8.22 (6H, a), 8.64 (1/4 κ IH, d, J=2Hz), 8.76 (3/4 κ IH, d, J=2Hz) (20) MASS (m/z) : 504 (M+H) + NMR (CDC1 3 , δ) : 2.36-2.61 (IH, a), 2.70-2.86 (IH, a), 2.72 (2/3 κ 3H, s), 2.91 (1/3 x 3K, s) , 2.92-3.20 (2H, a), 3.33-3.80 (9H, a), 4.51 (2/3 x IH, d, J=15Hz), 4.54 (1/3 x 2H, s), 4.85 (2/3 κ IK, a, J=15Hz) , 5.13-5.28 (IH, rc.) , 7.10-7.60 (8H, a), 7.98-8.25 (3H, a), 8.90 (IH, a, J=2Hz) (21) MASS (a/z) : 511 (M+H) τ NMR (CDC1 3 , δ) : 2.21 (3H, s), 2.40-2.61 (IH, a), 2.66 (3/4 κ 3H, s ) , 2.70-2.86 (IK, a), 2.78 (1/4 κ 3H, s), 2.92-3.20 (2H, m) , 3.34-3.78 (9K, a), 4.24 (1/4 κ 2H, ABq, , 4.28 (3/4 κ IH, d, J=15Hz), 4.59 (3/4 κ IH, d, J=15Kz) , 5.05-5.22 (IH, a) , 7.10-7.45 (6H, a), 7.91-8.24 (4H, a) (22) NMR (CDCI3, δ) : 1.80-2.00 (2H, a), 2.22-2.32 (IH, a), 2.30 (3H, s), 2.33-2.42 (4H, a), 2.63 (3 x 2/3H, s), 2.90 (3 x 1/3H, s) , 2.92-3.12 (2H, a), 3.27- 3.40 (IH, m) , 3.36-3.47 (2H, a), 3.53-3.70 (2H, m) , 4.32-4.43 (3 x 2/3H, a), 4.70 (3 x 1/3H, d, J=15Hz), 5.19 (IK, q, J=8Hz), 7.01-7.12 (2H, m) , 7.20-7.32 (8H, a), 7.93 (1 κ 1/3H, d, J=8Hz) , 8.00 (1 x 2/3H, d, J=8Hz) (23) NMR (CDCI3, δ) : 2.53-3.03 (4K, a), 3.46 (2H, a), 3.66 (6H, a), 3.79-3.89 (IH, a), 4.61-4.71 (IH, a), 4.93 (IH, a, J=16Hz), 5.42 (IH, d, J=16Hz), 6.92 (IH, d, J=8Hz), 7.01 (IH, t, J=8Hz), 7.14 (IH, t, J=8Hz), 7.20-7.32 (6H, a), 8.45 (IH, t, J=7Hz) (24) MASS (a/z) : 459 (M+l) + NMR (CDCI3, δ) : 2.40-2.63 (IH, a), 2.73-2.94 (IH, a), 2.84 (3H x 2/3, s), 2.92 (3H x 1/3, s), 3.11-3.50 (5H, a), 3.51-3.79 (7H, a), 4.39 (IK x 2/3, d, J=14.5Hz), 4.50 (IH x 2/3, s), 4.70 (IH x 2/3, d, J=14.5Hz), 5.10-5.23 (IH, a), 6.79-6.96 (2H, a), 7.01-7.20 (3H, a), 7.22-7.35 (4H, a) , 8.12 (IH x 1/3, br a, J=7.5Hz), 8.21 (IK x 2/3, br d, J=7.5Hz) (25) MASS (a/z) : 533 (M-rH) ~ NMR (CDC1 3 , δ) : 2.28-2.55 (IH, a), 2.67 (2/3 κ 3H, s), 2.69-2.85 (IH, a), 2.87 (1/3 x 3H, s) , 2.92- 3.16 (2H, a), 2.33-3.79 (9H, a), 3.94 (3H, s), 4.32 (2/3 x IH, d, J=15Hz), 4.36 (1/3 κ 2H, A3q, Δ=0.08, J=17Hz) , 4.71 (2/3 κ IH, d, J=15Hz), 5.10-5.25 (IH, m) , 6.50 (1/3 x IH, d, J=2Hz) , 6.52 (2/3 x IH, a, J=2Hz), 6.95-7.42 (8H, a), 7.65-7.75 (2H, a), 8.02- 8.21 (IH, a) (26) MASS (a/z) : 497 (M+H) * NMR (CDCI3, δ) : 2.33-2.52 (IH, a), 2.61 (2/3 κ 3H, s), 2.71-2.36 (IH, a), 2.76 (1/3 κ 3H, s), 2.91- 3.15 (2H, a), 3.05 (1/3 κ 6K, s), 3.07 (2/3 x 6H, s), 3.35-3.76 (9H, a) , 3.95 (1/3 κ IH, a, J=17Hz) , 4.28 (1/3 κ IH, d, J=17Hz) , 4.34 (2/3 κ 2H, ABq, Δ=0.22, J=15Hz), 5.03-5.33 (IH, a) , 6.41 (1/3 κ IK, d, J=9Hz), 6.46 (2/3 κ IH, d, J=9Hz), 7.02-7.33 (6H, a), 7.88 (1/3 κ IK, d, J=2Hz), 7.97 (2/3 κ IH, d, J=2Hz), 8.06-8.19 (IH, a) (27) MASS (a/z) : 519 (M+H) + NMR (CDCI3, δ) : 2.40-2.62 (IH, a) , 2.70-2.85 (IH, a), 2.72 (3/4 κ 3H, s) , 2.85 (1/4 κ 3H, s) , 2.92-3.22 (2H, a), 3.35-3.79 (9H, m) , 4.37 (1/4 x 2H, s), 4.53 (3/4 κ 2H, ABq, Δ=0.22, J=15Hz) , 5.08-5.25 (IH, a), 6.98-7.33 (11H, a), 7.82 (IH, s) , 8.10- 8.22 (IH, a) (28) MASS (a/z) : 521 (M+H) + NMR (CDCI3, δ) : 2.26-2.52 (IH, a), 2.59 (3H, s), 2.66 (3/5 x 3H, s), 2.68-2.82 (IH, a), 2.83 (2/5 x 3H, s), 2.92-3.16 (2H, a), 3 ' .35-3.80 (9K, a), 3.70 (2/5 κ 3H, s), 3.72 (3/5 κ 3H, s) , 4.23 (2/5 κ IH, d, J=17Hz), 4.56 (2/5 x IH, d, J=17Hz) , 4.61 (3/5 x 2H, ABq, Δ=0.07, J=15Hz), 5.06-5.25 (IH, a), 6.86- 7.50 (8H, a), 8.05-8.22 (IH, a) (29) MASS (a/z) : 443 (M+H) + NMR (CDC1 3 , δ) : 2.43-2.67 (IH, m) , 2.71-3.03 (3H, m) , 2.90 (2/3 x 3H, s), 2.92 (1/3 x 3H, s), 3.33-3.78 (9H, ) , 4.38 (2/3 κ IH, d, J=15Hz) , 4.54 (1/3 κ 2K, ABq, Δ=0.08, J=17Hz), 4.72 (2/3 κ IH, d, J=15Hz), 5.02-5.16 (IH, a), 6.22 (1/3 x IH, s), 6.29 (2/3 x IH, s), 7.03-7.39 (7H, a), 8.02-8.23 (IH, ) (30) MASS (m/z) : 457 (M+H) + NMR (CDCI3, δ) : 2.38-2.57 (IH, a) , 2.69 (2/3 x 3H, s), 2.71-2.87 (IH, a), 2.84 (1/3 κ 3H, s) , 2.90- 3.20 (2H, a), 3.36-3.75 (9H, a), 3.80 (1/3 κ 3H, s), 3.87 (2/3 x 3H, s) , 4.15 (2/3 x IH, d, J=15Hz) , 4.15 (1/3 x 2E, ABq, J=17Hz), 4.45 (2/3 κ IH, d, J=15Hz), 5.02-5.29 (IH, a), 6.98-7.35 (7H, a) , 8.04-8.20 (IH, a) (31) MASS (a/z) : 487 (M+HA NMR (CDCI3, δ) : 2.25-2.58 (IH, a), 2.58-2.80 (IH, a), 2.77 (2/3 κ 3H, s), 2.82-3.14 (2H, a), 2.91 (1/3 x 3K, s), 3.30-3.80 (9H, a), 4.30 (2/3 κ IK, d, J=15Hz), 4.49 (1/3 κ 2H, ABq, J=17Hz), 4.72 (2/3 x IH, a, =15Hz;. , 5.05-5.23 (IH, m) , 6.90-7.40 (9K, a), 6.04 (1/3 x IH, d, J=9Hz), 6.15 (2/3 κ IH, a, J=9H∑) (32) MASS (a/z) : 443 (M+H) " " NMR (CDCI3, δ) : 2.41-2.64 (IH, a), 2.73-2.96 (IH, a) , 2.83 (2/3 κ 3H, s), 2.90 (1/3 κ 3H, s), 2.96-3.20 (2H, a) , 3.38-3.81 (9H, a), 4.33 (2/3 κ IK, d, J=15Hz) , 4.50 (1/3 κ 2H, ABq, Δ=0.07, J=17HZ) , 4.79 (2/3 κ IH, d, J=15Hz) , 5.15-5.31 (IH, m) , 6.10 (IH, a) , 6.21-6.31 (IH, a), 7.07-7.40 (6H, a), 8.11 (1/3 κ IH, d, J=8Hz) , 8.19 (2/3 x IK, d, J=8Hz) (33) MASS : 505 (M+l) NMR (CDC1 3 , δ) :2.38-2.60 (IH, a), 2.78 (3 x 2/3H, s) , 2.79 (IH, t, J=16Hz), 2.91 (3 κ 1/3H, s) , 2.98-3.19 (2H, a), 3.38-3.49 (2H, a), 3.52-3.70 (6H, a), 3.71-3.80 (IH, a), 4.51 (2 κ 1/6H, d, J=16Hz) , 4.60 (2 κ 1/6H, d, J=16Kz), 4.65 (2 κ 1/3H, d, J=15Hz), 4.81 (2 κ 1/3H, d, J=15Hz), 5.13-5.28 (IH, a), 7.13-7.29 (5H, a), 7.31 (1 κ 1/3H, d, J=8Hz) , 7.43 (1 κ 2/3H, d, J=8Hz), 7.78 (1 κ 1/3H, s), 7.83 (1 κ 2/3H, s), 7.99-8.03 (IH, m) , 8.14 (1 κ 1/3H, d, J=8Hz), 8.19 (1 κ 2/3H, d, J=8Hz), 8.82 (2H, s) (34) MASS : 503 (M+l) NMR (CDCI3, δ) : 2.12 (3 x 2/3H, s), 2.19-2.30 (1 x 1/3H, s) , 2.41-2.51 (1 x 2/3H, s), 2.66-2.89 (IH, a), 2.79 (3 κ 1/3H, s), 3.30-3.48 (3H, a), 3.52- 3.79 (8H, a), 4.03 (2 x 1/6H, d, J=16Hz), 4.27 (2 x 1/6H, d, , 4.49 (2 x 1/3H, d, J=15Hz) , 5.29-5.41 (IH, a), 6.77-6.83 (2 x 1/3K, a), 6.93-7.02 [2 x 2/3H, a), 7.13-7.31 (5H, a), 7.32-7.60 (3H, a), 7.69-7.87 (2K, a , 8.30-8.39 (IK, a) (35) MASS : 454 (M+l) NMR (CDCI3, δ) : 2.33-2.60 (IH, a), 2.62-2.79 (IH, a), 2.80 (3 κ 2/3H, s), 2.92 (3 κ 1/3H, s), 2.86-3.19 (2H, a), 3.33-3.48 (2H, a), 3.49-3.72 (7H, a, , 4.4C (2 x I/3H, d, J=15Hz), 4.45 (2 x 1/6H, a, J=I6Hz), 4.53 (2 x 1/6H, d, J=16Hz) , 4.63 12 x 1/3H, d, J=15Hz), 5.08-5.22 (IH, m) , 6.98- 7 .20 (3H, m) , 7.22-7.37 (3H, m) , 7.43 (1 x 1/3H, d, J=8Hz), 7.51 (I x 2/3H, d, J=8Hz), 8.11 (I x 1/3H, d, J=8Hz), 8.22 (1 κ 2/3H, d, J=8Hz) , 8.36 (1 κ 1/3H, s), 8.45 (1 κ 2/3H, s) , 8.45 (IH, s) (36) MASS : 484 (M-ri) NMR (CDC1 3 , δ) : 2.43-2.70 (IH, a) , 2.61 (3 κ 3/4H, s), 2.73-2.88 (IH, m) , 2.79 (3 κ 1/4H, s), 2.93- 3.18 (2H, m) , 3.40-3.49 (2H, m) , 3.51-3.70 (6H, a), 3.71-3.80 (IH, a), 3.91 (3K, s), 4.10 (2 κ 1/6H, d, J=16Hz), 4.23 (2 κ 1/3K, d, J=15Hz) , 4.30 (2 κ 1/6H, d, J=16Hz), 4.53 (2 x 1/3H, d, J=15Hz) , 5.03- 5.23 (IH, m) , 6.59-6.70 (IH, m) , 7.07-7.33 (6H, m) , 7.83 (1 x 1/4H, s), 7.93 (1 x 3/4H, s), 8.10-8.22 (IH, m) (37) MASS : 419 (M+l) NMR (CDCI3, δ) : 0.79-1.00 (3H, a), 1.15-1.48 (4H, m) , 1.55-1.90 (2H, m) , 2.58-2.72 (IH, m) , 2.80-2.90 (IH, m) , 2.92 (3 x 1/3H, s), 2.97 (3 x 2/3H, s), 3.40-3.50 (2H, m) , 3.51-3.70 (6H, m) , 3.71-3.79 (IH, m) , 4.43 (2 x I/3H, a, J=15Hz), 4.60 (2 x 1/6H, d, J=16Hz), 4.68 (2 κ I/6H, d, J=16Hz), 4.75 (2 x 1/3H, d, J=15Hz), 4.86-4.99 (IH, m) , 7.17-7.40 (5H, m) , 8.07 (1 x 1/3H, d, J=8Hz) , 8.12 (1 κ 2/3H, d, J=8Hz) Preparation 67 Starting Compound (1.14 g) was dissolved m 30O methylamine in methanol (7 al) and heated at 50°C for 1 hour. After the aixture was alloweα to cool to rooa temperature, the solvent was evaporated then suspended in etnanol (15 ml) . Sodium borohydride (277 ag) was added to the suspension with ice-cooling, and the aiκture was stirred at 0°C for 1 hour. After the solvent was evaporated, the residue was diluted with water, eκtracted three tiaes with chlorofora, and dried over aagnesiua sulfate. Evaporation of the solvent followed by coluan chroaatography (silica gel, chiorofora/aethanol = 5/1) gave Object Coapound (708 ag) as a colorless oil. MASS (m/z) : 173 (M+H) " NMR (CDCI 3 , δ) : 2.51 (3H, s), 3.96 (2H, s), 7.48-7.85 (3H, a), 8.05-8.14 (2H, a), 8.89 (IH, d, J=2Hz) Preparation 68 Starting Coapound (1.30 g) was dissolved in 30- methylamine in methanol (8 ml) and heated at 60°C for 1 hour. After the mixture was allowed to cool to rooa temperature, the solvent was evaporated then suspended in ethanol (20 ml) . The suspension was cooled in ice and added sodium borohydride (305 ag) . The aixture was stirred at the teaperature fcr 1 hour and the solvent was evaporated. The residue was diluted with water, and extracted three times with chloroform. The organic layer was washed with brine and dried over potassium carbonate. Evaporation of the solvent followed by column chromatography (silica gel, chloroform/methanol = 5/1) gave Object Compound (923 mg) as a light yellow oil. MASS (m/z) : 180 (M+H) + NMR (CDCI3, δ) : 2.18 (3H, s), 2.43 (3H, s), 3.70 (2K, s), 7.67 (IH, dd, J=9, 2Hz), 8.15 (IH, d, J=9Hz), 3.20 (IH, d, J=2Hz), 8.31 (IK, br s) Preparation 69 The following object compounds were obtained according to a similar manner to that of Preparation 22, 23, 25, 67 or 68. (1) MASS (m/z) : 220 (M + +l) NMR (CDC1 3 , δ) : 2.35 (3H, s), 2.44 (3H, s), 2.57 (4H, t, J=5Hz) , 3.19 (4K, t, J=5Hz), 3.65 (2H, s) , 6.89 (2H, d, J=8Hz) , 7.21 (2H, d, J=8Hz) (2) MASS (m/z) : 173 (M+H) ÷ NMR (CDCI3, δ) : 2.51 (3H, s), 3.96 (2H, s) , 7.40 (IH, dd, J=9, 5Hz), 7.70 (IH, d, J=9Hz), 7.77 (IH, s) , 8.08 (IH, d, J=9Hz) , 8.13 (IH, d, J=9Hz) , 8.89 (IH, d, J=5Hz) (3) Mass : 200 (M+l) NMR (CDCI3, δ) : 2.45 (3H, s), 3.81 (2H, s) , 7.28-7.32 (IH, m) , 7.80 (2H, t, J=7Hz) , 8.36 (IH, a, J=7Hz) , 8.38 (IH, d, J=7Hz), 8.61 (IH, s) , 8.67 (IH, d, J=5Hz) (4) MASS : 200 (M+l) NMR (CDC1 3 , δ) : 2.49 (3H, s), 3.80 (2H, s) , 7.39 (IH, dd, J=8, 5Hz), 7.63 (IH, d, J=8Hz) , 7.80 (IH, dd, J=8, 2Hz), 8.31 (IH, dd, J=8, 2Hz), 8.63-8.68 (2K, m) , 9.20 (IH, s) (5) MASS : 125 (M+2) NMR (CDCI3, δ) : 2.50 (3H, s) , 3.90 (2H, s) , 8.51 (2H, d, J=16Hz), 8.62 (IH, s! (6) MASS : 173 (M+l) NMR (CDCI3, δ) : 2.52 (3H, s) , 4.00 (2H, s) , 7.38 (IH, dd, J=8, 3Hz), 7.58 (IH, d, J=8Hz) , 7.8C (IK, d, J=8Hz) , 7.99 (IH, s), 8.13 (IH, d, J=8Hz) , 8.90 (IH, d, J=5Hz) (7) MASS : 173 (M+l) NMR (CDCI3, δ) : 2.52 (3H, s), 4.07 (2K, s), 7.46 (IH, d, J=8Hz), 7.51 (IH, :, J=8Hz), 7.73 (IH, z , J=8Hz), 7.80 (IH, d, J=8Hz), 8.07 (IH, d, J=8Hz), 8.12 (IH, d, J=8Hz) (8) MASS : 174 (M+l) NMR (CDC1 3 , δ) : 2.58 (3H, s), 4.12 (2K, s) , 7.70-7.80 (2H, a), 8.03-8.12 (2H, a), 8.90 (IH, s) (9) MASS : 125 (M+l) NMR (CDCI3, δ) : 2.49 (3H, s), 3.89 (2H, s), 7.37 (IH, d, J=7Hz), 8.67 (IH, d, J=7Hz) , 9.17 (IH, s, (10) MASS : 173 (M+l) NMR (CDCI3, δ) : 2.48 (3H, s) , 4.00 (2K, sj, 7.60 (IH, d, J=8Hz), 8.02 (IH, s), 8.09 (IH, d, J=8Hz), 8.80- 8.87 (2H, m) (11) MASS (m/z) : 126 (M+H) + NMR (CDCI3, δ) : 2.45 (3H, s), 3.61 (2H, s), 3.87 (3H, s), 7.29 (IH, s), 7.41 (IH, s) (12) mp : 102-103°C MASS (m/z) : 159 (M-30A, 190 (M+H) ÷ NMR (CDCI3, δ) : 2.45 (3H, s), 2.58 (3H, s) , 3.70 (3H, s), 3.85 (2H, s) , 7.22 (2H, s), 7.58 (IH, s) (13) MASS (m/z) : 188 (M+H) ÷ NMR (CDCI3, δ) : 2.48 (3H, s), 3.79 (2H, s), 7.19 (IH, S), 7.27 (IH, s), 7.35 (2H, d, J=8Hz) , 7.42 (2H, a, J=8Hz), 7.83 (IH, s) (14) MASS (m/z) : 166 (M+H) τ NMR (CDCI3, δ) : 2.42 (3H, s) , 3.07 (6H, s), 3.61 (2H, s), 6.51 (IK, d, J=9Hz), 7.46 (IH, dd, J=9, 2Hz), 8.07 (IH, d, J=2Hz) (15) MASS (m/z) : 202 (M+H) + NMR (CDC1 3 , δ) : 2.45 (3H, s), 3.78 (2H, s), 3.93 (3H, s), 6.52 (IH, d, J=2Hz), 7.34 (2H, d, J=8Hz), 7.37 (IH, d, J=2Hz), 7.74 (2K, d, J=8Kz) Preparation 70 A slurry of Starting Compound (6.45 g) , selenium dioxide (7.48 g) , and water (1.2 al) in 285 al of dioxane was refluxed for 6 days. The aixture was filtered while still warm, and the filtrate was evaporated. The residue was purified using silica gel coluan chromatography (eluent : hexane/ethyl acetate (2:1)) yielding Object Compound (380 mg) . MASS : 158 (M+l) NMR (CDCI3, δ) : 7.52-7.67 (IH, m) , 7.93 (IH, d, J=8Hz), 8.07 (IH, d, J=8Hz) , 8.23 (IH, d, J=8Hz) , 8.53 (IH, s), 9.03 (IH, d, J=5Hz), 10.25 (IH, s) Preparation ~ l The following object compounds were obtained according to a similar manner to that of Preparation 70. (1) mp : 65-68°C NMR (CDCI3, δ) : 7.68 (IH, t, J=8Hz) , 7.82 (IH, t, J=8Hz), 7.90 (IH, d, J=8Hz) , 8.02 (IH, d, J=8Hz), 8.27 (IH, d, J=8Hz), 8.31 (IH, d, J=8Hz), 10.22 (IH, s) (2) mp : 108-109 β C MASS : 159 (M+l) NMR (CDCI3, δ) : 7.87-7.99 (2H, m) , 8.18-8.29 (2H, a) , 9.40 (IH, s), 10.29 (IH, s) (3) NMR (CDCI3, δ) : 7.85 (IH, d, J=8Hz), 9.04 (IH, d, J=8Hz), 9.47 (IH, s) 96/16981 - 506 - (4) mp : 137-139°C MASS : 159 (M+l) NMR (CDC1 3 , δ) : 8.23 (IH, d, J=8Hz), 8.29 (IH, d, J=8Hz), 8.60 (IH, s), 8.97 (2H, s), 10.27 (IH, s) Preparation 72 To a solution of dimethylsulfoκide (0.86 al) in dichloroaethane (20 al) was added oκalyl chloride (0.53 al) at -78°C. After the solution was stirred at -78°C for 10 ainutes, Starting Coapound (900 ag) in dichloroaethane (10 al) was added thereto. The solution was stirred at -78°C fo 15 ainutes, and triethyl amine (3.7 al) was added thereto. The solution was allowed to aabient teaperature and stirred for 1 hour. Water was added thereto and the aqueous layer was extracted with chlorofora. The organic layer was dried over magnesium sulfate and concentrated. The residue was purified by chromatography on silica gel [chloroform-methano (30:1) ] to give Object Compound (720 mg) as a solid, ap : 85-88°C MASS : 185 (M+l) NMR (CDCI3, δ) : 7.37-7.42 (IH, a), 7.82-7.90 (IH, a), 8.29 (IH, d, J=8Hz), 8.51 (IH, d, J=8Hz) , 8.62 (IH, d, J=8Hz), 8.72 (IH, d, J=5Hz) , 9.11 (IH, s), 10.1 (IH, s) Preparation 73 The following object coapounds were obtained according to a similar manner to that of Preparation 72. ' (1) NMR (CDCI3, δ) : 8.70 (2H, dd, J=12, 3Hz) , 9.19 (IK, s), 10.21 (IH, s) (2) mp : 66-72°C MASS : 185 (M+l) NMR (CDCI3, δ) : 7.48 (IH, da, J=8, 5Hz), 7.95 (IH, a, J=8Hz) , 8.29 (IH, dd, J=8, 5Hz), 8.42 (IH, dd, J=8, 2Hz), 8.72 (IH, d, J=5Hz) , 9.17 (IH, d, J=2Hz) , 9.30 (IH, d, J=2Hz), 10.20 (IH, s) Preparation 7 To a solution of Starting Compound (1.15 g) in anhydrous tetrahydrofuran (20 ml) at -78°C was added 5.04 ml of a 1M solution of lithium aluminium hydride in tetrahydrofuran. The reaction miκture was allowed to warm to the temperature (-20°C) which the solution became completely homogeneous. The reaction miκture was stirred at this temperature for 30 minutes and then cooled back down to -78°C and quenched slowly with 15 ml of 10c aqueous tetrahydrofuran. After being warmed to ambient temperature, the reaction mixture was stirred with dry Celite for 15 minutes and then filtered. The solution was then concentrated under reduced pressure. The residue was purified by chromatography on silica gel [chloroform-methanol (10:1)] to give Object Compound (900 mg) as an oil. MASS : 187 (M+l) NMR (CDCI3, δ) : 3.07 (IH, br s), 4.74 (2H, s), 7.29- 7.32 (IH, m) , 7.78-7.85 (2H, m) , 8.31 (2H, t, J=8Hz), 8.57 (IH, s), 8.66 (IH, d, J=6Hz) Preparation 75 The following object compounds were obtained according to a similar manner to that of Preparation 74. (1) mp : 92-95 β C MASS : 187 (M+l) NMR (CDCI3, δ) : 2.57 (IH, br ' s), 4.80 (2H, s), 7.40 (IH, dd, J=12, 5Hz), 7.70 (IH, dd, J=8Hz) , 7.81 (IH, dd, J=8, 2Hz), 8.29 (IH, dd, J=8, 2Hz) , 8.60 (IH, d, J=5Hz), 8.67 (IH, s) , 9.02 (IH, s) (2) MASS : 112 (M+2) NMR (CDC1 3 , δ) : 3.32 (IH, t, J=7Hz) , 4.87 (2H, d, J=7Hz), 8.50-8.52 (2H, m) , 8.62 (IH, s) Preparation 76 To a mixture of Starting Compound (434 mg) and N,0- dimethylhydroκylamine-hydrochloride (246 mg) in dichloromethane-N,N-dimethylformamide (1:1, 5 ml) was added l-ethyl-3- (3-dimethylaminopropyl) carbodiimide-hydrochloride (534 mg) at room temperature. The reaction mixture was stirred at room temperature for 12 hours. The solution was diluted with ethyl acetate, washed twice with saturated sodium bicarbonate, once with brine, and dried over magnesium sulfate. Purification by flash chromatography (silica gel, hexane/ethyl acetate = 1/3) gave Object Compound (303 mg, MASS (m/z) : 217 (M+H) + NMR (CDCI3, δ) : 3.42 (3H, s), 3.56 (3H, s) , 7.46 (IH, dd, J=9, 5Hz), 8.06 (2H, ABq, Δ=0.12, J=9Hz) , 8.21 (IH, s), 8.22 (IH, dd, J=9, 2Hz) , 8.98 (IH, dd, J=5, 2Hz) Preparation 77 To an ice-cooled solution of Starting Compound (543 mg) in dry ether (6.3 ml) was added lithium aluminum hydride (96 mg) and stirred at 0°C for 1 hour. After the reaction mixture was diluted with ether, lOo citric acid (0.3 ml) was added dropwise with vigorous stirring. The precipitate was filtered off, and the residue was purified by column chromatography (silica gel, hexane/ethyl acetate = 1/1) to give the product (268 mg) as white crystals, mp : 70-71°C MASS (m/z) : 158 (M+H) + NMR (CDCI3, δ) : 7.52 (IH, dd, J=9, 3Hz) , 8.21 (2H, ABq, Δ=0.04, J=9Hz) , 8.33 (IH, d, J=9Hz), 8.36 (IH, s ) , 9 . 05 ( IH, d, J=3Hz ) , 10 . 21 ( IH, s ) Preparation 78 A mixture of Starting Compound (3.0 g) , 1-methylpiperazine (2.7 g) and potassium carbonate (4.0 g) in N,N-dimethylformamide (5 ml) was stirred at 120°C for 2 hours. After cooling potassium carbonate was removed by filtration. Evaporation of N,N-dimethylformamide in vacuo gave a residue which was taken up in chloroform and water. The organic solution was washed with water, and dried. Evaporation of solvent gave a residue which was chromatographed on silica gel. Elution with methanol- chloroform (1:50) afforded Object Compound (2.63 g) MASS (m/z) : 205 (M + +l) NMR (CDC1 3 , δ) : 2.36 (3H, s) , 2.55 (4H, t, J=5Hz) , 3.41 (4H, t, J=5Hz), 6.92 (2H, d, J=8Hz) , 7.75 (2H, d, J=8Hz), 9.78 (IH, s) Preparation 79 The following object compounds were obtained according to a similar manner to that of Preparation 29. (1) MASS : 236 (M+l) NMR (CDC1 3 , δ) : 1.48 (9H, s), 2.26 (3H, s) , 2.79 (3H, s), 4.43 (2H, s) , 7.09-7.19 (4H, m) (2) MASS : 336 (M+l) NMR (CDC1 3 , δ) : 1.47 (9H, s), 2.33 (3H, s) , 2.80 (3H, br s), 4.38 (2H, s) , 6.97-7.08 (3H, m) , 7.22 (IH, dd, J=15, 8Hz) Preparation 80 The following object compounds were obtained according to a similar manner to that of Preparation 3, 4, 8 or 41. (1) MASS : 136 (M+l) NMR (CDC1 3 , δ) : 2.37 (3H, s), 2.51 (3H, s), 2.71 (2H, s), 7.13-7.18 (3H, a), 7.23- 7 .30 (IH, ) (2) MASS : 136 (M+l) NMR (CDCI3, δ) : 2.35 (3H, s), 2.43 (3H, si, 3.70 (2H, sj , 7.06-7.27 (4H, a) Preparation 81 The following object compound was obtained accordidng t a similar manner to that of Preparation 6. MASS : 351 (M+l) NMR (CDCI3, δ) : 1.42 (9H, s), 2.87 (IH, dd, J=17, 5Hz), 2.91 (3H, s), 2.97 (3H, s), 3.17 (IH, dd, J=16, 5Hz), 4.58-4.63 (IK, m) , 5.13 (2 x 1/2H, d, J=12Hz), 5.21 (2 x 1/2H, d, J=12Hz), 5.88 (IH, d, J=8Hz), 7.29-7.37 (5H, s) Preparation 82 The following object compound was obtained according to a similar aanner to that of Preparation 10. MASS : 261 (M+l) NMR (CDCI3, δ) : 1.38 (9H, s) , 2.67-2.77 (IH, a), 3.00 (3H, s), 3.05 (3H, s), 3.21 (IH, a, J=15Hz), 4.51 (IH, t, J=8Hz), 5.88 (IH, br s, Preparation 83 The following object coapound was obtained according to a siailar aanner to that of Preparation 10. NMR (CDCI3, δ) : 1.42 (9H, s), 1.82-1.98 (IK, a), 2.00-2.18 (IH, a), 2.38-2.60 (2H, a), 2.70 (3 x 2/3H, s), 2.83 (3 κ 1/3H, s), 3.00-3.15 (2H, a), 4.28-5.20 (3H, m) , 5.21-5.30 (IH, m) , 5.50-5.60 (IH, m) , 6.90-7.00 (2H, m) , 7.09-7.30 (8H, a) , 8.18-8.30 (IH, m) Preparation 84 The following object compound was obtained according to a similar manner to that of Preparation 1. NMR (CDCI3, δ) : 1.47 (9H, s), 1.90-2.00 (IH, m) , 2.00-2.20 (IH, m) , 2.31 (3H, s) , 2.32-2.53 (6H, m) , 2.63 (3 x 2/3H, s), 2.82 (3 x 1/3H, s), 2.98-3.10 (2H, m) , 3.40-3.48 (2H, a), 3.60-3.70 (2H, m) , 4.07-4.18 (IH, m) , 4.20 (2 x 1/4H, d, J=16Hz), 4.32 (2 x 1/4H, d, J=16Hz), 4.35 (2 x 1/4H, d, J=15Hz) , 4.61 (2 κ 1/4H, d, J=15Hz), 5.11 (IH, q, J=8Kz) , 5.58-5.66 (IH, m) , 6.98 (2 κ 1/3H, d, J=8Hz) , 7.08 (2 x 2/3H, d, J=8Hz), 7.12-7.31 (8H, m) , 7.45-7.55 (IH, m) Preparation 95 The following object compound was obtained according to similar manners to those of Preparations 10 and 6. MASS (m/z) : 567 (M+H) ÷ NMR (CDC1 3 , δ) : 1.45 (9H, s) , 1.8-2.2 (2H, a), 2.3- 2.6 (2H, m) , 2.63 (2/3 x 3H, s), 2.84 (1/3 x 3H, s), 3.0-3.1 (2H, a), 3.4-3.5 (2H, m) , 3.6-3.7 (6H, m) , 4.1-4.2 (IK, ) , 4.28 (1/3 x 2H, ABq, Δ=0.20, J=15Hz), 4.50 (2/3 κ 2H, ABq, Δ=0.22, J=15Hz) , 5.1- 5.2 (IH, m) , 5.5-5.6 (IH, a), 7.0-7.6 (11H, a) Preparation 95 To a stirred suspension of sodiua hydride (0.31 g, 60%) in N,N-dimethylformamide (10 ml) was added a solution of Starting Compound (0.7 g) in dimethylformamide (2 ml) at 0°C. The mixture was stirred at room temperature for 1 hour. To this mixture was added dropwise benzylbromide (0.63 g) at 0°C. The mixture was stirred at room temperature for 1 hour. The reaction mixture was poured into water and extracted with ethy acetate. The organic layer was washed with water and dried. Evaporation of solvent gave a residue which was chromatographe on silica gel. Elution with a mixture of methanol-chloroform (1:100) provided Object Compound (0.56 g) . MASS (m/z) : 253 (M + +l) NMR (CDC1 3 , δ) : 2.94 (IH, t, J=15Hz) , 3.15 (IH, dd, J=5, 15Hz), 3.72 (IH, dd, J=5, 15Hz) , 4.97 (IH, d, J=16Hz), 5.40 (IH, d, J=16Hz) , 6.88 (IH, d, J=8Hz) , 6.99 (IH, t, J=8Hz), 7.13 (IH, t, J=8Hz) , 7.20-7.33 (6H, m) Preparation 87 A mixture of Starting Compuond (4.85 g) and N,N- dimethylformamide dimethyl acetal (17 ml) in benzene (12.5 ml) was distilled. The distillation was continued by occasional addition of benzene until most of the starting material was consumed. Then water was added thereto, the mixture was extracted three times with ether, washed with brine, and dried over magnesium sulfate. The product was purified by column chromatography (silica gel, chloroform/methanol = 30/1) followed by recrystallization from toluene to give Object Compound (4.48 g) of yellow crystals. mp : 99-100°C MASS (m/z) : 248 (M+H) + NMR (CDC1 3 , δ) : 1.40 (3H, t, J=7Hz) , 2.95 (3H, br s), 3.18 (3H, br s) , 4.40 (2H, q, J=7Hz) , 6.22 (IH, d, J=13Hz), 7.83 (IH, d, J=13Hz) , 7.92 (2H, d, J=7Hz) , 8.05 (2H, d, J=7Hz) Preparation 88 Starting compound (2.47 g) was dissolved in acetic acid (10 ml) and methylhydrazine (519 mg) was added dropwise at room temperature. The reaction mixture was stirred at the temperature for 1 hour. The aixture was neutralized with 15 sodiua hydroxide with ice-cooling, extracted three tiaes with ethyl acetate, washed with brine, and dried over magnesium sulfate. The crude product was the 57:43 isomeric mixture of Object Coapound A and Object Coapound 3 determined by NMR. The two isomers were separated by column chromatography (silica gel, chloroform) , and the first eluate was Object Compound A as white crystals (1.1I g) and the second was Object Compound 3 as an oil (646 mg) . Object Compound A mp : 79-80°C MASS (m/z) : 231 (M+H) + NMR (CDC1 3 , δ) : 1.41 (3H, t, J=7Hz) , 3.97 (3H, s), 4.38 (2H, q, J=7Hz) , 6.60 (IH, d, J=2Hz), 7.40 (IH, d, J=2Hz), 7.85 (2H, d, J=7Hz) , 8.06 (2H, d, J=7Hz) Object Compound B MASS (m/z) : 231 (M+H) + NMR (CDCI3, δ) : 1.41 (3H, t, J=7Hz) , 3.91 (3H, s), 4.41 (2K, q, J=7Hz), 6.37 (IK, d, J=lHz) , 7.49 (2H, d, J=7Hz), 7.52 (IH, a, J=lHz) , 8.12 (2H, a, J=7Hz) Preparation 89 To an ice-cooled suspension of lithium aluminum hydride (183 ag) in tetrahydrofuran (12 al) was added Starting Coapound (1.08 g) in tetrahydrofuran (12 al) . After the mixture was stirred at 0°C for 1 hour, sodium fluoride (790 mg) and water (0.25 ml) were successively added thereto and the whole was stirred at room temperature for 1 hour. The precipitate formed was filtered off, and the resulting solution was evaporated tc give Object Compound (876 mg) as white crystals. ap : 92-93°C MASS (a/z) : 189 (M+H A NMR (CDC1 3 , δ) : 3.92 (3H, s), 4.69 (2H, d, J=5Hz) , 6.52 (IH, d, J=lHz) , 7.36 (IH, d, J=IHz) , 7.38 (2 d, J=8Hz) , 7.77 (2H, a, J=8Hzι Preparation 90 To an acetone (45 ml) solution of Starting Compound (8 mg) was added activated manganese dioκide powder (7.82 g) a the miκture was refluκed for I hour. After the miκture was filtered, the Object Compound was isolated by column chromatography (silica gel, hexane/ethyl acetate = 1/1) as white crystals (550 mg) . mp : 88-90°C MASS (m/z) : 187 (M+H) τ NMR (CDCI3, δ) : 3.97 (3H, s), 6.62 (IH, d, J=2Hz), 7.41 (IH, d, J=2Hz) , 7.82-8.03 (4H, m) , IC.OI (IH, s) Preparation 91 To a methanol (20 ml) solution of Starting Compound (2.36 g) was added 50% aqueous dimethylamine solution (20 ml), and the aixture was refluxed fcr 12 hours. After the aethanol was evaporated, sodium chloride was added thereto, and the mixture was extracted three times with ether. The organic layer was dried over magnesium sulfate. Evaporatio of the solvent followed by column chromatography (silica ge hexane/ethyl acetate = 20/1) gave Object Compound (1.39 g) white crystals. p : 40-41°C MASS (m/z) : 201, 203 (M+H)" NMR (CDCI3, δ) : 3.03 (6H, s), 6.39 (IH, d, J=9Hz), 7.47 (IH, dd, J=9, 2Hz) , 8.14 (IH, d, J=2Hz) Preparation 92 To a stirred solution of Starting Compound (1.33 g) in tetrahydrofuran (16.5 ml) at -78°C was added n-butyllithium (1.6M in hexane, 4.4 ml). After 2 hours, N,N- dimethylformamide (968 mg) was added thereto and the stirring was continued for 1 hour at -78 β C. To the cold mixture was added saturated sodium hydrogen carbonate solution (20 ml) and the mixture was extracted three times with ether. The organic layer was dried over magnesium sulfate. Evaporation of the solvent followed by column chromatography (hexane/ethyl acetate = 2/1) gave Object Compound (777 ag) as white crystals. mp : 44-45 β C MASS (m/z) : 151 (M+H) + NMR (CDC1 3 , δ) : 3.20 (6H, s), 6.56 (IH, d, J=9Hz) , 7.91 (IH, dd, J=9, 2Hz), 8.55 (IH, d, J=2Hz) , 9.76 (IH, s) Preparation 93 A mixture of 4-fluorobenzonitrile (6.05 g) , imidazole (4.09 g) , and potassium carbonate (8.33 g) in N,N- dimethylformamide (50 ml) was heated at 120 β C for 2 hours. The mixture was cooled and evaporated. Then the mixture was diluted with water (50 ml), added IN sodium hydroxide solution to make basic, and extracted three times with ethyl acetate. The organic layer was dried over magnesium sulfate. Evaporation of the solvent followed by column chromatography (silica gel, ethyl acetate) gave Object Compound (7.75 g) as white crystals. mp : 151-152°C MASS (m/z) : 170 (M+H) + NMR (CDC1 3 , δ) : 7.26 (IH, s) , 7.32 (IH, s), 7.53 (2H, d, J=8Hz), 7.80 (2H, d, J=8Hz) , 7.93 (IH, s) Preparation 94 981 - 516- Tc a stirred solution of Starting Compound 4.13 .;. in dichloromethane '125 ml) at 70°C was added αropwise diisobutyi aluminum hydride in toluene (1.5M, 41.5 mil for 1 minutes. The stirring was continued at -7CC for 1 nour. Tc this cold mixture were added water (50 mi) and saturated ammonium chloride (50 mi: . The precipitate formed was filtered off, ana the remaining solution was extracted three tiaes with dichloroaethane. The organic layer was cried eve aagnesiua sulfate. Evaporation of the solvent followed cv coluan chromatography (silica gel, chlorofcra/methanoi = 20/1) gave Object Compound (1.44 g) as white crystals, mp : 147-148°C MASS : 173 (M+H NMR (CDC1 3 , 5) : 7.27 :1H, S ), 7.37 (IH, s), 7.53 (2H, a, J=8Hz), 7.98 'IH, s), 8.03 (2K, c, J=8Hz,, 10.0 (IK, s) Preparation 95 A mixture of Starting Compound [ 1 . 12 q ) , lodomethane (5.47 g), and potassium carbonate (6.34 g) in N,N- dimethylformamide (30 ml) was heated at 60°C for 3 hours. The mixture was evaporated, then diluted with water, and extracted three times with ethyl acetate. The organic layer was dried over magnesium sulfate. Evaporation of the solvent followed by column chromatography (silica gel, hexane/ethyl acetate = 3/2) gave Object Compound (8.14 g) as a yellow oil. MASS (m/z) : 267 (M+H NMR (CDCI3, δ) : 1.42 (2/5 x 3H, t, J=7Hz), 1.44 (3/5 x 3H, t, J=7Hz), 1.82 (3/5 x 3H, s), 2.25 '2/5 x 3H, s), 3.22 (3/5 x 3H, si, 3.46 (2/5 x 3H, s) , 4.42 (2/5 x 2H, q, J=7Hz) , 4.44 (3/5 x 2H, q, J=7Hz), 7.40 (2/5 x IH, d, J=8Hz) , 7.46 (3/5 x IH, d, J=8Hz), 8.30 (2/5 x IH, dd, J=6, 2Hz), S.34 (3/5 x IH, dd, J=8, 2Hzi, 6.58 (2/5 x IH, d, J=2Hz), 8.62 (3/5 x IH, a, J=2Hz! Preparation 96 A mixture of Starting Compound (S.C9 c and powdered iron v 17.0 g) in acetic acid-ethanol (1:1, 163 ml) was slowly heated until the reaction was initiated (about 7CC . The inner temperature rose tc 89°C. After the reaction subsided, the mixture was refluxed for 1 nour ana I.owed tc cool tc room temperature. The miκture was carefully poured into the suspension cf sodium carbonate (145 g) in water (600 ml) . The precipitate foraed was filtered, then the filtrate was aade basic by adding IN sodiua hydroxide, extracted three tiaes with ethyl acetate, washed once with bri e, and dried over aagnesium sulfate. Evaporation of the solvent gave crude product (5.74 g) as crystals. This was recrystallized from toluene (18 ml) - hexane (36 ml) tc give Object Compound (5.55 g) of colorless crystals, mp : 13C-I31 β C MASS (m/z) : 219 (M+H) ~ NMR (CDC1 3 , δ) : 1.41 (3H, t, J=7Hz), 2.60 (3H, s), 3.73 (3H, s), 4.29 (2H, q, J=7Kz) , 7.26 (IH, d, J=9Hz), 7.98 (IH, d, J=9Hz) , 8.39 ,IH, s) Preparation 9 ~ To an ice-cooled suspension cf lithium aluminum nydride (950 mg) in tetrahydrofuran (50 ml) was added Starting Compound (5.45 g) , and the mixture was stirred at rooa temperature for 1 hour. The mixture was cooled with ice and diluted with ether (100 al) . Then, -water '0.95 ml), 15 sodium hydroxide (0.95 al) , and water (1.9 ml) were added dropwise to the mixture and filtered. To the precipitate was added ethanol, and the insoluble matter was filtered off. The combined filtrate was evaporated to give Object Compound (4.29 g) as white crystals, mp : 162-164°C MASS (m/z) : 177 (M+HA NMR (CDCI3, δ) : 2.57 (3H, s), 3.69 (3H, s), 4.75 (2H, s) , 7.25 (2H, A3q, Λ=0.05, J=8Kzι , " .61 A-:, s Preparation 98 Tc a stirred solution cf cxalyi chloride ( 5. ÷5 g m dichloromethane ;23 ml) below -60'C was acaec α met v_ suifoxide (4.50 g) dropwise. Tc th s solution was -.deed dropwise Starting Compound ■ 4.03 ~ ] r. dimethyl, silfcxice (2C ml) - dichloromethane (73 mi; with cooling oeiow -55 'C. The stirring was continued at -6G°C fcr 1 hour, then triethylamine (16.0 ml) was added dropwise, and tne aixture was allowed to warm to rooa temperature. Water ; 0 ml was added thereto, then the mixture was extractec fo times with chloroform and dried over magnesium sulfate. Evaporation of the solvent followed by column chromatography 'silica gel, chicroform/methanol = 30/1' gave Object Ccmpomd ,3.3 " g, as off-white crystals, mp : 73-74°C MASS (m/z) : 175 (M+H) ~ NMR (CDC1 3 , δ) : 2.64 (3H, s) , 3.77 (3H, sj , .37 (i , d, J=8Hz), 7.34 (IH, a, =3Hz) , 8.1c (IH, 5, , 10.06 (IH, s) Preparation 99 The following object compounds were obtained according tc a similar manner to that of Preparation I, 6, 11, 33, 52 or 56. (1) MASS : 530 (MA) NMR (CDC1 3 , δ) : 1.4C (9H, s) , 2.29 (3H, si, 2.52 (3 x 2/3H, sj, 2.80 (3 x 1/3H, si , 2.90-3.06 ,41-:, m) , 4.02 [2 x 1/6H, a, .7=16Hz, , 4.22 (2 x 1/όK, d, J=16Hz), 4.30 (2 x 1/3K, α, J=15Hzj , 4.Ξ3 [2 x 1/3H, a, J=15Hz), 4.23-4.42 (IH, a) , 4.63-4.95 (IH, m) , 5.07-5.18 (IH, a), 6.69 ;i x I/3H, a, AάHz) , 6.80 (1 x 2/3H, d, J=8Hz;, 6.69 ;i x 2/3H, t, J=3Hz C8 7=8 Hz' ;3H, m. ' W T ;2. MASS : 526 (M+l) NMR (CDC1 3 , δ) : 1.30 (9 x 1/3H, s,, 1.31 X x 2/3H, s), 2.70-3.25 (8H, m; , 4.40-5.09 -5H, a), 5.13-5.26 (IH, a; , 6.32-7.46 'I4K, a; NMR (CDCI3, δ : 0.80 {3 x 1/5H, t, =SHz, , 0.35 (3 x 4/5H, t, J=8Hz), 1.18-1.40 (4H, a) , 1.43 (9H, s) , 1.57-1.82 (2H, a), 2.97 ' 3 x I/5H, si , 3.08 (3 x 4/5H, s), 3.58-3.68 (IK, a), 3.90-4.03 (2H, a) , 4.20-4.31 (IH, m) , 4.19 [2 x 2/5K, d, J=15Hz) , 4.21 (2 x 1/lOH, a, =16Hz) , 4.84 (2 x 2/5H, a, J=15Hz), 4.90 (2 κ 1/lOK, d, J=16Hz) , 4.86-5. CO (IH, ) , 5.52 (IH, d, J=7Hz), 7.08- 7 .20 (IK, a, , 7.57 (IH, q, J=8Kz) , 7.70 (IH, t, =3Hz; , 7.60 (1 x 4/5H, d, J=8Hz) , 7.83 (I x I/5H, a, J=6Hz; , 8.00 (1 x 4/5H, s), 8.12 (1 κ 1/5H, s) , 8.10 (IH, a, J=9Hz, , 6.78 (1 κ 4/5H, s) , 8.83 (1 κ 1/5K, s) (4) MASS : 534 (MA) NMR (CDCI3, δ) : 0.73 (3 x 1/4H, t.. J=8Hz), 0.79 (3 x 3/4H, t, J=8Hz) , 0.98-1.30 (4K, x: , 1.32-1.62 (IK, a) , 1.47 (9H, s), 1.63-1.70 (IH, a) , 2.92 (3 x 1/4H, s), 3.00 (3 x 3/4H, s) , 3.19 (1 x 1/4H, sj , 3.22 (1 x 3/4H, si , 3.23-2.42 (IK, mi , 4.52 (2 x 3/8H, d, J=15Hzi , 4.53-4.53 (IH, a ' , 4. 2 (2 x 1/8H, d, J=16Hz) , 4.67 (2 x 1/3H, a, J=16Hz / , 4.92 (2 x 3/8H, a, J=15Hz), 4.81-4.92 (IH, m) , 6.5C-6.6C (IH, a), 7.10-7.2 (2H, a, , 7.50-7.61 ;3H, a), 7.70 (IH, t, J=8Hz), 7.72-7.88 (IH, a) , 7.98 ;IH, s), 8.09 (1 x 3/4H, a, J=3Kz;, 3.11 (1 x 1/4H, a, , 6.76 (IH, si (5) MASS : 531 (MA) NMR (CDC1 3 , δ! : 1.47 (9H, s), 1.62-1.93 (IH, a, , 1.99-2.10 (IH, a), 2.09 (3H, s,, 2.47-2.53 (2H, a) , 2.58 (3 x 2/3H, s) , 2.75 (3 x 1/3H, s t l 3.00 (2H, d, J=8Hz) , 3.90 (3 x 1/3H, s), 3.91 (3 x 2/3H, s) , 4.20-4.30 (IH, a), 4.29 ( 2 x I/2H, d, J=15Hz) , 4.4 (2 x 1/2H, d, J=15Hz) , 5.C2-5.27 (2H, a), 6.61 (I 1/3H, d, J=3Hz), 6.67 (1 x 2/3K, d, J=6Hz), 7.00 (IH, d, J=8Hz), 7.07-7.30 (5H, a), 7.32 (IH, dd, J=3, 2Hz), 7.82 (1 κ 1/3H, d, J=2Hz) , 7.94 (1 x 2/3H, a, J=2Hz) (6) MASS : 517 (M+l) NMR (CDCI3, δ) : 0.80 (3 κ 1/4H, t, J=8Hz) , 0.34 (3 x 3/4H, t, J=8Hz), 1.18-1.40 (4H, a) , 1.43 (9H, s) , 1.53-1.70 (IK, a), 1.70-1.82 (IH, a), 1.86-1.99 (IH, a) , 2.00-2.12 (IH, a) , 2.08 (3H, s) , 2.50-2.60 (2H, a), 2.93 (3 κ 1/4H, s) , 3.09 (3 κ 3/4H, s) , 4.22-4.38 (IH, a), 4.63 (2 x 3/8H, d, J=15Hz) , 4.87 (2 x 3/8H, d, J=15Kz) , 4.92 (2 x 1/4H, s) , 4.90- 5.03 (IH, a), 5.14-5.28 (IH, a), 6.90-7.03 (IH, a), 7.56 (IH, q, J=8Hz) , 7.70 (IH, q, =8Hz) , 7.80 (IH, q, J=8Hz), 8.00 (IH, s), 8.10 (1 x 3/4H, a, J=8Hz), 8.11 (1 x 1/4H, d, J=8Hz) , 8.78-8.82 (IH, a) (7) MASS : 523 (M+l) NMR (CDCI3, δ) : 0.78 (3 x 1/4H, t, J=8Hz) , 0.33 (3 X 3/4H, t, J=8Kz), 1.1C-1.38 (4K, a), 1.40 (9H, s) , 1.51-1.80 (2H, a) , 2.92-3.20 (3H, a, , 2.98 (3 x 1/4H, s) , 3.05 (3 x 3/4H, s) , 4.37-4.49 (IH, a) , 4.68-4.92 (3H, a) , 6.78-6.88 (IH, a) , 7.21- " .30 (IH, a) , 7.49 (1 x 3/4H, s), 7.52 (1 x 1/4H, s) , 7.52-7.61 (IH, a), 1X1 (IH, t, J=8Hz) , 7.79 (I κ 3/4H, d, J=8Hz) , 7.34 (1 x 1/4H, d, J=8Hz) , 3.00 (IH, s) , 8.09 (1 x 3/4H, d, J=8Hz) , 8.11 (1 κ 1/4H, a, J=8Hz, , o.7? (1 /4H, ≤) , 8.81 (1 x 1, .:H, ≤ (3 MASS : 611 (MA NMR (CDCI 3 , δ) : 1.39 '3H, t, J=6Kz , 1.43 (9H, ≤ , 2.29 '3H, si , 2.32-2.4 , 4K/ 2 , . f 2.50 3 x 3/4H, s) , 2.71 (3 x 1/4H, s>, 2.49-2.62 (IH, a), 2.93- 3.29 (3H, a), 3.40-3.52 V 2H, a) , 3.53-3.64 (2H, a), 3.92 (2 x 1/6H, a, J=lcHzi, 4.18 .2 x 3/8H, d. J=15Hz / / 4.26 [2 x 1/3H, d, AlcHtl , 4.ΞC v 2 x 3/8H, d, 4.45-4.53 (IH, a;, 5.00-5.22 (IH, a , 6.01 ..IH, α, A5Kz, , 6.53 (I x 1/4H, a, =8Hz), 6.62 (1 x 3/4H, a, J=8Hz) , 6.92 (1 x 1/4K, d, J=8Hz), 7.20 (1 x 3/4H, d, J=6Hz), 7.11-7.30 -:5H, a), 7.40 (I x 1/4H, d, J=8Hz), 7.43 (1 x 3/4H, a, J=8Hz;, 7. ~S (1 x 1/4H, s), 1 x 3/4K, (9) MASS : 567 (M+l NMR (CDCI3, δ) : 48 (9H, sj , 2.3 ( x 3/4H, s: , 2.32 (3 x 1/4H, s), 2.43-2.62 ( lH, a;, 2.53 (3 x 3/4H, s), 2.80 (3 x I/4H, s), 2.83-3.09 (2H, a) , 3.10-3.23 (IH, a), 3.36-3.49 (2K, a), 3.52-3.62 (2H, a), 3.63-3.76 (4H, a; , 4.12 (2 x 1/8H, a, J=16Hzi , 4.30 (2 x 3/8H, a, J=15Hz) , 4.56 (2 x 1/8K, d, J=16Hz l , 4.62 (2 x 3/6H, a, A15Hz , 4.43- 4.62 (IH, aj , 5.02-5.13 ,1H, a), c.CC (IH, a, J=8Hz), 6.63 (1 v 3/4H, a), c. 8- 03 1 x H, a) , 6.98-7.13 (5H, m- , ' '.18-1.32 3H, m v , 7.39 X 1/4H, d, J=8Kz), 7.43 '1 x 3/4H, a, 0 ~ =6Hz, (lOj MASS : 505 (M+li NM? (CDC1 3 , δ) : 0.83 (3 x 1/3H, t, =8Hz. , 0.92 (2 x 2/3H, t, J=8Kz), 1.22-1.50 (2H, a. , 1.43 (9H, s,, 1.53-1.78 (IH, a) , 2.48-2.61 (IH, a), 2.90 v 3 x 1/3H, S), 2.96 [3 x 2/3H, ≤J, 3.11-3.23 (IH, a) . 3.38-3.50 (2H, a, , 3.53-3. A ,2H, a , -..62--A0 (4H, a: , 4. C (2 x 1/3K, a, 0 " =15Hz, , 4.47-4.59 '2H, a) , 4.60 '2 x 1/3H, 5, , -.72 2 x 1 3H, a, J=15Hz , 4.34-4.99 (IH, mi , όA7 IH, a, J=3Hz , 7.13-7.46 (6H, a; >.ll) MASS : 613 ( A' NMP (CDC1 3 , δ. : 1.41 '3K, s , 2.26 3K, s . 2.32-2.50 (4H, a) , 2.50-2.62 (IH, a , 2.51 V 3H, ≤ , 2.52 3 x 3/4H, Si , 2.71 (3 x 1/4H, 5 , 2. 3-3. J. (3H, a, , 3.38-3.52 (2H, , , 3.54-3.65 (2H, a) , 2.99 ,2 x 1/8H, α, =16Hz) , 4.19 (2 x 1/3H, a, J=16Hz , 4.2C (2 x 3/8H, d, J=15Hz) , 4.51 (2 x 3/6H, a, J=15HzJ , 4.47-4.60 (IH, a, , 5.01-5.2- (IH, m; , 5.95-0.00 (IH, a) , 6.31-7.21 -7H, r , " .39 (1 v. A4H, a, J=8Hz), 7.41 (I x 3/4K, α, J=8Hz) , 6.05 (1 x 1/4H, s; , 8.20 (1 x 3/4H, 3, (12 MASS : 570 (MA, NMR (CDC1 3 , δ) : 1.30 (3 x 1/4H, t, J=8Hz , 1.3c (3 x 3/4H, t, J=8Hz), 1.17-1.40 4H, a: , 1.46 (9H, s, , 1.57-1.66 (2H, a), 2.58 'IH, da, =15, 4Hz) , 2.99 (3 x 1/4H, s), 3.04 (3 x 3/4H, s;, 3.18 (IH, d, J=16Hz), 3.38-3.50 (2H, a; , 2.52-3.61 (2H, a , 3.62-3.78 (4H, a), 4.50-4.69 (IH, a), 4.61 \2 x I/2H, a, J=16Hz) , 4.8C-5.03 (IH, a), 4.96 '2 x 1/2H, d, J=16Hz), 6.09 X?., a, J=8Hz, , A 32-A 50 (IH, a) , 7.58 (IK, ς, J=5Hz , ".7 , IH, t, J=8Hz , 7.78-7.84 (IK, a, , 6.00 IH, ≤ , £.08-6.16 'IH, m■ , 6.60 IH, a, J=2Hz (13) MASS : 625 (M+l* NMR (CDC1 3 , δ) : 0.91 (3 κ 1/5H, t, J=6Hz), 0.92 (3 κ 4/5H, t, J=6Hz), 1.43 (9H, s; , 1.63-1.80 (2H, a) , 2.30 (3K, s), 2.32-2.50 '4H, m , 2.50-2.63 (IH, a) , m; If _ = a '- . — — .-., ^ , J=8Hz,, -.40 (1 x 1AH, a. 8H= , c. 5 ,1 x 5K, a, J=8Hz , 5.93-7. A 'IH, a , --.p_τ.3' 6 , __-., , 7.33-7.47 (IH, a) (14) MASS : 584 (M+l) NMR (CDCI 3 , δ) : 1.41 (9H, s), 2.50 (3 x 2/3H, s) , 2.50-2.60 (IH, a), 2.71 (3 x 1/3H, si, 2. 2-2.03 (2H, a), 3.20 (IH, d, J=15Hz,, 3.5e-3.-A ;2H, a) , 3.52-3.60 (2H, a), 3.60-2. 3 (4H, a) , 3.90 , 3 x 1/3H, s), 3.91 (3 x 2/3H, s), 4.20 (2 x 1/2H, a, J=l5Hz), 4.49 (2 x 1/2H, a, J=15Hz( , 4.5C-4.6C (IH, a), 5.01-5.11 (1 κ 2 3H, a), 5.12-5.23 (1 κ 1/3H, a), 6.01 (IH, d, 6.64 (1 x 2/3H, a, J=8Hz), 7.10- ' .22 (4K, a) , 7.22- 7.30 (2H, a) , 7.38-7.46 ;1H, a), 7.79 ,1 x 1/3H, d, J=2Hz), 7.91 (1 x 2/3H, d, J=2Hz; Preoaration IOC The following object compounds were obtained according to a similar manner to that of Preparation 3, 4, 3, 41 cr 54. (!) MASS : 430 (M+l) NMR (CDC1 5) : 2.30 .'3H, s ' , 2.36-2.^6 ,1 x 1/3K, a), 2.50-2.60 (1 x 2/3H, a, , 2.6c ;2 x 2/3H, s,, 2.62 ;3 x 1/3H, s) , 2.63-3.13 (3H, a), 3.46 (1 x 1/3H, dd, J=12, 4Hz;, 3.57 '1 x 2'3H, ad, =12, 4Kz) , 4.30 (2 x 1/3H, a, J=15Hz) , 4.31 (2 x 1/6H, a, J=16Hz) , 4.40 (2 κ I/6H, a, J=16Kz , 4.6" ,2 κ 1/3H, d, 5.19 (IH, q, , 6.93- 7 .30 (14H, a; , 7.91 (I x 1/3H, a, J=8Hz % , 3. CO X κ 981 - 524 - 2/3K.. a, J=8Ez NMR (CDC1 3 , δ) : 2.70-2.33 2H, a), 2.99-2.25 ■ 2H, a; , 3.00 (3 κ 1/3H, s) , 5-05 ' 3 x 2/3h, s , , 3.92-4.15 (IH, a) , 4.41-3.0" -3H, m. , 3.30-5.40 CH, .-., , 7.00-7.30 (I4H, a; NMR (CDC1 3 , δ) : 0.81 (3 x 1/4H, t, =6Hz , 0.55 (3 κ 3/4H, t, J=8Hz), 1.17-1.42 (4H, a), 1.59-1.86 (2H, a), 3.00 (3 κ 1/4H, s), 2.07 ;3 x 3/4H, s' , 3.41 (1 x 1/4K, t, J=5Hz), 3.50 1 x 3/4H, t, J=5Hz , 3.60- 3.75 (IK, a) , 3.30-3.90 - % IH, a) , 4.63 (2 x 1/8H, d, J=16Hz) , 4.7C (2 x 3/9K, d, J=15Hz) , 4.31 ,2 x 1/8H, d, J=16Hz), 4.90 (2 x 3/8H, d, 15Kz. , 4.31- 5.0" (IH, a), 7.59 (IH, a, J=3Hz), 7.68-7.9: (3H, a), 8.01 (1 x 3/4H, si , 5.12 (1 x 1/4H, ≤, , 3.10 (IH, d, J=8Hz), 8.80 (1 x 3/4H, s), 8.82 '1 x 1/4H, s) (4) MASS : 434 (MAL) NMR (CDCI3, S, : 0.79 (3 x 1/3H, t, J=8Hz;, 0.57 (3 x 2/3H, t, J=8Hz), 1.10-1.35 (4H, m) , 1.50-1.80 (2H, m) , 2.98 (3 κ 1/3H, s) , 3.04 (3 κ 2/3H, si, 3.0C-3.12 (IH, m) , 3.22-3.37 (IH, m) , 3.63-3.71 (1 κ 1/3H, m) , 3.75-3.85 ; 1 x 2/3H, a), 4.61 (2 x 1/3H, a, J=15Hz,, 4.33 2 x 1/6H, a, =16Hz , 4.92 (2 x 1/3H, a, 4.9C-5.05 (IH, a) , 7.11-7.30 (2H, a, , A51-A66 (2H, a) , 7.71 (IH, t, J=6Hz), 7.8C (IH, d, J=8Hz) , 8.01 (IH, s), 8.10 (1 x 2/3H, a, J=8Hz;, 8.12 (1 x 1/3H, d, J=3Hz), 8.20 (1 κ 1/2H, d, J=8Hz) , 6.22 (1 κ 2/3H, d, J=8Hz), 8.50-3.56 (IH, a) , 8.31 (IH, d, J=2Hz) ( 51 MASS : 431 (MA ) NMR (CDC1 3 , δ) : 1.62-1.79 (IH, a), 1.97-2.11 (IH, a), 2.09 (3 κ 1/4H, s), 2.10 (3 κ 3/4H, s) , 2.48 (2 κ 1/4H, t, J=8Hz) , 2.51 (2 κ 2/4H, t, J=3Hz ; , 2.68 (3 x 3/4H, s), 2.78 (3 x 1/4K, s), 2.90-3.18 (2H, a), 3.40-3.51 (IH, a) , 3.90 (3 x 1/4H, si, 3.91 (3 x 3/4H, s), 4.11 (2 κ 1/8H, d, J=lόHz), 4.24 (2 κ 3/8H, d, J=I5Hz), 4.33 (2 κ 3/8H, a, J=15Hz), 4.57 (2 κ 1/8H, d, J=16Hz) , 5.08-5.18 (1 x 3/4H, a), 5.20-5.30 (1 x 1/4H, a), 6.62 (1 x 1/4H, d, J=6Hz) , 6.63 (1 κ 3/4H, d, J=8Hz) , 7.10-7.37 (6H, a) , 7.88 (1 κ 1/4H, d, J=2Hz), 7.90 (IH, a, J=8Hz), 7.94 (1 x 3/4H, d, J=2Hz) (6) MASS : 417 (M+l) NMR (CDCI3, δ) : 0.80 (3 x 1/4H, t, 0.84 (3 x 3/4H, t, J=8Hz), 1.17-1.47 (4H, a), 1.50-1.90 (3H, a), 2.08-2.22 (IH, a), 2.09 (3 κ 1/4H, s), 2.10 (3 κ 3/4H, s), 2.60 (2 κ 1/4H, t, J=8Hz) , 2.62 (2 κ 3/4H, t, J=8Hz), 3.00 (3 κ 1/4H, si, 3.07 (3 κ 3/4H, s), 3.40-3.48 (1 κ 1/4H, a), 3.50-3.58 (1 κ 3/4H, a), 4.62 (2 κ 1/2H, d, J=15Hz), 4.92 (2 κ 1/2H, d, J=15Hz), 4.80-5.06 (IH, a), 7.53 (1 κ 3/4H, t, J=8Hz), 7.57 (1 κ 1/4H, t, J=8Hz), 7.70 (IH, t, J=8Hz), 7.79 (IH, d, J=7Hz) , 7.90 (IH, d, J=8Hz), 8.01 (IH, s), 8.09 (1 κ 3/4H, d, =7Hz) , 8.11 (1 κ 1/4H, d, J=7Kz) , 8.81 (IH, a, J=2Hz) (7) MASS : 423 (M+l) NMR (CDCI3, δ) : 0.79 (3 κ 1/4H, t, J=8Hz) , 0.8" (3 κ 3/4H, t, J=8Hz), 1.00-1.40 (4H, a) , 2.53-2.50 (2H, a), 2.90-3.06 (2H, a), 2.98 (3 κ 1/4H, s), 2.04 (3 κ 3/4H, s), 3.49-3.58 (1 κ 1/4H, a) , 3.60-3.70 (I x 3/4H, a), 4.78 (2 x 3/4H, s), 4.81-4.93 (2 κ 1/4H, s), 4.81-5.02 (IH, a), 6.86 (IH, s) , 7.50-7.60 (2H, a) , 7. A n, t, A8Hz; , "A? _.-., a, J=8Hz , A 90 (1 x 3/4H, a, J=8Hz , " .93 . x . '4H, a. J=8H=1 , 5.30 ,1 x 3/4K, s 5.02 1 x A H, s , 5.09 (1 x 3/4 ' ή, a, J=8Hz, , 3.1- ■ _ κ 1/4H, a, =5Hz, , 5 9 ,1 x 3/4H, ≤, , 6.61 1 x 1/4H, s (3) MASS : 511 ( M+l) NMR (CDC1 3 , δ) : 1.38 (5H, t, J=8Hz , 2.29 Xr., ε> , 2.32-2.52 (5H, a 1 , 2.61 '3 x 3/4K, ≤, , 2 , ~~ (3 x :/4H, &/ , 2.70-2.35 IH, a, , 2.90-3.15 (2H, a , 2.3 7 -3.48 !2K, a , j.51-2. .3H, a' , 4.11 (2 x 1/8K, d, JAόHzj , 4.20 (2 x 3/8H, a, J=15Hz, , 4.32 (2 x 1/8H, a, J=16Hz) , 4.53 (2 x 3/6H, a, J=15Hz) , 4.29 (2H, a, J=3Hz) , 5.11 (1 x 3/4H, q, J=8Hz) , 5.20 (1 x 1/4H, q, J=8Hz), 6.59 1 x 1/4H, a, J=3Hz) , 6.62 (1 x 3/4H, a, J=3Hz, , ~ .0" (1 x 1/4H, d, J=8Hz), 7.15 (1 x 3/4H, a, J=6Hz, , 7.10-7.32 (5H, a), 7.81 (1 x 1/4H, s,, 7.91 ,1 x 3/4H, s) , 8.12 ,1 x 1/4H, a, J=8Hz, , £-16 1 x 3/4H, a, J=8Hz) (9) MASS : 46" (M+l) NMR (CDCI3, δ) : 2.28 <3H, s,, 2.33-2.56 'IH, a, , 2.68 (3 κ 2/3H, s), 2.80 (IH, da, J=l " , 2Hz) , 2.53 (3 κ 1/3H, s), 2.90-2.10 (2H, rc.X 3.33-3.48 (2H, a) , 3.50-5.78 (7H, a, , 4.32 '2 x 1 /3H, a, =15Hz) , 4.38 X x 1/3H, si , 4.69 (2 x l/A, a, =15Kz), 5.08-5.20 (IH, a;, 6. 3-".13 (6H, a; , ~.20-7.32 (3H, a), 8.03 .1 x I/3K, d, J=3Hz, , 3.11 (1 x 2/3H, d, J=8Hz) !10' MASS : 405 (M-i, NMR (CDCI3, δ) : 0.87 3 x 1/3H, t.. J=6HzJ , 0.93 (3 x 2/3H, t, J=8Hz,, 1.22-1.50 (2H, a, , 1.56-1.60 (2H, a), 2.58-2.72 (IH, a , 2.50-2.91 ,1H, a,, 2.92 (3 x 1/3H, s), 3.01 (3 x 2/3H, s , 3.40-3.51 (2H, a) , 3.52-3.71 (6H, a), 3.72-3.30 , '1H, mi , 4.46 (2 x 1/3H, a, J=15Hz) , 4.67 (2 κ 1/3H, s) , 7 (2 κ 1/3K, a, J=15Hz), <_ .88-5. CJ . IH, a, , -7.42 (5H, a), 8.03 (1 κ 1/3K, a, J=8Hz) , 6.12 ,1 x 2/3H, d, J=8Hz) (11) MASS : 513 (M-ri; NMR (CDC1 3 , δ) : 2.32 (3H, sj, 2.38-2.52 : £H, aj , 2.52 (3 κ 1/3H, s), 2.53 (3 x 2/3H, s l , 2.64 (3 x 2/3H, s), 2.79 (3 κ 1/3H, s > , 2. "3-2.35 'IH, a) , 2.93- 3.20 (IH, a) , 3.42-3.51 (2H, m, , 3.53-3.75 :3H, m) , 4.18 (2 κ I/6H, a, J=16FA, 4.28 2 x 1/3H, d, J=15K∑), 4.31 (2 x 1/6H, d, J=16Hz), 4.55 '2 x 1/3H, a, J=15Hz), 5.07-5.21 (IH, a; , 6.97-7.32 (7H, m) , 8.12 (IK, s) , 8.16 (1 x 1/3H, s), 5.22 ;1 κ 2/3H, s) (12) MASS : 470 (M+l) NMR (CDC1 3 , δj : 0.30 (3 κ 1/5H, t, J=8Hz), 0.85 (3 κ 4/5H, t, J=3Hz), 1.15-1.40 (4H, a , l.cO-1.90 (2H, a), 2.63 (1 κ 1/5H, a, J=SKz), 2.70 (1 x 4/5H, d, J=8Hz), 2.80 (IH, t, J=15Hz), 2.99 (3 κ 1/5H, s) , 3.03 (3 κ 4/5H, s) , 3.40-3.50 (2K, a) , 3.50-3.70 (6H, a), 3.70-3.80 (IH, a), 4.63 (2 x. 1/2H, a, J=15Hz), 4.80-5.02 (IH, a) , 4.90 (2 κ 1/2H, d, J=15Hz), 7.50-7.60 (IH, m) , 7.71 (IK, t, J=3Hz), 7.80 (IH, a, J=8Hz), 8.01 (in, si , 5.10 (2 x 4/5H, d, , 8.80 (IH, d, J=8Hz) (13) MASS : 525 (MA) NMR (CDCI 3 , δ) : 0.90 (3 x 1/5H, t, J=6Hz,, 0.92 (3 κ 4/5H, t, J=8Hz), 1.67-1.90 [ 2ή ' , τc>, , 2.29 (3H, s) , 2.33-2.48 (4H, a ; , 2.49-2.60 (IK, a; , 2.61 (3 κ 4/5H, s), 2.76 (3 κ 1/5H, s), 2.72-2.88 (IH, a) , 2.92-3.09 (2H, a), 3.40-3.50 (2K, a), 3.51-3.72 (3H, a), 3.79 (2 κ I/IOH, a, J=16Hz), 3.85 (2H, t, J=8Hz), 3.99 (2 κ 2/5H, d, J=15Hz), 4.06 '2 x I/IOH, d, J=16Hz), 4.39 (2 x 2/5H, a, J=15Hz) , 5.01-5.20 (IH, m) , 6.41 (1 x 1/5H, d, J=8Hz) , 6.49 (1 κ 4/5H, d, J=8Hz), 6.81 (1 κ 1/5H, d, J=8Hz; , 7.03 (1 κ 4/5H, d, J=8Hz), 7.10-7.32 (6H, ) , 3.15 (IH, d, J=8Hz) (14) MASS : 484 (M+l) NMR (CDC1 3 , δ) : 2.40-2.58 (IH, m) , 2.63 (3 κ 3/4H, s), 2.70-2.82 (IH, a), 2.78 (3 κ 1/4H, s), 2.93- 3.18 (2H, m) , 3.38-3.50 (2H, m) , 3.51-3.74 (7H, a), 3.90 (3 κ 1/4H, s), 3.91 (3 κ 3/4H, s) , 4.10 (2 κ 1/8H, d, J=16Hz), 4.23 (2 κ 3/8H, a, J=15Hz) , 4.31 (2 κ 1/8H, d, J=16Hz) , 4.56 (2 κ 3/8H, d, J=15Hz), 5.04-5.27 (IH, m) , 6.61 (1 κ 1/4H, d, J=8Hz) , 6.68 (1 κ 3/4H, d, J=8Hz) , 7.03-7.36 (6H, m) , 7.34 (1 κ 1/4H, s), 7.93 (1 x 3/4H, s) , 8.11 (1 x 1/4H, d, J=8Hz), 8.13 (1 x 3/4H, d, J=8Hz) Preparation 101 The following object compounds were obtained according to a similar manner to that of Preparation 1, 6, 11, 38, 52 or 56. (1) MASS : 414 (M+l) NMR (CDCI3, δ) : 1.35 (3H, t, J=8Hz), 1.39 (9H, s) , 2.58 (3 κ 3/4H, s), 2.77 (3 κ 1/4H, s), 2.90-3.10 (2H, a), 3.90 (2 κ 1/8H, d, J=16Hz), 4.26 (2 κ 1/8H, d, J=16Hz), 4.31 (2H q, J=8Hz) , 4.33 (2 κ 3/8H, d, J=15Hz), 4.43 (2 κ 3/8H, d, J=15HzJ , 4.73- 4.88 (1 κ 2/3H, a) 4.90-5.00 (1 x 1/3H, m) , 5.30- 5.43 (IH, a), 6.59 (1 x 1/4H, d, J=8Hz) , 6.63 (1 κ 3/4H, d, J=8Kz), 7 .02-7.36 '6H, a) , A 81 'I x 1/4H, s) , 7.92 (1 x 3/4H, s, (2) MASS : 383 (M+li NMR (CDC1 3 , δ) : 1.40 (9 x 1/3H, s,, 1.42 (9 x 2/3H, s), 2.28 (3 κ 2/3H, si , 2.30 (3 x 1/3H, si , 2.61 (3 x 2/3H, s), 2.81 (3 κ 1/3H, s), 2.87-3.00 (2H, m) , 4.14 (2 x 1/6H, d, J=16Hz), 4.37 (2 x 1/6H, a, J=16Hz), 4.42 (2 x 1/3H, d, J=15Kz) , 4.56 (2 κ 1/3H, d, J=15Hz), 4.79-4.92 (IH, ) , 5.32 (1 x 1/3H, d, J=8Hz), 5.40 (1 x 2/3H, d, =SHz), 6.91- 7.18 (6H, m) , 7.20-7.31 (3H, a; (3) MASS : 321 (M+l) NMR (CDC1 3 , δ) : 0.83 (3 κ 1/3H, t, J=8Hz), 0.90 (3 κ 2/3H, t, J=3Hz), 1.20-1.78 ( 4≡, m) , 1.41 (9 κ 1/3H, s), 1.43 (9 x 2/3H, S), 2.90 (3 x 1/3H, s), 2.94 (3 x 2/3H, s), 4.51 (2 κ 1/2H, d, J=15Hz) , 4.68 (2 κ 1/2H, d, J=15Hz), 4.59-4.73 (IH, a) , 5.31 (1 x 1/3H, d, J=8Hz), 5.39 (I x 2/3H, d, J=8Hz) , 7.12- 7.40 (5H, m) (4) MASS : 416 (M+l) NMR (CDCI3, δ) : 1.40 (9H, s) , 2.51 (3 x 1/5H, s), 2.53 (3 x 4/5H, s) , 2.58 (3 x 1/5H, s), 2.75 (3 x 4/5H, s), 2.90-3.07 (2H, a), 3.97 (2 κ I/IOH, d, J=16Hz), 4.29 (2 x 1/lOK, d, J=16Hz), 4.32 [ 2 x 2/5K, d, J=15Hz) , 4.42 (2 x 2/5K, d, , 4.77- 4.97 (IH, m) , 5.29-5.40 (IH, m) , 6.93-7.30 (7H, a, , 8.10 (1 κ I/5H, s) , 8.21 (1 x 4/5H, s) (5) MASS : 386 (M+l) NMR (CDCl-a, δ) : 0.80 (3 x 1/4H, t, , 0.66 (3 κ 3/4H, t, J=8Kz), 1.18-1.38 (3H, a) , 1.39 (9 κ 1/4H, s) , 1.41 (9 κ 3/4H, s), 1.51-1.63 (IH, a) , 1.64- 1.73 (2H, ) , 2.99 (3 x 1/4K, s), 3.08 (3 κ 3/4H, s), 4.60-4.69 (IH, m) , 4.70 (2 κ 3/8H, d, J=15Hz), 4.78 (2 κ 1/8H, d, J=17Hz), 4.87 (2 x 3/8H, d, J=15Hz), 4.89 (2 x 1/8H, d, J=17Kz) , 5.29 (1 κ 1/4H, d, J=8Hz), 5.33 (1 κ 3/4H, d, J=8Hz) , 7.53 (IH, t, J=8HZ), 7.70 (IH, t, J=8Hz) , 7.79 (IH, d, J=8Hz), 8.00 (IH, s), 8.09 (IH, d, J=8Hz) , 8.81 (IH, d, J=2Hz) (6) MASS : 428 (M+l) NMR (CDCI T , δ) : 0.90 (3 x 1/5K, t, J=8Hz) , 0.93 (3 x 4/5H, t, J=8Hz), 1.39 (9H, s), 1.65-1.82 (2H, m) , 2.60 (3 κ 4/5H, s) , 2.75 (3 κ 1/5K, s), 2.90-3?03 (2H, m) , 3.51 (2 κ 1/lOH, d, J=16Hz) , 3.77-3.90 (2H, m) , 4.10 (2 κ 1/10H, d, J=16Hz) , 4.11 (2 κ 2/5H, d, J=15Hz), 4.22 (2 κ 2/5H, d, J=15Hz), 4.73- 5.92 (IH, m) , 5.32 (IH, d, J=8Hz) , 6.43 (1 κ 1/5H, d, J=8Hz), 6.49 (1 x 4/5H, d, J=8Hz) , 6.85 (1 x 1/5H, dd, J=12, 3Hz), 7.10 (1 κ 4/5H, dd, J=12, 3Hz) , 7.02-7.32 (6H, m) (7) MASS : 381 (M+l) NMR (CDC1 3 , δ) : 1.35 (9 κ 2/9H, s), 1.39 (9 κ 2/9H, s), 1.49 (9 κ 5/9H, s), 2.83-3.20 (2H, m) , 3.03 (3H, s), 4.33-4.71 (2H, m) , 4.73-5.00 (2H, m) , 5.21-5.38 (IH, m) , 7.08-7.45 (9H, m) Prppararinn 102 The following object compounds were obtained according to a similar manner to that of Preparation 3, 4, 8, 41 or 54. (1) MASS : 314 (M+l) NMR (CDC1 3 , δ) : 1.39 (3K, t, J=8Hz) , 2.62 (3 κ 3/4H, s), 2.88 (3 κ 1/4H, s), 2.72-2.88 (IH, m) , 2.88- 3.08 (IH, m) , 3.88-4.00 (IH, m) , 4.03 (2 x 1/8H, d, J=16Hzi , 4.30 (2 x i/8H, ' d, J=16Hz , 4.32 (2 x 3/8H, d, J=15Hz» , 4.32 V 2H, q, J=3Hz / , 4.53 (2 x 3/8H, d, J=I5Hz) , 6.63 ■ 1 x 1/4H, a, J=8Hzj , 6.67 (1 x 3/4H, d, J=8Hz, , 7.10- 7 .32 5H, a, , " .41 (IH, dd, J=6, 2Hz) , 7.88 (1 κ 1/4H, s) , 7.97 (1 x 3/4H, s) (2) MASS : 283 (M+l) NMR (CDC1 3 , δ) : 2.28 (3H, si, 2.63-2.50 (IH, a, , 2.71 (3 x 2/3H, s), 2.90 (3 x 1/3H, s) , 2.33-3. CO (IH, a), 3.86 (1 x 1/3H, t, J=8Hz), 3.9" (I κ 2/3H, t, J=8H∑), 4.20 (2 κ 1/6H, a, J=16Hzi , 4.40 >2 x 1/6H, d, J=16Hz), 4.45 (2 x 1/3H, d, J=15Hz), 4.63 (2 κ 1/3H, d, J=15Hz), 6.97-7.18 (6H, a) , 7.20-7.38 (3H, a) (3) MASS : 221 (M+l) NMR (CDC1 3 , δ) : 0.82-1.00 (3H, m) , 1.3C-I.7C (4H, a) , 2.91 (3 κ 2/3H, s; , 2.94 (3 κ I/3H, s) , 3.63-3.82 (IH, a) , 4.46 (2 κ I/6H, a, J=16Hz; , 4.50 (2 κ 1/3H, d, J=15Hz) , 4.68 (2 κ I/6H, a, J=16Hz) , 4.71 (2 κ 1/3K, d, J=15Hz) , 7.13-7.41 (5H, a) (4) MASS : 316 (M+l) NMR (CDCI3, δ) : 2.55 (3H, sj , 2.59 (3 x 3/4H, si , 2.73-2.89 (IH, a) , 2.38 (3 x 1/4H, s) , 2.90-3.08 (IH, a) , 3.87-4.00 (IH, a) , 4.09 (2 κ 1/8H, a, J=16Hz) , 4.31 (2 x 1/8K, d, J=16Hz) , 4.3 " (2 x 3/8H, d, J=15Hz) , 4.57 (2 x 3/8H, a, J=15Kz) , 7.02- 7.35 (7H, m) , 8.18 (1 κ 1/4H, s) , 6.27 (1 x 3/4H, s) (5) MASS : 286 (M+l) NMR (CDCI3, δ) : 0.90 (3H, t, J=8Hz) , 1.20-1.58 (6H, m) , 3.00 (3H, s) , 3.72 (IH, a, J=8Kz) , 4.68 (2 x 3/8H, d, J=15Hz) , 4.71 (2 x 1/8H, a, J=16H= , 4.63 (2 κ 1/8H, d, J=16Hz) , 4.91 (2 κ 3/8H, a, =15Hz) , 7.53 (IH, t, J=8Hz) , 7.7C (IH, t, J=8Hz), ".30 (IH, d, J=8Hz), 7.92 (1 κ 1/4H, s) , 8.01 (1 x 3/4K, s) , 8.09 (IH, d, J=8Hz) , 3.80 (IH, si (6) MASS : 328 (M+l) NMR (CDC1 3 , δ) : 0.98 (3K, t, J=3Hz) , 1.70-1.84 (2K, m) , 2.63 (3 x 3/4H, s) , 2.61 (3 κ 1/4H, s) , 2.74- 2.89 (IH, m) , 2.90-3.00 (IH, m) , 3.83 (2H, t, J=8Hz), 3.92 (IH, t, J=8Hzi , 4.10 (2 κ 1/2K, a, J=15Hz), 4.38 (2 κ I/2H, d, J=8Hz( , 6.51 (IH, a, J=8Hz) , 7.10-7.21 (4H, m) , 7.21-7.33 (3H, a, (7) MASS : 281 (M+l) NMR (CDCI3, δ) : 2.70-2.91 (IH, a), 2.92-3.17 (IH, m) , 2.99 (3 κ 1/2H, s), 3.00 (3 κ 1/2H, s) , 3.85-4.18 (3H, a) , 4.60 (2 κ 1/3H, d, J=17Hz) , 4.66 (2 κ 1/3H, s), 4.78 (2 x 1/3H, d, J=17Hz; , 6.98- 7 .40 (9H, a) Preparation 103 The following object coapounds were obtained according to a similar manner to that of Preparation 22, 23, 23, 67 or 68. (1) MASS : 167 (M+l) NMR (CDCI3, δ) : 1.32 (3H, t, J=8Hz) , 2.42 (3H, sj , 3.62 (2H, S) , 4.31 (2H, q, J=8Hz) , 6.69 (IH, a, J=8Hz) , 7.57 (IH, dd, J=8, 2Hz) , 8.C3 (IH, a, J=2Hz) (2) MASS : 169 (M+l) NMR (CDCI3, δ) : 2.43 (3H, s), 2.57 (3H, s) , 3.66 (2K, s), 7.16 (IH, d, J=8Hz), 7.49 (IH, dd, J=8, 3Hz), 8.37 (IH, s) (3) MASS : 181 (M+l) NMR (CDC1 3 , δ) : 1.43 (3H, t, J=8Hz) , 1.70-1.84 (2H, m) , 2.39 (3H, s), 3.50 (2H, s) , 3.89 (2H, t, J=8Hz), 6.52 (IH, d, J=8Hz) , 7.20 (IH, d, J=2Hz) , 7.30 (IH, dd, J=8, 2Hz) Preparation 104 The following object compounds were obtained according to a similar manner to that of Preparation 1, 6, 11, 38, 52 or 56. (1) MASS : 413 (M+l) NMR (CDCI3, δ) : 0.85 (3 x 1/6H, t, J=8Hz) , 0.90 (3 x 5/6H, t, J=8Hz), 1.20-1.40 (4H, m) , 1.41 (9 x 1/6H, s), 1.42 (9 x 5/6H, s) , 1.50-1.78 (2H, m) , 2.96 (3 x 1/6H, s), 3.09 (3 x 5/6H, s) , 4.58-4.81 (3H, m) , 5.29 (1 x 1/6H, d, J=8Hz) , 5.32 (1 x 5/6H, d, J=8Hz), 7.37-7.43 (IH, m) , 7.68-7.80 (2H, m) , 8.30 (IH, d, J=8Hz), 8.60 (IH, s) , 8.65 (IH, d, J=2Hz) , 9.20 (IH, s) (2) MASS (m/z) : 350 (M + +l) NMR (CDCI3, δ) : 0.89 (3H, m) , 1.33 (4H, m) , 1.54-1.67 (2H, m) , 2.55 (3H, s) , 2.89 (3H x 1/4, s) , 3.01 (3H x 3/4, s), 4.46-4.66 (3H, ) , 5.33 (IH, m) , 7.12 (IH, d, J=8Hz), 7.47 (IH, dd, J=2, 8Hz) , 8.37 (IH, d, J=2Hz) (3) MASS : 400 (M+l) NMR (CDCI3, δ) : 1.38 (9 x 1/4H, s) , 1.39 (9 x 3/4H, S), 2.61 (3 x 3/4H, s), 2.79 (3 x 1/4H, s), 2.99 (2 x 3/4H, d, J=8Hz) , 3.01 (2 x 1/4H, d, J=8Hz) , 3.80 (3 x 1.4H, s), 3.81 (3 x 3/4H, s), 3.78 (2 x 1/8H, d, J=16Hz), 4.38 (2 x 1/8H, d, J=16Hz) , 4.41 (2 x 3/8H, d, J=15Hz), 4.52 (2 x 3/8H, d, J=15Hz) , 4.82 (1 x 3/4H, q, J=8Hz) , 4.93 (1 x 1/4H, q, J=8Hz), 5.29-5.40 (IH, m) , 7.01 (1 x 1/4H, s), 7.08 (1 x 3/4H, s), 7.10-7.32 (5H, m) , 7.89 (1 x 1/4H, s), 8.01 (1 x 3/4H, s), 8.21 (1 x 1/4H, s), 8.23 (1 x 3/4H, s) (4) MASS : 400 (M+l) NMR (CDC1 3 , δ) : 1.41 (9H, s) , 2.65 (3 x 2/3H, s) , 2.71 (3 x 1/3H, s), 2.90-3.10 (2H, m) , 3.50 (2 x 1/6H, d, J=16Hz), 3.80 (3 x 1/3H, s), 3.82 (3 x 2/3H, s), 4.40 (2 x 1/6H, d, J=16Hz) , 4.42 (2 x 1/3H, d, J=15Hz), 4.58 (2 x 1/3H, d, J=15Hz) , 4.83 (1 x 2/3H, m) , 5.16 (1 x 1/3H, m) , 5.40 (1 x 2/3H, d, J=8Hz), 5.52 (1 x 1/3H, d, J=8Hz) , 6.72 (1 x 1/3H, d, J=6Hz), 6.76 (1 x 2/3H, d, J=6Hz) , 7.09- 7.32 (5H, m) , 8.06 (1 x 1/3H, s), 8.23 (1 x 2/3H, s), 8.42 (IH, d, J=6Hz) (5) MASS : 448 (M+l) NMR (CDCI3, δ) : 1.41 (9 x 1/6H, s) , 1.42 (9 x 5/6H, s), 2.61 (3 x 5/6H, s) , 2.79 (3 x 1/6H, s), 2.91- 3.10 (2H, m) , 3.91 (2 x 1/12H, d, J=16Hz) , 4.38 (2 x 1/12H, d, J=16Hz), 4.41 (2 x 5/12H, d, J=15Hz) , 4.50 (2 x 5/12H, d, J=15Hz) , 4.78-4.93 (IH, m) , 5.28-5.41 (IH, m) , 7.11-7.31 (5H, m) , 7.51 (1 x 1/6H, s), 7.69 (1 x 5/6H, s), 8.18 (1 x 1/6H, s), 8.31 (1 x 5/6H, s), 8.61 (IH, s) Preparation 105 The following object compounds were obtained according to a similar manner to that of Preparation 3, 4, 8, 41 or 54. (1) MASS : 313 (M+l) NMR (CDC1 3 , δ) : 0.90 (3H, t, J=8Hz) , 1.20-1.58 (4H, m) , 1.59-1.80 (2H, a), 3.00 (3H, s) , 3.62-3.78 (IH, m) , 4.57 (2 x 1/2H, d, J=15Hz) , 4.74 (2 x 1/2H, d, J=15Hz), 7.35-7.44 (IH, m) , 7.60-7.80 (2H, m) , 8.30 (IH, d, J=8Hz), 8.60 (IH, s) , 8.66 (IH, d, J=3Hz) , 9.19 (IH, s) (2) NMR (CDCI3, δ) : 0.92 (3H, t, J=7Hz) , 1.31-1.58 (6H, m) , 2.54 (3H, s), 2.94 (3H, s) , 3.68 (IH, m) , 4.45 (IH, d, J=15Hz), 4.67 (IH, d, J=15Hz) , 7.13 (IH, d, J=8Hz), 7.50 (IH, dd, J=2, 8Hz) , 8.37 (IH, d, J=2Hz) (3) MASS : 300 (M+l) NMR (CDCI3, δ) : 2.70 (3 x 3/4H, s), 2.73-2.87 (IH, m) , 2.90 (3 x 1/4H, s), 2.93-3.07 (IH, a) , 3.82 (3 x 1/4H, s), 3.86 (3 x 3/4H, s) , 3.88 (1 x 1/4H, s), 3.96 (1 x 3/4H, s) , 4.12 (2 x 1/6H, d, J=16Hz) , 4.40 (2 x 1/6H, d, J=15Hz) , 4.48 (2 x 1/3H, d, J=15Hz), 4.60 (2 x 1/3H, d, J=15Hz) , 6.91 (1 x 1/4H, s), 7.11 (1 x 3/4H, s) , 7.09-7.33 (5H, m) , 7.98 (1 x 1/4H, s), 8.07 (1 x 3/4H, s) , 8.23 (IH, d, J=2Hz) (4) MASS : 300 (M+l) NMR (CDCI3, δ) : 2.38-2.45 (IH, m) , 2.45-2.52 (IH, m) , 2.41 (3 x 2/3H, s) , 2.43 (3 x 1/3H, s), 3.93 (3H, s), 3.94-4.03 (IH, m) , 3.98 (2 x 1/6H, d, J=16Hz) , 4.22 (2 x 1/6H, d, J=16Hz) , 4.23 (2 x 1/3H, d, J=15Hz), 4.33 (2 x 1/3H, d, J=15Hz) , 6.38-6.41 (IH, ) , 6.66-6.70 (5H, m) , 8.07 (1 x 1/3H, s), 8.13 (1 x 2/3H, s), 8.20-8.27 (IH, m) (5) MASS : 348 (M+l) NMR (CDCI3, δ) : 2.68 (3 x 5/6H, s), 2.85 (3 x 1/6H, s), 2.78-2.90 (IH, m) , 2.92-3.08 (IH, m) , 3.83 (1 x 1/6H, t, J=8Hz), 3.97 (1 x 5/6H, t, J=8Hz) , 4.11 (2 x 1/12H, d, J=16Hz), 4.38 (2 x 1/12H, d, J=16Hz) , 4.39 (2 x 5/12H, d, J=15Hz) , 4.61 (2 x 5/12H, d, J=15Hz), 7.10-7.35 (5H, m) , 7.50 (1 x 1/6H, s) , 7.71 (1 x 5/6H, s), 8.26 (1 x 1/6H, s), 8.38 (1 x 5/6H, s), 8.60 (IH, d, J=2Hz) Preparation 106 The following object compounds were obtained according to a similar manner to that of Preparation 1, 6, 11, 38, 52 or 56. (1) MASS : 597 (M+l) NMR (CDCI3, δ) : 0.85 (3 x 1/4H, t, J=8Hz) , 0.89 (3 x 3/4H, t, J=8Hz), 1.20-1.41 (4H, m) , 1.47 (9H, s) , 1.58-1.85 (2H, m) , 2.57 (IH, dd, J=17, 4Hz) , 2.92 (3 x 1/4H, s), 3.04 (3 x 3/4H, s), 3.19 (IH, dd, J=17, 2Hz), 3.40-3.50 (2H, m) , 3.52-3.61 (2H, a), 3.62-3.85 (4H, m) , 4.50-4.60 (IH, m) , 4.57 (2 x 1/2H, d, J=15Hz), 4.71 (2 x 1/2H, d, J=15Hz) , 4.83- 5.00 (IH, m) , 6.08 (IH, d, J=8Hz) , 7.30-7.50 (2H, m) , 7.65-7.81 (2H, m) , 8.31 (IH, d, J=8Hz), 8.59 (IH, s), 8.67 (IH, d, J=2Hz) , 9.20 (IH, s) (2) MASS : 561 (M+l) NMR (CDCI3, δ) : 0.79 (3 x 1/4H, t, J=8Hz) , 0.80 (3 x 3/4H, t, J=8Hz), 0.93-1.30 (4H, m) , 1.30-1.52 (IH, m) , 1.43 (9H, s), 1.52-1.70 (IH, m) , 2.90 (3 x 1/4H, s), 3.01 (3 x 3/4H, s) , 3.19 (1 x 1/4H, d, J=5Hz), 3.21 (1 x 3/4H, d, J=5Hz) , 3.28-3.40 (IH, m) , 4.51 (2 x 1/2H, d, J=15Hz) , 4.51-4.62 (IH, m) , 4.69 (2 x 1/2H, d, J=15Hz) , 5.80-5.93 (IH, m) , 6.50-6.60 (IH, m) , 7.10-7.22 (2H, a), 7.37-7.45 (IH, m) , 7.46-7.80 (4H, m) , 8.31 (IH, d, J=7Hz), 8.51 (IH, d, J=4Hz), 8.58 (IH, s) , 8.65 (IH, d, J=2Hz), 9.19 (IH, s) (3) MASS : 544 (M+l) NMR (CDC1 3 , δ) : 0.86 (3 x 1/5H, t, J=8Hz) , 0.90 (3 x 4/5H, t, J=8Hz), 1.29 (4 x 1/5H, t, J=8Hz) , 1.31 (4 x 4/5H, t, J=8Hz), 1.42 (9H, s) , 1.55-1.70 (IH, m) , 1.70-1.85 (IH, m) , 1.87-2.18 (2H, m) , 2.09 (3H, s), 2.58 (2H, t, J=8Hz), 2.94 (3 x 1/5H, s), 3.09 (3 x 4/5H, s), 4.22-4.35 (IH, m) , 4.59 (2 x 1/2H, d, J=15Hz), 4.70 (2 x 1/2H, d, J=15Hz) , 4.88-5.02 (IH, m) , 5.12-5.23 (IH, m) , 6.83-6.98 (IH, m) , 7.41 (IH, dd, J=8, 6Hz), 7.67-7.81 (2H, m) , 8.30 (IH, d, J=8Hz), 8.59 (IH, s) , 8.66 (IH, d, J=2Hz) , 9.19 (IH, s) (4) MASS (m/z) : 534 (M + +l) NMR (CDCI3, δ) : 0.87 (3H, t, J=7Hz) , 1.31 (4H, m) , 1.47 (9H, s), 1.60-1.75 (2H, m) , 2.54 (3H, s) , 2.87 (3H x 1/4, s), 2.98 (3H x 3/4, s) , 3.17 (IH, m) , 3.43-3.57 (5H, m) , 3.65 (4H, m) , 4.40 (IH x 3/4, d, J=15Hz), 4.53 (IH, m) , 4.68 (2H x 1/4, s) , 4.67 (IH x 3/4, d, J=15Hz), 4.87 (IH, m) , 6.06 (IH, d, J=7Hz), 7.11-7.17 (IH, m) , 7.32-7.47 (2H, m) , 8.35 (IH, m) (5) MASS (m/z) : 498 (M + +l) NMR (CDCI3, δ) : 0.80 (3H, t, J=7Hz) , 1.03 (2H, m) , 1.17 (2H, m) , 1.40 (IH, m) , 1.46 (9H, s) , 1.57 (IH, m) , 2.53 (3H x 3/4, s), 2.54 (3H x 1/4, s), 2.85 (3H x 1/4, s), 2.95 (3H x 3/4, s) , 3.18 (IH, dd, J=5, 14Hz) , 3.35 (IH, m) , 4.37 (IH x 3/4, d, J=15Hz), 4.54 (2H x 1/4, s) , 4.57 (IH, m) , 4.63 (IH x 3/4, d, J=15Hz), 4.82 (IH, m) , 6.56 (IH, d. J=7Hz), 7.08-7.20 (3H, m) , 7.43 (IH, dd, J=2, 8Hz) , 7.53 (IH, m) , 7.58 (IH, m) , 8.33 (IH, d, J=2Hz) , 8.49 (IH, d, J=5Hz) (6) MASS : 481 (M + +l) NMR (CDC1 3 , δ) : 0.87 (3H, t, J=7Hz) , 1.31 (4H, m) , 1.44 (9H, s), 1.61 (IH, m) , 1.72 (IH, m) , 1.94 (IH, m) , 2.05 (IH, m) , 2.11 (3H, s) , 2.54 (3H, s) , 2.56 (2H, m) , 2.89 (3H x 1/4, s) , 3.00 (3H x 3/4, s) , 4.28 (IH, m) , 4.44 (IH x 3/4, d, J=15Hz) , 4.54 (IH x 1/4, d, J=16Hz), 4.63 (IH x 1/4, d, J=16Hz) , 4.65 (IH x 3/4, d, J=15Hz), 4.89 (IH, m) , 5.22 (IH, m) , 6.94 (IH, d, J=7Hz), 7.13 (IH x 3/4, d, J=8Hz) , 7.17 (IH x 1/4, d, J=8Hz), 7.46 (IH, dd, J=2, 8Hz) , 8.35 (IH, d, J=2Hz) (7) MASS (m/z) : 437 (M + +l) NMR (CDCI3, δ) : 0.87 (3H, t, J=7Hz) , 1.33 (4H, m) , 1.44 (9H, s), 1.67 (2H, m) , 2.54 (3H x 3/4, s) , 2.55 (3H x 1/4, s) , 2.88 (3H x 1/4, s) , 3.02 (3H x 3/4, s), 3.63 (IH, m) , 3.96 (IH, m) , 4.23 (2H, m) , 4.47 (IH x 1/4, d, J=16Hz), 4.51 (IH x 3/4, d, J=15Hz), 4.61 (IH x 3/4, d, J=15Hz) , 4.70 (IH x 1/4, d, J=16Hz), 4.85 (IH, m) , 5.56 (IH, d, J=7Hz) , 7.13 (IH, d, J=8Hz), 7.21 (IH, d, J=7Hz) , 7.46 (IH x 3/4, d, J=2, 8Hz), 7.57 (IH x 1/4, d, J=2, 8Hz) , 8.34 (IH x 3/4, d, J=2Hz) , 8.48 (IH x 1/4, d, J=2Hz) (8) MASS : 597 (M+l) NMR (CDCI3, δ) : 1.47 (9H, s) , 2.29 (3H, s), 2.33-2.50 (4H, m) , 2.53 (3 x 3/4H, s) , 2.58 (IH, dd, J=16 and 2Hz), 2.78 (3 x 1/4H, s), 2.98-3.09 (2H, m) , 3.12- 3.28 (IH, ) , 3.40-3.50 (2H, m) , 3.58-3.65 (2H, a), 3.79 (3 x 1/4H, s) , 3.81 (3 x 3/4H, s), 3.89 (2 x 1/8H, d, J=16Hz), 4.28 (2 x 1/8H, d, J=16Hz) , 4.38 (2 x 3/8H, d, J=15Hz), 4.50 (2 x 3/8H, d, J=15Hz) , 4.49-4.59 (IH, m) , 5.07 (1 x 3/4H, q, J=8Hz), 5.19 (1 x 1/4H, q, J=8Hz), 6.02 (IH, d, J=8Hz) , 6.88 (1 x 1/4H, s), 7.03 (1 x 3/4H, s) , 7.13-7.23 (5H, m) , 7.43 (1 x 1/4H, d, J=8Hz) , 7.47 (1 x 3/4H, d, J=8Hz), 7.82 (1 x 1/4H, s) , 7.98 (1 x 3/4H, s), 8.19 (1 x 1/4H, d, J=2Hz) , 8.21 (1 x 3/4H, d, J=2Hz) (9) NMR (CDC1 3 , δ) : 1.43 (9H, s) , 2.29 (3H, s) , 2.31-2.50 (4H, m) , 2.60 (3 x 2/3H, s) , 2.70 (3 x 1/3H, s), 2.90-3.30 (4H, m) , 3.40-3.53 (2H, m) , 3.53-3.70 (2H, m) , 3.77 (3 x 1/3H, s) , 3.81 (3 x 2/3H, s) , 4.31 (2 x 1/2H, d, J=15Hz) , 4.43-4.58 (1 x 2/3H, m) , 4.60 (2 x 1/2H, d, J=15Hz) , 5.08 (1 x 2/3H, q, J=8Hz), 5.32-5.46 (1 x 1/3H, m) , 5.77 (1 x 1/3H, q, J=8Hz), 6.02 (IH, t, J=8Hz), 6.70-6.80 (IH, m) , 7.10-7.33 (5H, m) , 7.43 (1 x 2/3H, d, J=8Hz) , 7.50 (1 x 1/3H, d, J=8Hz), 8.00 (1 x 1/3H, s) , 8.20 (1 x 2/3H, s) , 8.38-8.47 (IH, m) (10) M7ASS : 645 (M+l) NMR (CDCI3, δ) : 1.47 (9H, s) , 2.30 (3H, s) , 2.32-2.50 (4H, m) , 2.50-2.71 (IH, ) , 2.56 (3 x 4/5H, s), 2.78 (3 x 1/5H, s) , 2.96-3.13 (2H, m) , 3.14-3.29 (IH, m), 3.42-3.50 (2H, m) , 3.58-3.67 (2H, m) , 4.11 (2 x 1/lOH, d, J=15Hz) , 4.19 (2 x 2/5H, d, J=16Hz) , 4.22 (2 x 1/10H, d, J=15Hz) , 4.61 (2 x 2/5H, d, J=16Hz), 4.48-4.58 (IH, m) , 5.00-5.13 (IH, m) , 5.98-6.08 (IH, m) , 7.12-7.23 (5H, m) , 7.32 (1 x 1/5H, s), 7.62 (1 x 4/5H, s) , 7.40 (1 x 1/5H, d, J=8Hz), 7.47 (1 x 4/5H, d, J=8Hz) , 8.10 (1 x 1/5H, s), 8.27 (1 x 4/5H, s) , 8.52 (1 x 1/5H, s) , 8.58 (1 x 4/5H, s) Preparation 107 The following object compounds were obtained according to a similar manner to that of Preparation 3, 4, 8, 41 or 54. (1) MASS : 497 (M+l) NMR (CDC1 3 , δ) : 0.88 (3 x 1/4H, t, J=8Hz) , 0.89 (3 x 3/4H, t, J=8Hz), 1.20-1.42 (4H, m) , 1.58-1.82 (2H, m) , 2.60-2.90 (2H, m) , 2.93 (3 x 1/4H, s) , 3.06 (3 x 3/4H, s), 3.40-3.50 (2H, m) , 3.50-3.72 (6H, m) , 3.80-3.98 (IH, m) , 4.58 (2 x 1/8H, d, J=16Hz) , 4.59 (2 x 3/8H, d, J=15Hz), 4.69 (2 x 3/8H, d, J=15Hz) , 4.71 (2 x 1/8H, d, J=16Hz), 4.80-5.00 (IH, a), 7.33-7.45 (IH, m) , 7.63-7.80 (2H, m) , 8.18 (IH, d, J=8Hz), 8.30 (IH, d, J=8Hz) , 8.53-8.70 (2H, m) , 9.18 (IH, s) (2) MASS : 461 (M+l) NMR (CDCI3, δ) : 0.83 (3 x 1/4H, t, J=8Hz) , 0.89 (3 x 3/4H, t, J=8Hz), 1.10-1.40 (4H, m) , 1.52-1.80 (2H, m) , 2.97 (3 x 1/4H, s) , 3.10 (3 x 3/4H, s), 3.00- 3.13 (IH, ) , 3.25-3.38 (IH, ) , 3.70-3.79 (1 x 1/4H, m) , 3.80-3.85 (1 x 3/4H, a), 4.57 (2 x 3/8H, d, J=15Hz), 4.71 (2 x 3/8H, d, J=15Hz) , 4.73 (2 x 1/4H, s), 4.87-5.01 (IH, m) , 7.18 (IH, t, J=5Hz) , 7.22 (IH, d, J=8Hz), 7.37-7.45 (IH, m) , 7.61 (IH, t, J=8Hz), 7.68-7.81 (2H, a) , 8.18 (1 x 1/4H, d, J=8Hz), 8.20 (1 x 3/4H, d, J=8Hz) , 8.31 (IH, d, J=8Hz), 8.52 (IH, d, J=2Hz) , 8.59 (IH, s) , 8.63 (IH, d, J=2Hz), 9.18 (IH, s) (3) MASS : 444 (M+l) NMR (CDCI3, δ) : 0.85 (3 x 1/4H, t, J=8Hz) , 0.89 (3 x 3/4H, t, J=8Hz), 1.20-1.45 (4H, m) , 1.57-1.90 (3H, ) , 2.09-2.22 (IH, m) , 2.10 (3H, s) , 2.61 (2H, t, J=8Hz), 2.94 (3 x 1/4H, s), 3.09 (3 x 3/4H, s) . 3.43-3.60 (IH, m) , 4.58 (2 x 3/8H, d, J=15Hz), 4.71 (2 x 3/8H, d, J=15Hz), 4.70 (2 x 1/8H, d, J=16Hz) , 4.75 (2 x 1/8H, d, J=16Hz) , 4.88-5.12 (IH, m) , 7.40 (IH, dd, J=8, 5Hz), 7.64-7.81 (2H, m) , 7.87 (IH, d, J=8Hz), 8.30 (IH, dd, J=8, 2Hz) , 8.59 (IH, s) , 8.63 (IH, d, J=2Hz), 9.18 (IH, s) (4) NMR (CDC1 3 , δ) : 0.88 (3H, t, J=7Hz) , 1.33 (4H, m) , 1.66 (2H, m) , 2.55 (3H, s) , 2.67 (IH, dd, J=7, 15Hz), 2.86 (IH, dd, J=3, 15Hz), 2.91 (3H x 1/4, s), 3.02 (3H x 3/4, s) , 3.47 (2H, m) , 3.67 (6H, m) , 3.73 (IH, m) , 4.43 (IH x 3/4, d, J=15Hz) , 4.63 (2H x 1/4, s), 4.68 (IH x 3/4, d, J=15Hz) , 4.89 (IH, m) , 7.13 (IH x 3/4, d, J=8Hz) , 7.16 (IH x 1/4, d, J=8Hz), 7.47 (IH, m) , 8.10 (IH, ) , 8.36 (IH, d, J=2Hz) (5) NMR (CDCI3, δ) : 0.86 (3H, t, J=7Hz) , 1.22 (4H, m) , 1.52-1.73 (2H, ) , 2.53 (3H, s) , 2.90 (3H x 1/4, s), 3.01 (3H x 3/4, s), 3.02-3.07 (IH, m) , 3.26- 3.34 (IH, a) , 3.73 (IH x 1/4, dd, J=3, 7Hz) , 3.80 (IH x 3/4, dd, J=3, 7Hz), 4.42 (IH x 3/4, d, J=15Hz), 4.63 (2H x 1/4, s), 4.67 (IH x 3/4, d, J=15Hz), 4.90 (IH, m) , 7.12-7.37 (3H, a), 7.47 (IH, m) , 7.62 (IH, m) , 8.17 (IH, m) , 8.35 (IH, s) (6) NMR (CDCI3, δ) : 0.89 (3H, t, J=7Hz) , 1.31 (4H, m) , 1.70 (2H, m) , 1.83 (IH, m) , 2.11 (3H, s), 2.15 (IH, m), 2.54 (3H, s) , 2.62 (2H, t, J=7Hz) , 2.92 (3H x 1/4, s), 3.03 (3H x 3/4, s) , 3.47 (IH x 1/4, m) , 3.53 (IH x 3/4, m) , 4.43 (IH x 3/4, d, J=15Hz) , 4.60 (IH x 1/4, d, J=16Hz) , 4.66 (IH x 1/4, d, J=16Hz), 4.67 (IH x 3/4, d, J=15Hz) , 4.92 (IH, m) , 7.13 (IH x 3/4, d, J=8Hz), 7.17 (IH x 1/4, d, J=8Hz), 7.47 (IH, d, J=8Hz) , 7.84 (IH, d, J=8Hz) , 8.35 (IH, s) (7) NMR (CDC1 3 , δ) : 0.88 (3H, t, J=7Hz) , 1.32 (4H, m) , 1.73 (2H, m) , 2.54 (3H, s) , 2.91 (3H x 1/4, s) , 3.02 (3H x 3/4, s) , 3.47 (IH, a) , 3.67 (IH, m) , 3.82 (IH, m) , 4.47 (IH x 3/4, d, J=15Hz) , 4.53 (IH x 1/4, d, J=16Hz) , 4.65 (IH x 3/4, d, J=15Hz), 4.69 (IH x 1/4, d, J=16Hz) , 4.88 (IH, a), 7.13 (IH x 3/4, d, J=8Hz), 7.19 (IH x 1/4, d, J=8Hz) , 7.47 (IH x 3/4, m) , 7.53 (IH x 1/4, m) , 7.71 (IH, m) (8) MASS : 497 (M+l) NMR (CDCI3, δ) : 2.31 (3H, s) , 2.33-2.45 (4H, m) , 2.43-2.53 (IH, m) , 2.68 (3 x 3/4H, s) , 2.71-2.85 (IH, m) , 2.81 (3 x 1/4H, s) , 2.97-3.16 (2H, a) , 3.38-3.50 (2H, m) , 3.52-3.73 (3H, m) , 3.80 (3 x 1/4H, s), 3.83 (3 x 3/4H, s) , 4.10 (2 x 1/8H, d, J=16Hz) , 4.40 (2 x 1/8H, d, J=16Hz) , 4.41 (2 x 3/8H, d, J=15Hz), 4.54 (2 x 3/8H, d, J=15Hz) , 5.10 (1 x 3/4H, q, J=8Hz) , 5.19 (1 x 1/4H, q, J=8Hz) , 6.94 (1 x 1/4H, s), 7.06 (1 x 3/4H, s) , 7.13-7.33 (5H, m) , 7.90 (1 x 1/4H, s) , 8.01 (1 x 3/4H, s), 8.11 (1 x 1/4H, s), 8.17 (1 x 3/4H, s) , 8.20 (1 x 1/4H, s) , 8.22 (1 x 3/4H, s) (9) NMR (CDCI3, δ) : 2.31 (3H, s) , 2.39-2.60 (4H, m) , 2.74 (3 x 2/3H, s), 2.80 (3 x 1/3H, s) , 2.76-2.86 (IH, m) , 2.92-3.10 (3H, m) , 3.40-3.50 (2H, m) , 3.52-3.72 (2H, m) , 3.67-3.72 (1 x 2/3H, m) , 3.75-3.81 (1 x 1/3H, m) , 3.81 (3 x 1/3H, s) , 3.82 (3 x 2/3H, s) , 3.87 (2 x 1/6H, d, J=16Hz) , 4.41 (2 x 1/6H, d, J=16Hz), 4.42 (2 x 1/3H, d, J=15Hz) , 4.56 (2 x 1/3H, d, J=15Hz), 5.10 (1 x 2/3H, q, J=8Hz) , 5.37 (1 x 1/3H, q, J=8Hz), 6.73 (1 x 1/3H, d, J=8Hz) , 6.78 (1 x 2/3H, d, J=8Hz) , 7.10-7.31 (5H, m) , 8.06 (1 x 1/3H, s), 8.21 (1 x 2/3H, s), 8.11-8.20 (IH, m) , 8.41 (IH, d, J=8Hz) (10) MASS : 545 (M+l) NMR (CDC1 3 , δ) : 2.40 (3H, s), 2.43-2.64 (5H, m) , 2.68 (3 x 4/5H, s), 2.71-2.88 (IH, m) , 2.81 (3 x 1/5H, s), 2.97-3.14 (2H, a) , 3.47-3.58 (2H, m) , 3.60-3.83 (3H, m) , 4.18 (2 x 1/8H, d, J=16Hz) , 4.30 (2 x 3/8H, d, J=15Hz), 4.38 (2 x 1/8H, d, J=16Hz) , 4.58 (2 x 3/8H, d, J=15Hz), 5.10 (IH, q, J=8Hz) , 7.11- 7.30 (5H, m) , 7.46 (1 x 1/4H, s) , 7.68 (1 x 3/4H, s), 8.18 (IH, q, J=8Hz), 8.20 (1 κ 1/4H, s), 8.30 (1 x 3/4H, s), 8.58 (1 x 1/4H, s) , 8.60 (1 x 3/4H, s) Preparation 108 The following compound was obtained according to a similar manner to that of Preparation 23. MASS : 201 (M+l) NMR (CDCI3, δ) : 2.49 (3H, s) , 3.77 (2H, s), 7.84 (IH, s), 8.47 (IH, s), 8.57 (IH, s) Prepa ation.109 To a solution of Starting Compound (1.02 g) in toluene (6 ml) was added Lawesson's reagent (1.29 g) , and the mixture was refluxed for 24 hours. After the mixture was allowed to cool to room temperature, it was subjected to silica gel column chromatography (hexane) to collect a yellow bond. The eluate was evaporated and recrystallized from hexane to give Object Compound (600 mg) as yellow crystals, mp : 78-79°C NMR (CDCI3, δ) : 4.28 (3H, s), 7.22-7.74 (5H, m) Preparation 110 The following object compound was obtained according to a similar manner to that of Preparation 1, 6, 11, 38, 52 or 56. MASS (m/z) : 368 (M+H) + NMR (CDC1 3 , δ) : 1.42 (9H, s) , 1.72-2.00 (2H, a), 2.02 (1/4 x 3H, s), 2.08 (3/4 x 3H, s) , 2.52 (3H, s) , 2.53 (2H, ) , 2.89 (1/4 x 3H, s) , 3.02 (3/4 x 3H, s), 4.51 (1/4 κ IH, d, J=17Hz) , 4.53 (3/4 κ 2H, ABq, Δ=0.12, J=15Hz) , 4.72 (1/4 x IH, d, J=17Hz) , 4.73-4.97 (IH, m) , 5.25-5.44 (IH, m) , 7.10 (3/4 x IH, d, J=8Hz), 7.15 (1/4 x IH, d, J=8Hz) , 7.46 (IH, dd, J=8, 2Hz), 8.36 (IH, d, J=2Hz) Preparation 111 The following object compound was obtained according to a similar manner to that of Preparation 3, 4, 8, 41 or 54. MASS (m/z) : 268 (M+H) + NMR (CDCI3, δ) : 1.58-1.95 (2H, m) , 2.03 (1/4 x 3H, s), 2.08 (3/4 x 3H, s) , 2.50-2.78 (2H, m) , 2.53 (3H, s), 2.92 (1/4 x 3H, s) , 2.98 (3/4 x 3H, s), 3.81-3.94 (IH, m) , 4.45 (1/4 x IH, d, J=17Hz) , 4.56 (3/4 x 2H, ABq, Δ=0.19, J=15Hz) , 4.72 (1/4 x IH, d, J=17Hz), 7.11 (3/4 x IH, d, J=8Hz) , 7.16 (1/4 x IH, d, J=8Hz), 7.41 (1/4 x IH, dd, J=8, 2Hz) , 7.48 (3/4 x IH, dd, J=8, 2Hz), 8.37 (IH, d, J=2Hz) Preparation 112 The following compounds were obtained according to a similar manner to that of Preparation 1, 6, 11, 38, 52 or 56. (1) MASS (m/z) : 516 (M+H) + NMR (CDCI3, δ) : 1.44 (9H, s), 1.56-1.97 (2H, m) , 1.92 (1/4 x 3H, s), 1.98 (3/4 x 3H, s), 2.11-2.26 (2H, m) , 2.52 (3H, s), 2.83 (1/4 x 3H, s) , 2.97 (3/4 x 3H, s), 3.08-3.46 (2H, m) , 4.48-4.62 (IH, m) , 4.50 (3/4 x 2H, ABq, J=15HZ) , 4.58 (1/4 x 2H, s) , 4.90-5.13 (IK, m) , 6.45-6.63 (IH, m) , 7.03-7.68 (6H, ) , 8.32 (IH, s) , 8.51 (IH, s) (2) MASS (m/z) : 455 (M+H) + NMR (CDC1 3 , δ) : 1.44 (9H, s) , 1.75-2.15 (2H, m) , 2.02 (1/4 x 3H, s), 2.07 (3/4 x 3H, s) , 2.45-2.59 (5H, ) , 2.87 (1/4 x 3H, s) , 3.03 (3/4 x 3H, s) , 3.50- 3.69 (IH, m) , 3.78 (IH, br s) , 3.85-4.10 (IH, m) , 4.10-4.30 (IH, m) , 4.46 (1/4 x IH, d, J=17Hz) , 4.53 (3/4 x 2H, ABq, Δ=0.13, J=15Hz) , 4.78 (1/4 x IH, d, J=17Hz), 4.98-5.22 (IH, m) , 5.42-5.58 (IH, m) , 7.03-7.62 (3H, m) , 8.32 (3/4 x IH, s) , 8.38 (1/4 x IH, s) (3) MASS (m/z) : 552 (M+H) + NMR (CDCI3, δ) : 1.47 (9H, s) , 1.81-2.10 (2H, m) , 2.02 (3H x 1/4, s), 2.08 (3H x 3/4, s) , 2.46-2.61 (6H, ) , 2.89 (3H x 1/4, s) , 3.02 (3H x 3/4, s) , 3.16- 3.28 (IH, m), 3.37-3.49 (2H, m) , 3.53-3.75 (6H, m) , 4.40 (IH x 3/4, d, J=15.0Hz), 4.48-4.60 (IH + IH x 1/4, ) , 4.68 (IH, d, J=15.0Hz), 5.01-5.11 (IH x 3/4, m) , 5.13-5.22 (IH x 1/4, m) , 6.02 (IH, d, J=8.5Hz), 7.12 (IH x 3/4, d, J=8.5Hz), 7.17 (IH x 1/4, d, J=8.5Hz), 7.35 (IH x 1/4, d, J=8.5Hz), 7.43 (IH x 3/4, d, J=8.5Hz), 7.46 (IH, dd, J=8.5, 1.0Hz), 8.36 (IH, d, J=1.0Hz) (4) MASS (m/z) : 499 (M+H) + NMR (CDCI3, δ) : 1.47 (9H, s) , 1.79-2.14 (4H, m) , 2.03 (3H x 1/4, s), 2.08 (3H x 3/4, s) , 2.11 (3H, s) , 2.45-2.62 (7H, s) , 2.89 (3H x 1/4, s) , 3.03 (3H x 3/4, s), 4.20-4.33 (IH, ) , 4.44 (IH x 3/4, d. J=15.0Hz), 4.54 (IH x 1/4, d, J=15.0Hz), 4.64 (IH x 3/4, d, J=15.0Hz), 4.72 ( IH x 1/4, d, J=15.0Hz), 5.02-5.25 (2H, ) , 6.93 (IH x 1/4, d, J=8.5Hz), 6.98 (IH x 3/4, d, J=8.5Hz), 7.13 (IH x 3/4, d, J=8.5Hz), 7.19 (IH x 1/4, d, J=8.5Hz), 7.46 (IH x 3/4, dd, J=8.5, 1.5Hz), 7.48 (IH x 1/4, dd, J=8.5, 1.5Hz), 8.37 (IH, d, J=1.5Hz) Preparation 113 The following compounds were obtained according to a similar manner to that of Preparation 3, 4, 8, 41 or 54. (1) MASS (m/z) : 416 (M+H) + NMR (CDC1 3 , δ) : 1.74-2.03 (2H, m) , 2.00 (1/4 x 3H, s), 2.06 (3/4 x 3H, s), 2.30-2.46 (2H, m) , 2.54 (3H, s), 2.88 (1/4 x 3H, s) , 3.02 (3/4 x 3H, s), 3.07-3.38 (2H, m) , 3.77-3.97 (IH, m) , 4.53 (3/4 x 2H, ABq, Δ=0.18, J=15Hz) , 4.62 (1/4 x 2H, ABq, Δ=0.13, J=17Hz), 4.98-5.22 (IH, m) , 7.07-7.68 (5H, m) , 8.17-8.32 (IH, m) , 8.36 (IH, s) , 8.48-8.55 (IH, m) (2) MASS (m/z) : 355 (M+H) + NMR (CDCI3, δ) : 1.80-2.10 (2H, m) , 2.02 (1/4 x 3H, s), 2.06 (3/4 x 3H, s), 2.42-2.58 (5H, m) , 2.90 (1/4 x 3H, s), 3.05 (3/4 x 3H, s) , 3.38-4.02 (3H, m) , 4.46 (1/4 x IH, d, J=17Hz) , 4.54 (3/4 x 2H, ABq, Δ=0.16, J=15Hz), 4.78 (1/4 x IH, d, J=17Hz) , 5.01-5.22 (IH, m) , 7.08-7.22 (IH, m) , 7.42-7.57 (IH, m) , 7.76-7.93 (IH, m) , 8.37 (IH, s) (3) MASS (m/z) : 452 (M+H) + NMR (CDCI3, δ) : 1.85-2.21 (2H, m) , 2.02 (3H x 1/4, s), 2.09 (3H x 3/4, s) , 2.49-2.61 (5H, m) , 2.73- 2.82 (2H, m) , 2.90 (3H x 1/4, s), 3.04 (3H x 3/4, s), 3.40-3.50 (2H, m) , 3.54-3.74 (7H, m) , 4.43 (IH x 3/4, d, J=15.0Hz), 4.59 (IH x 1/4, d, J=15.0Hz), 4.65 (IH x 3/4, d, J=15.0Hz), 4.71 (IH x 1/4, d, J=15.0Hz), 5.01-5.21 (IH, m) , 7.11 (IH x 3/4, d, J=8.5Hz), 7.17 (IH x 1/4, d, J=8.5Hz), 7.48 (IH, dd, J=8.5, 1.0Hz), 8.14 (IH x 1/4, d, J=8.5Hz), 8.20 (IH x 3/4, d, J=8.5Hz), 8.37 (IH, d, J=1.0Hz) (4) MASS (m/z) : 399 (M+H) + NMR (CDC1 3 , δ) : 1.71-2.22 (4H, m) , 2.03 (3H x 1/4, s), 2.09 (3H x 3/4, s) , 2.10 (3H, s) , 2.45-2.67 (4H, m) , 2.55 (3H, s) , 2.90 (3H x 1/4, s), 3.06 (3H x 3/4, s), 3.44 (IH x 1/4, dd, J=8.5, 5.5Hz), 3.52 (IH x 3/4, dd, J=8.5, 5.5Hz), 4.43 (IH x 3/4, d, J=14.5Hz), 4.60 (IH x 1/4, d, J=16.0Hz), 4.67 (IH x 3/4, d, J=14.5Hz), 4.73 (IH x 1/4, d, J=16.0Hz), 5.03-5.22 (IH, m) , 7.12 (IH x 3/4, d, J=8.5Hz), 7.17 (IH x 1/4, d, J=8.5Hz), 7.47 (IH x 3/4, dd, J=8.5, 1.0Hz), 7.50 (IH x 1/4, dd, J=8.5, 1.0Hz), 7.88-7.98 (IH, m) , 8.37 (IH, d, J=1.0Hz) Preparation 114 The following compound was obtained according to a similar manner to that of Preparation 23. (1) M7ASS : 153 (M+l) NMR (CDCI3, δ) : 2.43 (3H, s) , 3.78 (2H, s) , 3.96 (3H, s), 6.76 (IH, d, J=7Hz), 8.35 (IH, s), 8.43 (IH, d, J=7Hz) (2) MASS : 153 (M+l) NMR (CDCI3, δ) : 2.43 (3H, s) , 3.72 (2H, s) , 3.81 (3H, s), 7.20 (IH, s), 8.12 (IH, s) , 8.19 (IH, d, J=2Hz) Example 1 To an ice-cooled solution of benzo[b] furan-2-carboxylιc acid (70 mg) , Starting Compound (200 mg) , and 1-hydroxybenzotriazole (58 mg) in methylene chloride (20 ml) , was added l-ethyl-3- (3-dimethylaminopropyl) carbodiimide hydrochloride (82 mg) . The solution was stirred at the same temperature for an hour and at room temperature overnight. The mixture was concentrated under vacuum and the residue was diluted in water and extracted with chloroform. The organic layer was washed with saturated sodium hydrogencarbonate solution, water and brine, and was dried over magnesium sulfate. After evaporation, the crude material obtained was purified on a column of silica gel eluting with chloroform- methanol (30:1) to give Object Compound (260 mg) as an amorphous solid. MASS (FAB) (m/z) : 610 (M+H) + NMR (CDCI3, δ) : 2.28 (3H, s) , 2.36-2.50 (4H, a), 2.58 (3 x 2/3H, s), 2.62-2.71 (IH, m) , 2.80 (3 x 1/3H, s), 2.98-3.11 (2H, m) , 3.27-3.38 (IH, m) , 3.42-3.56 (2H, m) , 3.66-3.70 (2H, a), 4.11-4.38 (2 x 2/3H, a), 4.65 (2 x 1/3H, d, J=15Hz) , 5.02-5.17 (2H, m) , 6.93-7.06 (2H, m) , 7.12-7.21 (6H, m) , 7.22-7.32 (3H, m) , 7.43 (IH, t, J=8Hz) , 7.50 (IH, s) , 7.57 (IH, d, J=8Hz), 7.63-7.72 (2H, a), 8.19-8.23 (IH, m) Example 2 The following object compounds were obtained according to a similar manner to that of Example 1. (1) MASS (FAB) (m/z) : 626 (M+H) + NMR (CDCI3, δ) : 2.28 (3H, s) , 2.34-2.51 (4H, a), 2.56-2.68 (IH, m) , 2.62 (3 x 2/3H, s), 2.80 (3 x 1/3H, s), 3.00-3.07 (2H, m) , 3.31 (IH, t, J=15Hz), 3.42-3.58 (2H, m) , 3.62-3.70 (2H, m) , 4.12-4.41 (2 x 2/3H, m) , 4.64 (2 κ 1/3H, d, J=15Hz), 4.98-5.14 (2H, m) , 6.98-7.03 (2H, a), 7.12-7.21 (6H, m) , 7.23-7.31 (3H, a), 7.37-7.46 (2H, a), 7.68-7.75 (IH, m) , 7.80-7.88 (2H, a), 8.13 (IH, d, J=8Hz) (2) MASS (FAB) (m/z) : 613 (M+H) + NMR (CDC1 3 , δ) : 2.52-2.69 (IH, m) , 2.63 (3 x 2/3H, s), 2.83 (3 x 1/3H, s), 3.01-3.09 (2H, a) , 3.30 (IH, t, J=15Hz), 3.41-3.53 (2H, m) , 3.62-3.79 (6H, m), 4.12-4.43 (2 x 2/3H, ) , 4.63 (2 x 1/3H, d, J=15Hz), 4.98-5.13 (2H, m) , 6.99-7.21 (7H, m) , 7.23-7.33 (3H, m) , 7.36-7.45 (2H, m) , 7.67-7.90 (4H, m), 8.12 (IH, t, J=8Hz) (3) MASS (FAB) (m/z) : 596 (M+H) + NMR (CDCI3, δ) : 2.58-2.70 (IH, m) , 2.59 (3 x 2/3H, s), 2.82 (3 x 1/3H, s) , 3.04 (2H, t, J=8Hz) , 3.29 (IH, t, J=15Hz), 3.42-3.58 (2H, m) , 3.63-3.77 (6H, m) , 4.12-4.40 (2 x 2/3H, m) , 4.66 (2 x 1/3H, d, J=15Hz), 5.02-5.16 (2H, m) , 6.97-7.33 (11H, m) , 7.42-7.72 (5H, m) , 8.11 (IH, d, J=8Hz) (4) MASS (FAB) (m/z) : 630 (M+H) + NMR (CDCI3, δ) : 2.68 (3 x 2/3H, s), 2.72 (IH, dd, J=15, 7Hz), 2.83 (3 x 1/3H, s) , 2.95-3.08 (2H, m) , 3.11-3.22 (IH, a), 3.33-3.48 (2H, m) , 3.53-3.68 (6H, m) , 4.19-4.42 (2 x 2/3H, a), 4.72 (2 x 1/3H, d, J=15Hz), 5.13-5.32 (2H, m) , 6.88 (IH, d, J=8Hz), 6.98-7.12 (6H, m) , 7.18 (IH, d, J=8Hz) , 7.22-7.29 (4H, m) , 7.33 (IH, d, J=8Hz) , 7.59 (IH, s) , 8.04-8.22 (2H, m) (5) MASS (FAB) (m/z) : 626 (M+H) + NMR (CDCI3, δ) : 2.62 (3 x 2/3H, s) , 2.72 (IH, dd, J=15, 7Hz), 2.83 (3 x 1/3H, s) , 2.93-3.08 (2H, m) , 3.13-3.22 (IH, a) , 3.33-3.50 (2H, m) , 3.52-3.68 (6H, m) , 3.87 (3H, s), 4.17-4.40 (2 x 2/3H, m) , 4.71 (2 x 1/3H, d, J=15Hz), 5.12-5.30 (2H, m) , 6.89-7.00 (3H, m) , 7.02-7.16 (8H, m) , 7.27-7.33 (3H, m) , 7.95-8.13 (2H, m) (6) MASS (FAB) (m/z) : 614 (M+H) + NMR (CDC1 3 , δ) : 2.67 (3 x 2/3H, s) , 2.72 (IH, dd, J=15, 8Hz), 2.82 (3 x 1/3H, s), 2.99-3.03 (2H, m) , 3.13-3.24 (IH, m) , 3.33-3.49 (2H, m) , 3.53-3.68 (6H, m) , 4.19-4.41 (2 x 2/3H, m) , 4.70 (2 κ 1/3H, d, J=15Hz), 5.13-5.31 (2H, ) , 6.91-7.15 (9H, a), 7.25-7.29 (4H, m) , 7.32-7.38 (IH, m) , 8.02-8.17 (2H, m) (7) MASS (FAB) (m/z) : 597 (M + +l) NMR (CDCI3, δ) : 2.42 (1 x 1/3H, d, J=15Hz) , 2.61 (IH, a), 2.88 (3 x 1/3H, s), 2.97 (3 x 2/3H, s) , 3.05- 3.28 (3H, m) , 3.41 (2H, m) , 3.55-3.64 (6H, a) , 4.30 (1 x 1/3H, d, J=15Hz) , 4.75 (1 x 2/3H, d, J=15Hz) , 4.85 (1 κ 2/3H, d, J=15Hz) , 5.17 (IH, a) , 5.39 (IH, a), 6.98-7.17 (5H, m) , 7.22-7.33 (3H, m) , 7.37-7.66 (3H, m) , 8.00-8.48 (3H, m) (8) MASS (FAB) (m/z) : 610 (M + +l) NMR (CDCI3, δ) : 2.27 (3H, S), 2.24-2.38 (4H, a) , 2.55-2.67 (IH, a), 2.85 (3 κ 1/3H, s), 2.96 (3 x 2/3H, s), 3.07-3.32 (3H, m) , 3.45 (2H, m) , 3.62 (2H, a), 4.23 (1 x 2/3H, d, J=15H∑) , 4.53 (1 x 1/3H, d, J=15Hz), 4.81 (1 x 2/3H, d, J=15Hz) , 4.88 (1 x 1/3H, d, J=15Hz), 5.14 (IH, m) , 5.38 (IH, q, J=7HZ), 6.98-7.33 (10H, m) , 7.38-7.53 (2H, m) , 7.63 (IH, m) , 8.03-8.16 (2H, m) , 8.37 (IH, m) (9) MASS (FAB) (m/z) : 575 (M + +l) NMR (CDC1 3 , δ) : 1.75 (IH, m) , 2.17 (3H, s), 2.15-2.32 (3H, m) , 2.69 (IH, dd, J=6, 15H∑) , 2.93-3.03 (3H, m) , 3.23-3.67 (12H, m) , 5.12 (IH, m) , 5.17 (IH, m) , 7.00 (IH, d, J=2Hz), 7.12-7.22 (6H, m) , 7.30 (IH, t, J=8Hz), 7.44 (IH, d, J=8Hz), 7.66 (IH, d, J=8Hz), 7.91 (IH, d, J=7Hz), 8.04 (IH, d, J=8H∑) (10) MASS (FAB) (m/z) : 577 (M + +l) NMR (CDCI3, δ) : 2.17 (6 x 1/3H, s), 2.21 (6 x 2/3H, s), 2.30 (IH, m) , 2.65-2.75 (IH, m) , 2.72 (3 x 2/3H, s), 2.89 (3 x 1/3H, s) , 2.99 (2H, d, J=7Hz), 3.09 (IH, m) , 3.18-3.27 (2K, m) , 3.44 (2H, m) , 3.52 (IH, m) , 3.62 (6H, m) , 5.05 (IH, m) , 5.18 (IH, ) , 6.98 (IH, s) , 7.12-7.17 (6H, m) , 7.30 (IH, d, J=8Hz), 7.45 (IH, d, J=8Hz) , 7.65 (IH, d, J=8Hz), 7.88 (IH, m) , 7.95-8.02 (IH, m) (11) MASS (FAB) (m/z) : 582 (M + +l) NMR (CDCI3, δ) : 2.63-2.76 (2H, ) , 2.90 (IH, dd, J=7, 13Hz), 3.19 (3H, s) , 3.18-3.25 (IH, m) , 3.44 (2H, m) , 3.65 (6H, m) , 4.75 (IH, q, J=7Hz) , 5.12 (IH, m) , 6.88-6.95 (5H, m) , 7.12 (4H, m) , 7.28-7.33 (4H, m) , 7.44 (IH, d, J=8Hz) , 7.65 (IH, d, J=8Hz) , 7.80 (IH, d, J=7Hz), 7.94 (IH, d, J=8Hz) (12) MASS (FAB) (m/z) : 618 (M+H) + NMR (CDCI3, δ) : 2.60 (3 x 2/3H, s) , 2.72-2.88 (IH, m), 2.82 (3 x 1/3H, s) , 2.91-3.20 (3H, m) , 4.16- 4.40 (2 x 2/3H, m) , 4.65 (2 x 1/3H, d, J=15Hz) , 4.99-5.17 (2H, m) , 5.17 (2H, s), 6.98-7.15 (7H, a), 7.27-7.37 (10H, m) , 7.45 (IH, t, J=8Hz) , 7.51-7.55 (2H, ) , 7.68-7.78 (2H, m) (13) mp : 154°C MASS (FAB) (m/z) : 542 (M + +l) NMR (CDC1 3 , δ) : 1.24 (3H, t, J=7Hz) , 2.77 (IK, dd, J=7, 16Hz), 3.02-3.17 (3H, m) , 4.17 (2H, q, J=7Hz), 4.82 (IH, q, J=7Hz) , 5.07 (IH, m) , 5.14 (IH, d, J=15Hz), 5.20 (IH, d, J=15Hz) , 6.78 (IH, s) , 7.05 (5H, s), 7.14-7.21 (2H, m) , 7.29-7.37 (5H, m) , 7.43 (IH, d, J=8HZ), 7.54 (IH, d, J=8Hz) , 7.67 (IH, d, J=8Hz) , 9.15 (IH, br s) Example 3 Starting Compound (200 mg) , 4-cyclohexylpiperazine (64 mg) , and 1-hydrobenzotriazole (51 mg) were dissolved in a mixed solvent of methylene chloride (20 ml) and N,N- dimethylformamide (10 ml) . The mixture was ice-cooled and l-ethyl-3- (3-dimethylaminopropyl)carbodiimide hydrochloride (73 mg) was added thereto. The mixture was stirred at this temperature for 1 hour and at room temperature for overnight. The mixture was concentrated under vacuum and residue was diluted in water and extracted with chloroform. The organic layer was washed with saturated sodium hydrogencarbonate solution and brine. After evaporation, the crude material obtained was purified on a column of silica gel eluting with chloroform-methanol (60:1) to give Object Compound (210 mg) as an amorphous solid. MASS (FAB) (m/z) : 677 (M+H) + NMR (CDC1 3 , δ) : 0.98-1.21 (5H, m) , 1.53-1.61 (IH, a), 1.70-1.80 (4H, m) , 2.40-2.52 (4H, m) , 2.50-2.65 (IH, m) , 2.56 (3 x 2/3H, s), 2.62-2.77 (IH, m) , 2.80 (3 x 1/3H, s), 2.94-3.08 (2H, m) , 3.18-3.28 (IH, m) , 3.35-3.47 (2H, a)., 3.52-3.65 (2H, m) , 4.17-4.36 (2 x 2/3H, a), 4.69 (2 x 1/3H, d, J=15Hz), 5.11-5.27 (2H, m) , 6.93-7.15 (9H, a), 7.22-7.29 (4H, m) , 7.43 (IH, d, J=8Hz) , 7.66 (IK, d, J=8Hz), 7.99-8.12 (2H, m) Example 4 The following object compounds were obtained according to a similar manner to that of Example 3. (1) MASS (FAB) (m/z) : 637 (M+H) + NMR (CDC1 3 , δ) : 0.84 (3H, t, J=8Hz) , 1.41-1.52 (2H, m), 2.27 (2H, t, J=8Hz), 2.32-2.46 (4H, a), 2.58 (3 x 2/3H, s), 2.62-2.72 (IH, m) , 2.30 (3 x 1/3H, s), 2.95-3.08 (2H, m) , 3.22-3.31 (IH, m) , 3.40-3.51 (2H, m) , 3.56-3.70 (2H, a), 4.14-4.38 (2 x 2/3H, m) , 4.69 (2 x 1/3H, d, J=15Hz) , 5.10-5.21 (2H, m) , 6.95-7.18 (10H, a), 7.23-7.30 (3H, m) , 7.43 (IH, d, J=8Hz), 7.65 (IH, d, J=8Hz) , 7.89-7.97 (IH, m) , 8.04-8.11 (IH, m) , 9.87 (IH, br s) (2) MASS (FAB) (m/z) : 594 (M+H) + NMR (CDCI3, δ) : 1.28-1.53 (6H, m) , 1.75-1.92 (2H, m) , 2.62-2.76 (IH, m) , 2.72 (3 x 2/3H, s), 2.92 (3 x 1/3H, s), 2.83-3.19 (3H, ) , 4.09 (IH, m) , 4.22 (2 x 1/3H, d, J=15Hz) , 4.39 (2 x 1/3H, s), 4.90 (2 x 1/3H, d, J=15Hz), 5.23-5.41 (IH, m) , 5.60-5.80 (IH, m) , 6.85-7.11 (7H, a) , 7.12-7.16 (3H, m) , 7.22-7.30 (4H, m) , 7.43-7.50 (IH, m) , 7.62-7.68 (IH, m) , 8.04 (1 x 1/3H, d, J=8Hz) , 8.22 (1 x 2/3H, d, J=8Hz) , 8.91 (1 x 1/3H, d, J=8Hz) , 9.00 (1 x 2/3H, d, J=8Hz) (3) MASS (FAB) (m/z) : 667 (M+H) + NMR (CDCI3, δ) : 1.27 (3H, t, J=8Hz) , 2.58-2.71 (IH, ) , 2.65 (3 x 2/3H, s), 2.89 (3 x 1/3H, s) , 2.99-3.04 (2H, m) , 3.28 (IH, t, J=15Hz) , 3.40-3.58 (6H, ) , 3.60-3.67 (2H, m) , 4.15 (2K, q, J=8Hz) , 4.28-4.43 (2 x 2/3H, m) , 4.68 (2 x 1/3H, d, J=15Hz), 5.05-5.18 (2H, a), 6.98-7.20 (9H, m) , 7.26-7.33 (4H, m) , 7.45 (IH, d, J=8Hz) , 7.67-7.82 (2H, m) , 8.03 (IH, d, J=8Hz) , 9.41 (IH, d, J=8Hz) (4) mp : 85-90 β C MASS (FAB) (m/z) : 609 (M+H) ~ NMR (CDC1 3 , δ) : 2.30 (3H, s) , 2.33-2.52 (4H, m) , 2.57-2.69 (IH, m) , 2.62 (3 x 2/3H, s) , 2.73 (3 x 1/3H, s), 2.99-3.07 (2H, m) , 3.27-3.36 (IH, m) , 3.42-3.55 (2H, m) , 3.58-3.75 (2H, a) , 4.14-4.41 (2 x 2/3H, a), 4.67 (2 x 1/3H, a) , 5.12 (2H, t, J=8Hz), 6.95-7.21 (9H, a) , 7.23-7.35 (4H, a) , 7.43 (IH, d, J=8Hz), 7.69 (IH, d, J=8Hz) , 7.78 (IH, t, J=8Hz), 8.07 (IH, t, J=8Hz), 9.37 (IH, br s) (5) MASS (FAB) (m/z) : 594 (M+H) + NMR (CDCI3, δ) : 1.45-1.69 (6H, a), 2.60 (3 x 2/3H, s), 2.57-2.69 (IH, m) , 2.82 (3 x 1/3H, s), 3.00- 3.10 (2H, m), 3.25-3.43 (3H, m) , 3.45-3.70 (2H, a) , 4.15-4.40 (2 x 2/3H, a) , 4.67 (2 x 1/3H, d, J=15Hz), 5.02-5.18 (2H, a) , 6.95-7.08 (3H, a), 7.12-7.19 (6H, m) , 7.24-7.32 (4H, m) , 7.43 (IH, d, J=8Hz), 7.69 (IH, d, J=8Hz) , 7.73-7.82 (IH, m) , 8.14 (IH, t, J=8Hz), 9.41 (IH, br s) (6) MASS (FAB) (m/z) : 580 (M+H) + NMR (CDCI3, δ) : 1.80-1.95 (4H, m) , 2.53-2.68 (IH, m) , 2.61 (3 κ 2/3H, s), 2.82 (3 x 1/3H, s) , 2.98-3.07 (2H, m), 3.17 (IH, t, J=15Hz) , 3.29-3.40 (IH, m) , 3.42-3.57 (3H, m) , 4.18-4.39 (2 x 2/3H, a), 4.68 (2 x 1/3H, d, J=15Hz) , 5.10-5.17 (2H, m) , 6.94-7.16 (9H, m), 7.21-7.30 (4H, a), 7.43 (IH, d, J=8Hz) , 7.66 (IH, d, J=8HZ) , 7.98-8.02 (IH, a) , 8.40 (IH, t, J=8Hz), 9.80 (IH, d, J=10Hz) (7) MASS (FAB) (m/z) : 612 (M+H) + NMR (CDCI3, δ) : 2.52-2.62 (4H, a), 2.63 (3 x 2/3H, /16981 - 555 - s), 2.66-2.73 (IH, m) , 2.86 (3 x 1/3H, s), 2.99- 3.08 (2H, m) , 3.15-3.26 (IH, m) , 3.63-3.70 (2H, m) , 3.79-3.93 (2H, ) , 4.18-4.42 (2 x 2/3H, m) , 4.70 (2 x 1/3H, d, J=15Hz), 5.12-5.28 (2H, a), 6.97-7.15 (9H, m), 7.24-7.30 (4H, m) , 7.46 (IH, d, J=8Hz) , 7.67 (IH, d, J=8Hz), 7.98-8.08 (2H, m) (8) MASS (FAB) (m/z) : 566 (M+H) + NMR (CDC1 3 , δ) : 0.38-0.61 (4H, a) , 2.52-2.69 (2H, m) , 2.71 (3 x 2/3H, s) , 2.89-3.09 (2H, m) , 2.92 (3 x 1/3H, s), 3.11-3.22 (IH, a), 4.19-4.51 (2 x 2/3H, m) , 4.97 (2 x 1/3H, d, J=15Hz) , 5.30- 5.50 (IH, m) , 5.71-5.94 (IH, m) , 6.87-7.08 (6H, a), 7.12-7.18 (3H, m) , 7.22-7.28 (4H, m) , 7.39-7.50 (2H, m) , 7.62 (IH, d, J=8Hz) , 8.18 (1 x 1/3H, d, J=8Hz), 8.35 (1 x 2/3H, d, J=8Hz) , 9.10 (1 x 1/3H, d, J=8Hz), 9.21 (1 x 2/3H, d, J=8Hz) (9) MASS (FAB) (m/z) : 673 (M+H) + NMR (CDCI3, δ) : 2.63 (3 x 2/3H, s) , 2.67-2.80 (IH, m) , 2.81 (3 x 1/3H, s), 2.98-3.08 (2H, m) , 3.26 (IH, t, J=8Hz), 3.47-3.53 (2H, m) , 3.63-3.92 (6H, m) , 4.18-4.39 (2 x 2/3H, a), 4.72 (2 x 1/3H, d, J=15Hz), 5.12-5.31 (2H, a), 6.49-6.53 (IH, m) , 6.97-7.13 (9H, m) , 7.2-7.30 (4H, m) , 7.47 (IH, d, J=8Hz), 7.67 (IH, d, J=8Hz) , 8.00-8.10 (2H, m) , 8.30 (2H, d, J=5Hz) (10) MASS (FAB) (m/z) : 681 (M+H) + NMR (CDCI3, δ) : 1.23 (3H, t, J=8Hz) , 2.46-2.58 (4H, m) , 2.60 (3 x 2/3H, s) , 2.59-2.75 (IH, m) , 2.81 (3 x 1/3H, s), 2.99-3.03 (2H, m) , 3.17 (2H, s), 3.20-3.28 (IH, a), 3.47-3.51 (2H, m) , 3.60-3.73 (2H, m), 4.17 (2H, q, J=8Hz) , 4.19-4.39 (2 x 2/3K, m) , 4.71 (2 x 1/3H, d, J=15Hz) , 5.11-5.25 (2H, m) , 6.94-7.14 (9H, m) , 7.21-7.29 (4H, a), 7.43 (IH, a, J=8Hz), 7.63 (IH, d, J=8Hz) , 7.93-3.07 (2K, a) (11) MASS (FAB) (m/z) : 677 (M+H) + NMR (CDC1 3 , δ) : 1.32-1.47 (4H, m) , 1.50-1.60 (4H, m) , 1.78-1.82 (2K, m) , 2.42-2.52 (6H, m) , 2.55-3.03 (4H, m) , 2.62 (3 x 2/3H, s), 2.81 (3 κ 1/3H, s) , 3.18-3.30 (IH, m) , 3.80-3.90 (IH, m) , 4.18-4.37 (2 κ 2/3H, m) , 4.69 (2 κ 1/3H, d, J=15Hz) , 4.58- 4.62 (IH, m) , 5.11-5.25 (2H, m) , 6.93-7.03 (2H, m) , 7.08-7.18 (7H, m) , 7.25-7.30 (4H, m) , 7.44 (IH, d, J=8Hz), 7.65 (IH, d, J=8Hz), 7.98-8.13 (2H, m) (12) MASS (FAB) (m/z) : 580 (M+H) + NMR (CDCI3, δ) : 1.47-1.62 (2H, m) , 1.70-1.88 (2K, m) , 2.04-2.15 (IH, ) , 2.20-2.30 (IH, m) , 2.62-2.73 (IH, m) , 2.70 (3 x 2/3H, s) , 2.86-3.17 (3H, a), 2.92 (3 x 1/3H, s), 4.21-4.46 (2 x 2/3H, m) , 4.23- 4.32 (IH, m), 4.93 (2 x 1/3H, d, J=15Kz) , 5.27-5.43 (IH, ) , 5.67-5.88 (IH, m) , 6.90-7.13 (9H, a), 7.22-7.30 (5H, m) , 7.48 (IH, d, J=8Hz) , 7.64 (IH, d, J=8Hz), 8.03 (1 x 1/3H, d, J=8Hz) , 8.21 (1 x 2/3H, d, J=8Hz), 9.00 (1 x 1/3H, d, J=8Hz) , 9.10 (1 x 2/3H, d, J=8Hz) (13) MASS (FAB) (m/z) : 637 (M+H) + NMR (CDCI3, δ) : 1.99 (3 x 1/3H, s), 2.02 (3 x 2/3H, s), 2.61 [3 κ 2/3H, s) , 2.72 (IH, dd, J=15, 5Hz), 2.84 (3 x 1/3H, d, J=2Hz) , 2.97-3.07 (2H, m) , 3.13- 3.26 (IH, m) , 3.32-3.42 (4H, m) , 3.50-3.68 (4H, a), 4.15-4.42 (2 x 2/3H, m) , 4.69 (2 x 1/3H, t, J=15Hz), 5.11-5.32 (2H, m) , 6.93-7.14 (9H, m) , 7.22-7.31 (4H, a), 7.46 (IH, d, J=8Hz) , 7.65 (IH, d, J=8Hz), 7.95-8.17 (2H, m) (14) MASS (FAB) (m/z) : 608 (M+H) + NMR (CDC1 3 , δ) : 0.80-1.11 (3H, a), 1.17-1.31 (2H, a), 1.47-1.67 (3H, m) , 1.78-1.91 (2H, m) , 2.58-2.68 (IH, m), 2.69 (3 x 2/3H, s ) , 2 . 11-2 . 86 (IH, m) , 2.89 (3 x 1/3H, s), 3.00-3.12 (2H, a), 3.61-3.75 (IH, a), 4.20-4.42 (2 x 2/3H, m) , 4.88 (2 x 1/3H, d, J=15Hz), 5.18-5.31 (IH, m) , 5.38-5.52 (IH, m) , 6.38 (IH, t, J=8Hz), 6.98-7.10 (9H, m) , 7.21-7.32 (4H, m), 7.45 (IH, dd, J=8, 2Hz) 7.63 (IH, dd, J=8, 2Hz), 7.96 (1 x 1/3H, d, J=8Hz) , 8.07 (1 x 2/3H, d, J=8Hz), 8.60-8.67 (IH, m) (15) MASS (FAB) (m/z) : 610 (M+H) + NMR (CDC1 3 , δ) : 2.21 (6 x 1/3H, s) , 2.23 (6 x 2/3H, s>' 2.41-2.57 (3H, m) , 2.59 (3 x 2/3H, s) , 2.64- 2.73 (IH, m), 2.81 (3 x 1/3H, s) , 2.97-3.03 (2H, m), 3.02 (3H, s) , 3.18-3.60 (2H, m) , 4.17-4.38 (2 x 2/3H, m), 4.69 (2 x 1/3H, d, J=15Hz) , 5.10-5.21 (2H, m) , 6.94-7.06 (2H, m) , 7.10-7.18 (7H, m) , 7.23-7.31 (4H, m) , 7.45 (IH, d, J=8Hz) , 7.65 (IH, d, J=8Hz), 7.89-8.00 (IH, m) , 8.11-8.23 (IH, a), 9.90 (IH, br s) (16) MASS (FAB) (m/z) : 623 (M+H) + NMR (CDCI3, δ) : 1.82-1.97 (2H, m) , 2.32 (3H, s) , 2.51-2.73 (5H, m) , 2.62 (3 x 2/3H, s) , 2.81 (3 x 1/3H, s), 2.94-3.08 (2H, m) , 3.20-3.30 (IH, m) , 3.42-3.75 (4H, m) , 4.14-4.39 (2 x 2/3H, m) , 4.68 (2 x 1/3H, dd, J=15, 5Hz) , 5.09-5.21 (2K, m) , 6.97-7.05 (2H, m) , 7.10-7.15 (6H, m) , 7.22-7.30 (5H, a), 7.45 (IH, d, J=8Hz) , 7.66 (IH, d, J=8Hz) , 7.91-8.00 (IH, m), 8.14-8.23 (IH, m) (17) MASS (FAB) (m/z) : 597 NMR (CDCI3, δ) : 2.13 (6H, s) , 2.41 (2H, t, J=5Hz) , /16981 - 558 - 2.70 (3 x 2/3H, s) , 2.62-2.80 (IH, a), 2.90 (3 x 1/3H, s), 2.98-3.10 (3H, a), 3.27-3.35 (2H, m) , 4.28-4.43 (2 κ 2/3H, a), 4.83 (2 κ 1/3H, d, J=15Hz), 5.18-5.30 (IH, m) , 5.35-5.49 (IH, m) , 6.98-7.13 (9H, m) , 7.22-7.31 (5H, m) , 7.45 (IK, a, J=8Hz), 7.65 (IH, d, J=8Hz) , 7.92-8.05 (IK, m) , 8.62 (IH, d, J=8Hz) (18) MASS (FAB) (m/z) : 615 NMR (CDC1 3 , δ) : 2.52-2.70 (IH, m) , 2.73 (3 x 2/3K, S), 2.92 (3 x 1/3H, s), 2.75-2.90 (IH, m) , 2.97- 3.12 (2H, a), 4.12 (IH, d, J=15Hz) , 4.33 (IH, d, J=15Hz), 4.22-4.39 (2 x 2/3H, a), 4.83 (2 x 1/3H, d, J=15Hz), 5.22-5.34 (IH, a), 5.50-5.62 (IH, m) , 6.86-7.14 (14H, m) , 7.21-7.31 (5H, m) , 7.48 (IH, d, J=8Hz), 7.66 (IH, d, J=8Hz) , 7.86 (1 x 1/3H, d, J=8HZ), 7.97 (1 x 2/3H, d, J=8Hz) , 8.75 (IH, d, J=8Hz) (19) MASS (FAB) (m/z) : 611 NMR (DMSO-d 6 , δ) : 2.35-2.52 (IH, a), 2.68-2.73 (4H, a), 2.81 (3 x 1/2H, s), 2.83 (3 x 1/2H, s) , 2.76- 3.03 (4H, a), 3.40-3.80 (3H, m) , 4.34-4.56 (2H, m) , 4.80-5.02 (2H, a), 7.02-7.33 (13H, m) , 7.45 (IH, d, J=8Hz), 7.65 (IH, d, J=8Hz) , 8.12-8.40 (IH, m) , 8.43-8.62 (IH, m) , 8.87 (IH, m) (20) MASS (FAB) (m/z) : 540 NMR (CDCI3, δ) : 2.65-2.69 (4H, m) , 2.73 (3 x 2/3H, s), 2.97 (3 x 1/3H, s), 2.87-3.15 (3H, a), 4.29- 4.49 (2 x 2/3H, m) , 4.82 (2 x 1/3H, d, J=15Hz), 5.23-5.42 (IH, m) , 5.61-5.78 (IH, a), 6.85-6,93 (2H, m) , 7.02-7.14 (8H, m) , 7.16 (IH, d, J=8Hz), 7.18-7.30 (3H, m) , 7.48 (IH, d, J=8Hz) , 7.65 (IH, d, J=8Hz), 8.05 (1 x 1/3H, d, J=8Hz) , 8.17 (1 κ /16981 - 559 - 2/3H, d, J=8Hz), 8.93 (IH, t, J=8Hz) (21) NMR (CDC1 3 , δ) : 2.20-2.30 (1 x 1/2H, m) , 2.52-2.62 (1 x 1/2H, m) , 2.83 (3 x 2/3H, m) , 2.94-2.99 (IH, m) , 3.00 (3 x 1/3H, s) , 3.42-3.95 (3K, m) , 4.13- 4.70 (2H, m) , 5.26 (IH, t, J=8Hz) , 6.83-6.88 (2H, a), 7.02-7.38 (15H, m) , 7.52 (1 x 1/2H, d, J=8Hz), 7.60 (1 x 1/2H, d, J=8Hz), 7.80 (1 x 1/2H, d, J=8Hz), 8.00 (1 x 1/2H, s) , 9.04 (1 x 1/2H, s), 9.22 (1 x 1/2H, s) (22) MASS (FAB) (m/z) : 672 (M+H) + NMR (CDCI3, δ) : 2.61 (3 x 2/3H, s), 2.67-2.80 (IH, m) , 2.80 (3 x 1/3H, s), 2.97-3.04 (2H, ) , 3.22- 3.31 (IH, m) , 3.42-3.62 (6H, m) , 3.70-3.81 (2H, m) , 4.17-4.38 (2 x 2/3H, m) , 4.71 (2 x 1/3H, d, J=15Hz), 5.12-5.22 (IH, m) , 5.25-5.30 (IH, m) , 6.57 (IH, d, J=8Hz), 6.65 (IH, t, J=8Hz) , 6.95-7.05 (4H, m) , 7.10-7.14 (6H, m) , 7.23-7.28 (3H, a), 7.42-7.49 (2H, m) , 7.67 (IH, d, J=8Hz) , 8.01-8.10 (2H, m) , 8.18 (IH, d, J=5Hz) (23) MASS (FAB) (m/z) : 639 (M+H) + NMR (CDC1 3 , δ) : 2.38-2.51 (6H, m) , 2.61 (3 x 2/3H, s), 2.63-2.73 (IH, a), 2.82 (3 x 1/3H, s), 2.98- 3.06 (2H, m) , 3.18-3.28 (IH, m) , 3.40-3.48 (2K, m) , 3.60-3.70 (4H, a), 4.16-4.39 (2 x 2/3H, m) , 4.70 (2 x 1/3H, d, J=15Hz), 5.11-5.23 (2H, m) , 6.96-7.13 (9H, a), 7.22-7.28 (4H, a), 7.43 (IH, d, J=8Hz) , 7.65 (IH, d, J=8Hz) , 7.97-8.09 (2H, m) (24) MASS (FAB) (m/z) : 554 (M+H) + NMR (CDCI3, δ) : 2.60 (3 x 2/3H, s) , 2.56-2.70 (IH, m) , 2.82 (3 x 1/3H, s), 2.95 (6H, s), 3.00-3.06 (2H, a), 3.24 (IH, t, J=15Hz) , 4.19-4.39 (2 x 2/3H, /16981 - 560 - m) , 4.68 (2 x 1/3H, d, J=15Hz) , 5.09-5.20 (2H, a), 6.93-7.05 (3H, a), 7.08-7.16 (6H, a), 7.23-7.30 (4H, a), 7.43 (IH, d, J=8Hz) , 7.63 (IH, d, J=8Hz) , 7.99 (IH, t, J=8Hz), 8.17-8.25 (IH, m) (25) MASS (FAB) (m/z) : 671 (M+H) + NMR (CDC1 3 , δ) : 2.62 (3 x 2/3H, s) , 2.65-2.81 (IK, a), 2.82 (3 x 1/3H, s) , 3.02 (2H, t, J=8Kz), 3.08- 3.20 (4H, m) , 3.22-3.38 (IH, m) , 3.50-3.65 (2H, m) , 3.70-3.82 (2H, a), 4.16-4.39 (2 x 2/3H, m) , 4.69 (2 x 1/3H, d, J=15Hz), 5.11-5.20 (IH, m) , 5.21-5.28 (IH, m) , 6.89 (3H, t, J=8Hz) , 6.95-7.13 (9H, a), 7.22-7.31 (6H, m) , 7.45 (IH, d, J=8Hz) , 7.66 (IH, d, J=8Hz), 7.98-8.11 (2H, m) (26) MASS (FAB) (m/z) : 596 (M+H) + NMR (CDCI3, δ) : 2.55-2.67 (IH, m) , 2.61 (3 κ 2/3H, s), 2.79 (3 x 1/3H, s), 2.92-3.09 (2H, m) , 3.21- 3.48 (3H, a), 3.62-3.68 (6H, a), 4.15-4.42 (2 x 2/3H, m) , 4.65 (2 x 1/3H, d, J=15Hz) , 5.11- 5.23 (2H, m) , 6.96-7.37 (13H, m) , 7.75-7.93 (3H, m) , 8.07 (IH, d, J=8Hz) (27) MASS (FAB) (m/z) : 624 (M+H) + NMR (CDC1 3 ^ δ) : 1.87-2.03 (2H, m) , 2.35 (3H, s) , 2.57-2.72 (5H, m) , 2.60 (3 κ 2/3H, s) , 2.80 (3 x 1/3H, s), 3.00-3.12 (2H, m) , 3.32 (IH, t, J=15Hz), 3.47-3.76 (4H, a), 4.10-4.37 (2 x 2/3H, m) , 4.65 (2 x 1/3H, dd, J=15, 8Hz) , 5.02-5.18 (2H, m) , 6.92-7.08 (2H, a), 7.13-7.21 (5H, m) , 7.23-7.32 (4H, m) , 7.45 (IH, t, J=8Hz) , 7.52 (IH, s), 7.58 (IH, d, J=8HZ), 7.69 (IH, d, J=8Hz), 7.72-7.83 (IH, m) , 8.27-8.33 (IH, m) (28) MASS (FAB) (m/z) : 678 (M+H) + MR ( CDCA3,' δ) : i i ι 0 U 0 U - i l- J ~ Ω 0 / ( ςHμ, m -, ) . , .68 (2H, a ) , 1.72-1.87 ( 4H, m) , 2.50-2.61 (4H, a ) , 2.58 < 3 * 2/3H, s ) , 2.67 (IH, dd, J=15, 7 H z ) , 2.80 < 3 * 1/3H, s ) , 2.99-3.11 (2H, m) , 3.32 ( IH, t J=8Hz ) , 3.40-3.55 ( 2H, m) , 3.61-3.70 ( 2H, m ; , ' 4 12- 4-38 ( 2 x 2/3H, m), 4.67 (2 x 1/3H, d, J=8Hz ) , 5.02-5.18 ( 2H, m ) , 6.95-7.08 (2K, a), 7.13-7 20 ( 5H, a ) , 7.25-7.33 (4H, m) , 7.45 (IH, s ) , 7.51 ( IK s ) > 7.58 ( IH, d, J=8Hz), 7.64-7.73 (2K, a ) , 8 22- ' 8.28 (IH, a) ( 29 ) MASS ( FAB) (m/z) : 638 ( M+H ) + NM* ( CDC1 3 , δ ) : 0.90 (3K, t, J=8Hz) , 1.51 ( 2K, q, J=8Hz ) , 2.32 ( 2H, t, J=8Hz) , 2.38-2.52 ( 4H, m ) , 2-62 ( 3 x 2/3H, s ) , 2.68 (IH, dd, J=15, 7Hz ) , 2.83 < 3 x 1/3H, s ) , 3.02-3.12 (2H, m) , 3.31 ( IH, t, J=8Hz ) , 3.43-3.58 (2H, m) , 3.65-3.71 ( 2n, x . 12 - 4.40 ( 2 x 2/3H, m ) , 4.67 (2 x 1/3H, d, J=15Hz ) , 5.02-5.18 ( 2H, m ) , 6.93-7.08 (2H, m) , 7.14-7.20 ( 5H, m ) , 7.23-7.32 (4H, m) , 7.43 (IH, t, J=8Hz ) , 7.50 ( IH, s ) , 7.58 (IH, d, J=8Hz) , 7.63-7.73 ( 2H, a ) , 8.20-8.26 (IH, m) ( 30 ) MASS ( FAB) (m/z) : 674 ( M+H ) + N R ( CDCI3, δ ) : 2.53 (3 x 2/3H, s) , 2.72 ( IH, dd, J=15, 7Hz ) , 2.79 ( 3 x 1/3H, s) , 2.97-3.12 ( 2H, m ) , -36 ( IH, t, J=15Hz), 3.48-3.62 (2H, m ) , 3.68-3.75 ( 2H, m) , 3.79-3.99 (4H, m) , 4.II-4.40 ( 2 x 2/3H, m ) , 4.63 (2 x 1/3H, d, J=15Hz ) , 5.07-5.19 ( 2H, m ) , 6.53 (IH, t, J=5Hz) , 6.97-7.08 ( 2H, m ) , 7.12-7.20 (5H, m) , 7.23-7.31 ( 4H, m ) , -42 ( IH, t, J=8Hz), 7.48 (IH, s) , 7.57 ( lH, d, J=8Hz ) , 7.62-7.73 (2H, m) , 8.23 (IH, d, J=8Hz ) ,' 8.32 (2H, d, J=8Hz) 6/16981 - 562 - (31) MASS (FAB) (m/z) : 521 (M + +l) NMR (CDC1 3 , δ) : 1.21 (3H, t, J=7Hz) , 2.57 (IH, dd, J=7, 16Hz), 3.08 (2H, a), 3.23 (IH, dd, J=4, 16Hz) , 3.38-3.52 (2H, m) , 3.62-3.70 (6H, a), 4.13 (2H, q, J=7Hz), 4.77 (IH, q, J=7Hz) , 5.08 (IH, a) , 6.92 (IH, d, J=2Hz), 7.13 (5H, s), 7.31 (IH, t, J=8Hz) , 7.43 (IH, d, J=8Hz), 7.54 (IH, d, J=8Hz) , 7.67 (IH, d, J=8Hz), 8.07 (IH, d, J=7Hz) , 9.38 (IH, br s) Example 5 The following object compound was obtained according to a similar manner to that of Preparation 13. MASS : (FAB) (m/z) : 493 (M + +l) NMR (DMSO-d 6 , δ) : 2.78 (2H, m) , 2.94 (IH, m) , 3.04 (IH, a), 3.37-3.58 (8H, m) , 4.47 (IH, m) , 4.94 (IH, q, J=7Hz), 7.02-7.09 (3H, m) , 7.14-7.22 (5H, m) , 7.45 (IH, d, J=8Hz), 7.64 (IH, d, J=8Hz) , 7.95 (IH, d, J=8Hz), 8.58 (IH, d, J=7Hz) Example 6 The following object compound was obtained according to a similar manner to that of Preparation 10. mp : 245-250 β C NMR (DMS0-d 6 , δ) : 2.42-2.60 (IH, m) , 2.71 (3 x 1/3H, s), 2.77 (3 x 2/3H, s) , 2.81-2.93 (IK, a), 2.95- 3.03 (IH, m) , 3.40-3.48 (IH, m) , 4.32 (2 x 1/3H, d, J=15Hz), 4.43-4.57 (2 x 2/3H, m) , 4.68-4.77 (IH, a), 4.84-5.00 (IH, a), 6.98-7.36 (11H, a), 7.47 (IH, t, J=8Hz), 7.54 (IH, s)., 7.68 (IH, d, J=8Hz) , 7.78 (IH, d, J=8Hz), 8.71-8.98 (2H, m) ExamplP 7 The following object compound was obtained according to a similar manner to that of Preparation 10. 6/16981 - 563 - MASS (m/z) : 452 (M + +l) NMR (CDC1 3 , δ) : 1.13 (3H, t, J=7H∑) , 2.82 (2H, m) , 3.02 (2H, m) , 4.07 (2H, q, J=7Hz) , 4.84 (IH, q, J=7Hz), 5.25 (IH, m) , 6.88-7.10 (7H, m) , 7.22 (IH, d, J=8HZ), 7.34 (IH, d, J=8Hz) , 7.55 (IH, d, J=8Hz), 7.69 (IH, br s) , 7.87 (IH, br s) Example 8 Starting Compound (496 mg) was dissolved in dichloromethane (1 ml) and cooled to 0 β C. Trifluoroacetic acid (1 ml) was added to the solution and the mixture was stirred at 0"C for 3 hours. The reaction mixture was made basic with ice cooling by adding aqueous sodium hydroxide, and extracted three times with chloroform. The organic layer was washed with brine and dried over magnesium sulfate. Evaporation of the solvent gave Compound A as white solid. lH-Indole-2-carboxylic acid (75 mg) was dissolved in tetrahydrofuran (2 ml) and cooled to -15 β C. N-Methyl- morpholine (0.05 ml) and isobutyl chloroformate (73 mg) were added to the solution and stirred for 5 minutes. Compound A obtained above was dissolved in tetrahydrofuran (2.5 ml), added to the solution at -15 β C, and stirred at 0°C for 30 minutes. The reaction mixture was diluted with chloroform, washed with aqueous sodium hydrogen carbonate, washed with brine, and dried over magnesium sulfate. Evaporation of the solvent followed by column chromatography (silica gel, chloroform-methanol) afforded Object Compound (66 mg) as white powder. MASS (m/z) : 740 (M+H) + NMR (CDCI3, δ) : 2.36 (3H, s) , 2.55-2.72 (IK, m) , 2.80 (1/3 x 3H, s), 2.82-3.05 (2H, m) , 2.90 (2/3 x 3K, s), 3.20-3.35 (IH, m) , 3.35-3.73 (8H, m) , 4.20 (2/3 x IH, d, J=15Hz), 4.53 (1/3 x 2H, ABq, Δ=0.12, J=17Hz), 4.63 (2/3 x IH, d, J=17Hz) , 5.00-5.22 (2H, m) , 7.00-8.10 (18H, a), 9.65 (1/3 x IH, s) , 9 . 68 ( 2 / 3 x IH, s ) Eκamole 9 The following object compounds were obtained according to a similar manner to that of Example 8. (1) MASS (m/z) : 582 (M+H) + NMR (CDC1 3 , δ) : 2.67-2.75 (IH, m) , 3.02-3.15 (2H, m) , 3.20-3.30 (IH, m) , 3.30-3.50 (4H, m) , 3.50-3.65 (4H, m) , 4.29-4.51 (2H, m) , 4.65-4.75 (IH, m) , 4.85-4.92 (IH, m) , 6.80-7.43 (16H, m) , 7.63-7.75 (2H, m) , 8.97 (IH, br s) (2) MASS (m/z) : 492 (M+H) ÷ NMR (DMSO-d 6 , δ) : 2.67-2.92 (3H, a), 3.00-3.09 (IH, a), 3.38-3.60 (8H, a), 4.32-4.41 (IH, a), 4.82-4.92 (IH, a), 6.98-7.24 (10H, m) , 7.38 (IH, br s) , 7.47 (IH, d, J=8Hz) , 7.65 (IH, d, J=8Hz) , 8.00 (IH, d, J=8Hz), 8.58 (IH, d, J=8Hz) (3) MASS (m/z) : 506 (M+H) + NMR (CDCI3, δ) : 2.60-2.72 (IH, m) , 2.80 (2/3 x 3H, s), 2.92 (1/3 x 3H, s) , 3.28-3.78 (10H, a), 4.03- 4.15 (2H, a), 4.40 (1/3 x 2H, s) , 4.53 (2/3 x 2H, ABq, Δ=0.05, J=15Hz) , 5.10-5.23 (IH, a) , 7.00-8.23 (11H, a), 9.18 (1/3 x IH, br s), 9.22 (2/3 x IH, br s) (4) MASS (a/z) : 626 (M+H) + NMR (CDCI3, δ) : 2.62 (2/3 x 3H, s), 2.6-2.7 (IH, a) , 2.79 (1/3 x 3H, s), 3.0-3.1 (2H, a ) , 3.2-3.3 (IH, m) , 3.4-3.7 (8H, m) , 3.78 (3H, s) , 4.03 (1/3 x IH, d, J=17Hz), 4.23 (2/3 x IH, d, J=15Hz) , 4.34 (1/3 x IH, d, J=17Hz), 4.58 (2/3 x IH, d, J=15Hz) , 5.1-5.2 (2H, m) , 6.8-7.0 (4H, m) , 7.1-7.2 (7H, m) , 7.3-7.4 (IH, a), 7.44 (IH, d, J=9Hz), 7.63 (IH, d, J=9Hz), 7.72 (1/3 x IH, d, J=9Hz), 7.76 (2/3 x IH, a, J=9Hz), 8.05 (IH, d, J=9Hz), 9.35 (1/3 x IH, br s), 9.39 (2/3 κ IH, br s) (5) MASS (a/z) : 582 (M+H) + NMR (CDC1 3 , δ) : 2.63 (IH, dd, J=15, 7Hz), 2.76 (2/3 κ 3K, s), 2.82 (1/3 x 3H, s) , 3.23 (IK, dd, J=I5, 3HZ), 3.4-3.7 (8H, a), 4.28 (1/3 x IK, d, J=16Hz), 4.42 (2/3 x IH, d, J=14Hz) , 4.55 (1/3 x IH, d, J=16Hz), 4.70 (2/3 κ IH, d, J=14Hz) , 5.1-5.2 (IH, a), 5.78 (2/3 κ IH, d, J=7Hz), 5.80 (1/3 κ IH, d, J=7Hz), 6.9-7.4 (14H, a), 7.62 (IH, d, J=7Hz) , 8.07 (IH, d, J=7Hz), 8.35 (IH, d, J=7Hz) , 9.33 (IK, br s) (6) MASS (a/z) : 702 (M+H) + NMR (CDCI3, δ) : 2.52-2.78 (IH, m) , 2.67 (2/3 x 3H, s), 2.85 (1/3 x 3H, s), 2.88-3.05 (2H, m) , 3.12- 3.30 (IH, m) , 3.32-3.75 (8H, m) , 4.28 (2/3 x IH, d, J=15HZ), 4.33 (1/3 x 2H, ABq, J=17HZ) , 4.68 (2/3 x IH, d, J=15Hz), 4.82 (2H, s), 5.02-5.23 (2H, m) , 6.62-8.15 (21H, m) , 9.83 (1/3 x IH, s), 9.87 (2/3 κ IH, s) (7) MASS (m/z) : 715 (M+H) + NMR (CDCI3, δ) : 2.28 (3H, s), 2.28-2.52 (4H, m) , 2.52-2.71 (IH, m) , 2.64 (2/3 κ 3H, s), 2.82 (1/3 κ 3H, s), 2.88-3.00 (2H, m) , 3.20-3.38 (IH, m) , 3.38- 3.75 (4H, m) , 4.28 (2/3 x IH, d, J=15Hz), 4.32 (1/3 x 2H, ABq, Δ=0.16, J=17Hz) , 4.67 (2/3 x IH, d, J=15Hz), 4.85 (2H, s), 4.98-5.18 (2H, a), 6.65-8.15 (21H, a), 9.42 (1/3 x IH, s), 9.46 (2/3 κ IH, s) (8) MASS (a/z) : 612 (M+H) + NMR (CDCI3, δ) : 2.59-2.78 (IH, m) , 2.74 (2/3 κ 3K, s), 2.80-2.98 (2H, m) , 2.83 (1/3 κ 3H, s), 3.10- 3.25 (IH, m) , 3.30-3.70 (8H, a), 4.32 (2/3 κ IH, d, J=15Hz), 4.41 (1/3 κ 2H, ABq, J=17HZ) , 4.67 (2/3 x IH, d, J=15Hz), 5.02-5.25 (2H, a), 6.47-8.13 (17H, a) , 9.95 (IH, s) (9) MASS (a/z) : 610 (M+H) + NMR (CDC1 3 , δ) : 2.45-2.85 (4H, a), 2.64 (3/5 x 3H, s), 2.84 (2/5 κ 3H, s), 2.90-3.02 (2H, a), 3.18- 3.40 (2H, m) , 3.40-3.78 (8H, m) , 4.91-5.19 (2H, m) , 6.93-8.10 (17H, m) , 9.50 (2/5 κ IH, s), 9.52 (3/5 x IH, s) (10) MASS (m/z) : 654 (M+H) + NMR (CDCI3, δ) : 2.5-2.7 (IH, m) , 2.65 (2/3 x 3H, s), 2.80 (1/3 x 3H, s), 3.0-3.1 (2H, m) , 3.2-3.3 (IH, m) , 3.4-3.7 (8H, m) , 3.92 (3H, s) , 4.35 (2/3 x IH, d, J=15Hz), 4.43 (1/3 κ IH, d, J=15Hz) , 4.65 (1/3 κ IH, d, J=15Hz), 4.68 (2/3 κ IH, d, J=15Hz) , 4.8-5.2 (2H, m) , 6.9-7.5 (11H, m) , 7.6-8.1 (5H, m) , 9.19 (1/3 x IH, br s), 9.37 (2/3 x IH, br s) (11) MASS (m/z) : 646 (M+H) + NMR (CDCI3, δ) : 2.5-2.7 (IH, m) , 2.68 (2/3 κ 3H, s), 2.88 (1/3 x 3H, s), 3.0-3.1 (2H, m) , 3.1-3.3 (IH, m) , 3.3-3.7 (8H, m) , 4.30 (1/3 x IH, d, J=17Hz), 4.48 (2/3 x IH, d, J=15Hz), 4.56 (1/3 x IH, d, J=17Hz), 4.80 (2/3 κ IH, d, J=15Hz) , 5.0-5.2 (2H, m) , 6.9-7.9 (18H, m) , 8.08 (IH, d, J=9Hz), 9.47 (1/3 x IH, br s) , 9.50 (2/3 x IH, br s) (12) MASS (m/z) : 646 (M+H) + NMR {CDCI3, δ) : 2.40-2.65 (IH, m) , 2.60 (2/3 x 3H, s), 2.94 (1/3 x 3H, s), 2.95-3.10 (2H, m) , 3.20- 3.80 (9H, m) , 4.74 (1/3 x 2H, ABq, Δ=0.10, J=17Hz) , 6/16981 - 567 - 4.77 (2/3 x IH, d, J=15H∑), 4.88-5.20 (2H, aj , 5.22 (2/3 x IH, d, J=15Hz), 6.93-8.15 (19H, a), 9.23 (1/3 x IH, s), 9.35 (2/3 x IH, s) (13) MASS (m/z) : 612 (M+H) + NMR (CDC1 3 , δ) : 2.55-2.68 (IH, m) , 2.59 (2/3 x 3H, S), 2.72 (1/3 x 3H, s), 2.95-3.08 (2H, m ), 3.15- 3.70 (9H, m) , 3.75 (1/3 x IH, d, J=17Hz) , 4.30 (1/3 x IH, d, J=17Hz), 4.35 (2/3 x 2H, ABq, J=15Hz), 4.83-5.20 (2H, a), 6.65-8.35 (17H, a), 9.72 (IH, s) (14) MASS (m/z) : 613 (M+H) + NMR (CDCI3, δ) : 2.55-2.75 (IH, m) , 2.59 (2/3 x 3K, s) , 2.75 (1/3 x 3H, s) , 2.95-3.15 (2H, m) , 3.20- 3.75 (9H, m) , 3.84 (1/3 x IH, d, J=17Hz) , 4.30 (1/3 x IH, d, J=17Hz), 4.38 (2/3 x 2H, ABq, J=15Hz), 4.82-5.23 (2H, m) , 6.68-8.30 (17H, m) (15) MASS (m/z) : 638 (M + ) NMR (CDC1 3 , δ) : 2.60 (2/3 x 3H, s) , 2.6-2.7 (IH, a), 2.80 (1/3 x 3H, s), 2.92 (6H, s) , 3.0-3.1 (2H, a), 3.2-3.3 (IH, m), 3.4-3.7 (8H, m) , 3.98 (1/3 x IH, d, J=17Hz), 4.22 (2/3 x IH, d, J=15Hz) , 4.34 (1/3 x IH, d, J=17Hz), 4.58 (2/3 x IH, d, J=15Hz) , 5.0-5.2 (IH, m) , 6.63 (2H, d, J=8Hz) , 6.91 (1/3 x 2H, d, J=8Hz), 7.00 (2/3 x 2H, d, J=8Hz) , 7.1-7.2 (7H, m) , 7.2-7.3 (IH, m) , 7.43 (IH, d, J=7Hz) , 7.67 (IH, d, J=7Hz), 7.80 (1/3 x IH, d, J=8Hz) , 7.85 (2/3 x IH, d, J=8Hz), 8.05 (IH, d, J=8Hz) , 9.50 (1/3 x IH, br s) , 9.57 (2/3 x IH, br s) (16) MASS (m/z) : 597 (M+H) + NMR (CDCI3, δ) : 2.55-2.72 (IH, m) , 2.80 (2/3 x 3K, s), 2.90 (1/3 x 3H, s), 2.95-3.32 (3H, m) , 3.37- 3.74 (8H, m) , 4.43 (1/3 x 2H, ABq, Δ=0.05, J=17Hz) , 4.48 (2/3 x IK, d, J=15Hz) , 4.70 (2/3 x IH, d, J=15Hz), 5.07-5.21 (2H, m) , 6.93-8.10 (15H, m) , 8.45-8.55 (IH, m) , 9.63 (1/3 x IH, s) , 9.65 (2/3 x IH, s) (17) MASS (m/z) : 597 (M+H) + NMR (CDC1 3 , δ) : 2.55-2.72 (IH, ) , 2.70 (3/4 κ 3H, s), 2.82 (1/4 κ 3H, s), 2.90-3.15 (2H, m) , 3.18- 3.34 (IH, m) , 3.38-3.78 (8H, m) , 4.28 (1/4 κ 2H, ABq, Δ=0.05, J=17Hz), 4.31 (3/4 κ IH, d, J=15Hz) , 4.58 (3/4 κ IH, d, J=15Hz) , 4.93-5.22 (2H, m) , 6.75-8.10 (14H, m) , 8.43-8.51 (2H, m) , 9.58 (IH, s) (18) MASS (FAB) (m/z) : 668 (M+H) + NMR (CDCI3, δ) : 2.23 (3H, s) , 2.30-2.46 (4H, m) , 2.58-2.69 (IH, m) , 2.58 (3 x 2/3H, s), 2.73 (3 x 1/3H, s), 2.92-3.10 (2H, m) , 3.23-3.33 (IH, m) , 3.38-3.52 (2H, a), 3.60-3.67 (2H, a), 3.88 (3H, s) , 4.20-4.35 (2 x 2/3H, a), 4.66 (2 x 1/3H, d, J=15Hz), 5.01-5.18 (2H, m) , 6.95 (2 x 1/3H, d, J=8Hz), 7.03 (2 x 2/3H, d, J=8Hz) , 7.10-7.20 (5H, a), 7.26 (IH, t, J=8Hz) , 7.38 (IH, t, J=8Hz) , 7.47 (IH, s), 7.52 (IH, d, J=8Hz), 7.65 (IH, d, J=8Hz), 7.73 (IH, d, J=8Hz), 7.90 (2H, d, J=8Hz) , 8.19 (IH, t, J=8Hz) (19) MASS (FAB) (m/z) : 655 (M+H) + NMR (CDCI3, δ) : 2.58-2.70 (IH, m) , 2.67 (3 x 2/3H, s), 2.80 (3 x 1/3H, s) , 2.98-3.13 (2H, m) , 3.31 (IH, t, J=15Hz), 3.40-3.57 (2H, m) , 3.63-3.77 (6H, a), 3.91 (3H, s), 4.20-4.40 (2 x 2/3H, a), 4.70 (2 x 1/3H, d, J=15Hz), 5.03-5.18 (2H, m) , 6.99 (2 x 1/3H, d, J=8Hz), 7.09 (2 x 2/3H, d, J=8Hz) , 7.13- 7.23 (6H, m) , 7.31 (IH, t, J=8Hz) , 7.44 (IH, t. 6/16981 - 569 - J=8Hz), 7.51 (IH, s), 7.61 (IH, t, J=8Hz) , 7.70 (IH, d, J=8Hz), 7.93 (2H, d, J=8Hz) , 8.20 (IH, t, J=8Hz) Example 10 The following object compounds were obtained according to a similar manner to that of Example 1. (1) MASS (m/z) : 595 (M+H) + NMR (CDC1 3 , δ) : 2.25-2.45 (4H, m) , 2.27 (3H, s), 2.60-2.75 (IH, m) , 2.80 (2/3 x 3H, s), 2.85 (1/3 x 3H, s), 3.17-3.75 (5H, a), 4.29 (1/3 x IH, d, J=17Hz), 4.43 (1/3 x IH, d, J=17Hz) , 4.57 (2/3 x IH, d, J=15Hz), 4.72 (2/3 x IH, d, J=15Hz) , 5.05- 5.20 (IH, m), 5.70-5.87 (lH m), 6.75-7.48 (14H, m) , 7.58-7.70 (IH, m) , 7.98-8.18 (IH, m) , 8.35-8.45 (IH, m) , 9.42 (IH, br s) (2) MASS (m/z) : 596 (M+H) + NMR (CDCI3, δ) : 2.27 (3H, s) , 2.30-2.48 (4H, a), 2.65-2.80 (IH, m) , 2.81 (2/3 x 3H, s) , 2.85 (1/3 x 3H, s), 3.20-3.70 (5H, m) , 4.30 (1/3 x IH, d, J=17Hz), 4.45 (2/3 x IH, d, J=15Hz) , 4.58 (1/3 x IH, d, J=17Hz), 4.72 (2/3 x IH, d, J=17Hz), 5.04- 5.18 (IH, m), 5.77-5.88 (IH, m) , 6.80-7.70 (15H, m) , 8.12-8.50 (2H, m) (3) MASS (m/z) : 651 (M+H) + NMR (CDCI3, δ) : 2.28-2.52 (4H, a), 2.29 (3H, s), 2.55-2.72 (IH, m) , 2.58 (2/3 x 3H, s), 2.78 (1/3 x 3H, s), 2.92 (6H, s) , 2.95-3.10 (2H, m) , 3.22-3.78 (5H, m) , 3.98 (1/3 x IH, d, J=17Hz) , 4.20 (2/3 x IH, d, J=15Hz), 4.31 (1/3 x IH, d, J=17Hz) , 4.57 (2/3 x IH, d, J=15Hz), 5.02-5.25 (2H, m) , 6.47-8.12 (16H, m) , 9.25-9.58 (IH, br s) (4) MASS (m/z) : 652 (M+H) + NMR (CDC1 3 , δ) : 2.30 (3H, s) , 2.32-2.52 (4H, a) , 2.58 (2/3 x 3H, s), 2.60-2.72 (IH, a), 2.78 (1/3 x 3H, s), 2.92 (6H, s), 2.96-3.10 (2H, m) , 3.25-3.72 (5H, m) , 3.98 (1/3 κ IH, d, J=17Hz) , 4.21 (2/3 κ IH, d, J=15Hz), 4.30 (1/3 x IH, d, J=l7Hz), 4.54 (2/3 x IH, d, J=15Hz) , 5.02-5.25 (2H, a) , 6.58-7.75 (15H, a) , 8.15-8.28 (IH, a) (5) MASS (a/z) : 666 (M+H) + NMR (CDCI3, δ) : 2.22 (6H, s), 2.29 (3H, s), 2.30-2.52 (4H, a), 2.55-2.70 (IH, m) , 2.62 (2/3 κ 3H, s), 2.82 (1/3 κ 3H, s), 2.95-3.08 (2H, a), 3.22-3.78 (7H, a), 4.24 (1/3 x 2H, ABq, Δ=0.21, J=17Hz) , 4.29 (2/3 x IH, d, J=15Hz), 4.62 (2/3 x IH, d, J=15Hz) , 5.00-5.19 (2H, m) , 6.90-8.13 (16H, a), 9.35 (1/3 x IH, s) , 9.42 (2/3 κ IH, s) (6). MASS (m/z) : 667 (M+H) + NMR (CDCI3, δ) : 2.22 (6H, s) , 2.30 (3H, s), 2.32-2.53 (4H, m), 2.59 (2/3 x 3H, s) , 2.59-2.72 (IH, m) , 2.80 (1/3 x 3H, s), 2.94-3.12 (2H, a), 3.23-3.72 (7H, m) , 4.22 (1/3 x 2H, ABq, J=17Hz) , 4.27 (2/3 x IH, d, J=l5Hz), 4.63 (2/3 κ IH, d, J=15Hz), 5.00-5.20 (2H, a), 6.88-7.75 (15H, a), 8.15-8.25 (IH, a) (7) MASS (a/z) : 621 (M+H) + NMR (CDCI3, δ) : 2.20-2.50 (4H, a), 2.28 (3K, s), 2.55-2.82 (2H, m) , 2.92-3.85 (10H, m) , ' 3.98 (1/2 x IH, d, J-17HZ), 4.48 (1/2 x IH, d, J=17Hz), 4.62 (1/2 x 2H, ABq, Δ=0.15, J=17Hz) , 5.05-5.23 (2H, m) , 6.80-8.15 (16H, m) , 9.60 (IH, s) (8) MASS (m/z) : 622 (M+H) + 6/16981 - 571 - NMR (CDCI3, δ) : 2.30 (3H, S) , 2.30-2.55 (4H, m) , 2.55-3.82 (12H, m) , 3.94 (2/5 x IH, d, J=17Kz), 4.48 (2/5 x IK, d, J=17Hz) , 4.62 (3/5 x 2H, ABq, J=17Hz), 5.02-5.23 (2H, m) , 6.80-7.82 (15H, m) , 8.15-8.28 (IH, m) (9) MASS (m/z) : 643 (M+H) + NMR (CDCI3, δ) : 2.30 (3H, s) , 2.30-2.53 (4H, m) , 2.58-2.70 (IH, m) , 2.62 (3/4 x 3H, s), 2.78 (1/4 x 3H, s), 2.97-3.10 (2H, m) , 3.24-3.78 (5H, m) , 4.20 (1/4 κ 2H, ABq, Δ=0.16, J=17Hz) , 4.25 (3/4 κ IH, d, J=15Hz), 4.60 (3/4 x IH, d, J=15Hz) , 5.02-5.17 (2H, m) , 6.80-8.13 (16H, m) , 9.33 (IH, br s) (10) MASS (m/z) : 644 (M+H) + NMR (CDCI3, δ) : 2.30 (3H, s) , 2.30-2.52 (4H, m) , 2.60 (3/4 x 3H, s), 2.60-2.72 (IH, m) , 2.78 (1/4 x 3H, s), 2.95-3.15 (2H, m) , 3.25-3.74 (5H, m) , 4.19 (1/4 x 2H, ABq, J=17Hz) , 4.24 (3/4 x IH, d, J=15Hz), 4.59 (3/4 x IH, d, J=15Hz) , 5.02-5.18 (2H, m) , 6.80-7.01 (2H, m) , 7.17-7.74 (13H, m) , 8.13- 8.28 (IH, m) (11) MASS (m/z) : 687, 689 (M+H) + NMR (CDC1 3 , δ) : 2.25-2.52 (4H, m) , 2.30 (3H, s), 2.55-2.70 (IH, a), 2.62 (3/4 x 3H, s), 2.77 (1/4 x 3H, s), 2.92-3.12 (2H, a), 3.22-3.38 (IH, a), 3.40- 3.78 (4H, a), 4.20 (1/4 x 2H, ABq, Δ=0.15, J=17HZ) , 4.23 (3/4 x IH, d, J=15Hz) , 4.59 (3/4 x IH, d, J=15Hz), 5.03-5.18 (2H, a), 6.73-8.12 (16H, a), 9.43 (IH, br s) (12) MASS (m/z) : 688, 690 (M+H) + NMR (CDCI3, δ) : 2.30 (3H, s) , 2.30-2.52 (4H, m) , 2.60-2.71 (IH, m) , 2.62 (3/4 x 3H, s), 2.78 (1/4 x 3H, s), 2.95-3.17 (2H, a), 3.26-3.75 (5H, m> , 4.17 (1/4 x 2H, ABq, Δ=0.14, J=17Hz) , 4.22 (3/4 x IH, d, J=15Hz), 4.58 (3/4 κ IH, d, J=15Hz) , 5.02-5.18 (2H, a), 6.72-6.96 (2H, m) , 7.10-7.72 (13H, a), 8.15- 8.27 (IH, m) (13) MASS (m/z) : 627 (M+H) + NMR (CDC1 3 , δ) : 2.24-2.50 (4H, m) , 2.28 (3K, s), 2.60 (3/4 x 3H, s), 2.60-2.73 (IH, m) , 2.78 (1/4 x 3H, s), 2.93-3.13 (2H, a), 3.20-3.75 (5H, m) , 4.20 (1/4 x 2H, ABq, Δ=0.17, J=17Hz) , 4.21 (3/4 x IH, d, J=15Hz), 4.61 (3/4 x IH, d, J=15Hz) , 5.06-5.21 (2H, m) , 6.82-8.12 (16H, m) , 9.23 (IH, br s) (14) MASS (m/z) : 628 (M+H) + NMR (CDCI3, δ) : 2.30 (3H, s) , 2.32-2.55 (4H, a), 2.59 (3/4 x 3H, s), 2.60-2.72 (IH, m) , 2.78 (1/4 x 3H, s), 2.95-3.17 (2H, m) , 3.26-3.75 (5H, m) , 4.18 (1/4 x 2H, ABq, Δ=0.20, J=17Hz) , 4.23 (3/4 x IH, d, J=15Hz), 4.59 (3/4 x IH, d, J=15Hz) , 5.00-5.18 (2H, m) , 6.82-7.73 (15H, m) , 8.15-8.27 (IH, m) (15) MASS (m/z) : 640 (M+H) + NMR (CDCI3, δ) : 2.30 (3H, s), 2.30-2.58 (4H, m) , 2.59 (3/4 x 3H, s), 2.60-2.70 (IH, m) , 2.73 (1/4 x 3H, s), 2.98-3.15 (2H, m) , 3.20-3.35 (IH, a), 3.40-3.75 (4H, a), 3.92 (3H, s) , 3.95 (1/4 x IH, d, J=17Hz) , 4.21 (3/4 x IH, d, J=15Hz), 4.26 (1/4 x IH, d, J=17Hz), 4.50 (3/4 x IH, d, J=15Hz) , 5.02-5.25 (2H, a), 6.58-6.68 (IH, a), 6.95-8.13 (14H, a), 9.73 (1/4 x IH, br s), 9.78 (3/4 κ IH, br s) (16) MASS (m/z) : 641 (M+H) + NMR (CDC1 3 , δ) : 2.30 (3H, s) , 2.35-2.52 (4H, m) , 2.58 (3/4 x 3H, s), 2.60-2.72 (IH, m) , 2.73 (1/4 x 3H, 6/16981 - 573 - s), 2.98-3.16 (2H, a), 3.28-3.40 (IH, m) , 3.40-3.75 (4H, m) , 3.92 (3H, s), 3.95 (1/4 x IH, d, =17Hz) , 4.20 (3/4 x IH, d, J=15Hz), 4.26 (1/4 x IH, d, J=17Hz), 4.52 (3/4 x IH, d, J=15Hz) , 5.00-5.25 (2H, m) , 6.60-6.70 (IH, m) , 7.03-8.25 (14H, m) (17) MASS (m/z) : 657 (M+H) + NMR (CDC1 3 , δ) : 2.30 (3H, s) , 2.33-2.56 (4H, a,, 2.56-2.68 (IH, m) , 2.60 (3/4 x 3H, s), 2.75 (1/4 x 3H, s), 2.98-3.15 (2H, m) , 3.25-3.42 (IH, m) , 3.42- 3.73 (4H, m) , 3.91 (3H, s) , 3.94 (1/4 x IH, d, J=17Hz), 4.23 (3/4 x IH, d, J=15Hz) , 4.28 (1/4 x IH, d, J=17Hz), 4.52 (3/4 x IH, d, J=15Hz) , 4.98- 5.21 (2H, m) , 6.60-6.70 (IH, m) , 7.05-8.18 (14H, m) (18) MASS (m/z) : 623 (M+H) + NMR (CDC1 3 , δ) : 0.98 (3/5 x 3H, t, J=7Hz) , 1.01 (2/5 x 3H, t, J=7Hz), 2.25-2.74 (5H, m) , 2.28 (3K, s), 2.92-3.18 (4H, a), 3.22-3.38 (IH, m) , 3.40-3.75 (4H, m) , 4.17 (3/5 x IH, d, J=15Hz) , 4.19 (2/5 x 2H, ABq, Δ=0.18, J=17Hz), 4.84 (3/5 x IH, d, J=15Hz), 5.00-5.20 (2H, m) , 6.95-8.10 (17H, m) , 9.48 (2/5 x IH, br s), 9.53 (3/5 x IH, br s) (19) MASS (m/z) : 624 (M+H) + NMR (CDCI3, δ) : 0.97 (3/5 x 3H, t, J=7Hz) , 1.0C (2/5 x 3H, t, J=7Hz), 2.30 (3H, s) , 2.30-2.72 (5H, m) , 2.93-3.20 (4H, m) , 3.25-3.75 (5H, a), 4.17 (3/5 x IH, d, J=15Hz), 4.17 (2/5 x 2H, ABq, J=17Hz), 4.81 (3/5 x IH, d,. J=15Hz) , 4.97-5.13 (2H, m) , 6.93-7.72 (16H, m) , 8.15-8.27 (IH, m) (20) MASS (m/z) : 644 (M+H) + NMR (CDC1 3 , δ) : 2.28-2.55 (4H, m) , 2.30 (3H, s), 2.60-2.71 (IH, m) , 2.64 (4/5 x 3H, s), 2.74 (1/5 x 3H, s) , 2.93-3.16 (2H, a), 3.21-3.35 (IH, a), 3.40- 3.75 (4H, m) , 4.18 (1/5 κ 2H, ABq, Δ=0.21, J=17HZ) , 4.41 (4/5 κ 2H, ABq, Δ=0.15, J=15Hz) , 5.02-5.17 (2H, m) , 6.95-8.20 (15H, m) , 9.59 (1/5 κ IH, s) , 9.68 (4/5 x IH, s) (21) MASS (m/z) : 645 (M+H) + NMR (CDC1 3 , δ) : 2.30 (3K, s), 2.30-2.52 (4K, m) , 2.58-2.71 (IH, m) , 2.62 (4/5 x 3H, s), 2.73 (1/5 κ 3H, s), 2.96-3.20 (2H, m) , 3.25-3.40 (IH, a), 3.40- 3.73 (4H, a), 4.20 (1/5 κ 2H, ABq, Δ=0.19, J=17HZ) , 4.28 (4/5 κ IH, d, J=15Hz) , 4.54 (4/5 κ IH, d, J=15Hz), 5.02-5.15 (2H, m) , 7.05-7.73 (13H, m) , 8.02-8.25 (2H, m) (22) MASS (m/z) : 661 (M+H) + NMR (CDC1 3 , δ) : 2.30 (3H, s) , 2.30-2.53 (4H, a), 2.53-2.68 (IH, m) , 2.63 (4/5 x 3H, s) , 2.75 (1/5 x 3H, s), 2.95-3.12 (2H, m) , 3.26-3.40 (IH, m) , 3.40- 3.71 (4H, m) , 4.20 (1/5 x 2H, ABq, J=17Hz) , 4.43 (4/5 x 2H, ABq, Δ=0.21, J=15Hz) , 4.98-5.12 (2H, m) , 7.10-8.20 (15H, m) (23) MASS (m/z) : 624 (M+H) + NMR (CDC1 3 , δ) : 2.30 (3H, s) , 2.30-2.50 (4H, a), 2.52 (1/5 x 3H, s) , 2.55 (4/5 x 3H, s) , 2.58-2.70 (IH, a), 2.61 (4/5 x 3H, s) , 2.75 (1/5 κ 3H, s), 2.95-3.12 (2H, m) , 3.23-3.36 (IH, m) , 3.41-3.75 (4H, m) , 4.02 (1/5 x IH, d, J=17Hz) , 4.32 (1/5 x IH, d, J=17Hz), 4.41 (4/5 x 2H, ABq, J=15Hz), 5.00-5.20 (2H, m) , 6.96-8.31 (15H, m) , 9.34 (1/5 x IH, s), 9.61 (4/5 x IH, s) (24) MASS (m/z) : 625 (M+H) + NMR (CDC1 3 , δ) : 2.31 (3H, s) , 2.32-2.50 (4H, a), 2.53 (3H, s), 2.59 (3/4 x 3H, s), 2.60-2.71 (IH, a), 2.73 (1/4 x 3H, s), 2.98-3.15 (2H, a), 3.25-3.73 (5H, m) , 4.01 (1/4 x IH, d, J=17Hz) , 4.27 (3/4 x IH, d, J=15Hz), 4.30 (1/4 x IH, d, J=17Hz) , 4.56 (3/4 x IH, d, J=15Hz), 5.02-5.20 (2H, a), 7.02-7.75 (13H, a), 8.15-8.30 (2H, a) (25) MASS (m/z) : 641 (M+H) + NMR (CDC1 3 , δ) : 2.31 (3H, s), 2.32-2.50 (4H, m) , 2.52 (3H, s), 2.57-2.69 (IH, m) , 2.62 (3/4 κ 3H, s), 2.76 (1/4 x 3K, s), 2.98-3.14 (2H, m) , 3.26-3.72 (5H, m) , 4.02 (1/4 x IH, d, J=17Hz) , 4.30 (3/4 x IH, d, J=15Hz), 4.32 (1/4 x IH, d, J=17Hz), 4.56 (3/4 x IH, d, J=15Hz), 4.99-5.18 (2H, m) , 7.02-8.31 (15H, m) (26) MASS (m/z) : 6.11 (M+H) + NMR (CDC1 3 , δ) : 2.53 (1/4 x 3H, s) , 2.55 (3/4 x 3H, s), 2.60-2.71 (IH, m) , 2.62 (3/4 x 3H, s), 2.76 (1/4 x 3H, s), 2.92-3.15 (2H, m) , 3.18-3.35 (IH, m) , 3.35-3.78 (8H, m) , 4.02 (1/4 x IH, d, J=17Hz), 4.32 (1/4 κ IH, d, J=17Hz) , 4.42 (3/4 κ 2H, ABq, Δ=0.15, J=15Hz), 5.02-5.22 (2H, a), 6.92-8.35 (15H, m) , 9.62 (1/4 x IH, s) , 9.81 (3/4 x IH, s) (27) MASS (m/z) : 612 (M+H) + NMR (CDCI 3 , δ) : 2.52 (3H, s), 2.58-2.70 (IH, a), 2.60 (3/4 x 3H, s), 2.75 (1/4 x 3H, s), 2.95-3.15 (2H, m) , 3.22-3.39 (IH, m) , 3.39-3.80 (8H, m) , 4.00 (1/4 x IH, d, J=17Hz), 4.29 (3/4 X IH, d, J=15Hz) , 4.31 (1/4 x IH, d, J=l7Hz), 4.55 (3/4 x IK, d, J=15Hz) , 5.00-5.20 (2H, m) , 7.00-7.78 (13H, m) , 8.12-8.32 (2H, m) (28) MASS (m/z) : 628 (M+H) + Λ ,„, ΛM _. 96/16981 - 576 - NMR ( CDC1 3 , δ ) : 2.52 (3H, s), 2.55-2.68 ( IH, m ) , 2.62 ( 3/4 x 3H, S) , 2.76 (1/4 x 3H, s ) , 2.95-3.14 ( 2H, a ) , 3.22-3.38 (IH, a), 3.40-3.80 ( 8H, a ) , 4.02 ( 1/4 x IH, d, J=17H Z ), 4.35 (1/4 x IH, d, J=17Hz ) , 4.44 ( 3/4 x 2H, ABq, Δ =0.23, J=15Hz) , 4.98-5.18 ( 2H, m ) , 7.00-8.33 (15H, m) (29) MASS (m/z) : 614 ( M+H )+ NMR ( CDCI3, δ ) : 2.30 (3H, s>, 2.30-2.63 ( 5H, m ) , 2.62 ( 3/4 x 3H, s), 2.82 (1/4 x 3H, s ) . 2.93-3.10 ( 2H, m ) , 3.22-3.40 (IH, m) , 3.40-3.75 ( 4H, m ) , 4.26 ( 1/4 x 2H, ABq, Δ =0.21, J=17Hz) , 4.32 ( 1/4 x IK, d, J-15H Z) , 4.64 (1/4 x IH, d, J=l5Hz ) , 4.93-5.15 ( 2H, m ) , 6.04 (2H, s), 6.80-7.98 ( 15H, a ) (30) MASS (m/z) : 676 ( M+H )+ NMR ( CDCI3. δ) : 2.25-2.50 (4H, m ) , 2.28 ( 3H, s ) , 2.60-2.72 ( IH, a), 2.66 (2/3 x 3H, s ) , 2.80 ( 1/3 x 3H, s ) , 2.92-3.16 (2H, m) , 3.22-3.74 ( 5H, m ) , 4.27 ( 1/3 κ 2H, ABq, .=0.18, J=17Hz ) , 4.49 ( 2/3 κ 2H, ABq, Δ =0.22, J=l5Hz) , 5.05-5.21 ( 2H, m ) , 6.95-7.88 ( 15H, m ) , 8.01-8.13 (2H, a), 8.50 ( 2/3 κ IH, s ) , 8.52 (1/3 x IH, s ) (31) MASS (m/z) : 677 ( M+H )+ NMR ( CDCI3, δ ) : 2.30 (3H, s) , 2.30-2.54 ( 4H, m ) , 2.58-2.75 ( IH, m) , 2.67 (3/4 x 3H, s ) , 2.80 ( 1/4 x 3H, s ) , 2.97-3.21 (2H, m) , 3.28-3.77 ( 5H, m ) , 4.23 ( 1/4 x 2H, ABq, A -0.17, J-17HZ ) , 4.52 ( 3/4 κ 2H, ABq, Δ =0.23, J=l5Hz) , 5.02-5.22 ( 2H, m ) , 7.00-7.75 ( 15H, m ) , 8.10 (3/4 x IH, s), 8.18 ( 1/4 x IH, s ) , 8.20-8.28 ( IH, m) , 8.52 (3/4 x IH, s ) , 8.53 ( 1/4 x IH, s) (32) MASS (m/z) : 693 ( M+H ) + NMR (CDCI3, δ) : 2.31 (3H, s) , 2.31-2.70 (5H, m) , 2.68 (3/4 x 3H, s), 2.81 (1/4 x 3H, s) , 2.97-3.20 (2H, a), 3.25-3.73 (5H, m) , 4.31 (1/4 x 2H, ABq, Δ=0.21, J=17Hz), 4.53 (3/4 x 2H, ABq, Δ=0.18, J=15Hz) , 4.98-5.20 (2H, m) , 7.03-7.94 (15H, m),8.05-8.21 (2H, m) , 8.52 (3/4 x IH, s) , 8.53 (1/4 x IH, s) (33) MASS (m/z) : 644 (M+H) + NMR (CDCI3, δ) : 2.30 (3H, s) , 2.30-2.52 (4H, m) , 2.58-2.70 (IH, m) , 2.63 (4/5 x 3H, s), 2.78 (1/5 x 3H, s), 2.95-3.10 (2H, m) , 3.22-3.75 (5H, a), 4.21 (1/5 x 2H, ABq, Δ=0.24, J=17Hz) , 4.43 (4/5 x 2H, ABq, Δ=0.20, J=15Hz), 5.00-5.15 (2H, m) , 6.93-8.18 (13H, m) , 8.27 (IH, s) , 8.48 (IH, s) , 9.39 (1/5 x IH, s), 9.51 (4/5 x IH, s) (34) MASS (m/z) : 645 (M+H) + NMR (CDCI3, δ) : 2.31 (3H, s) , 2.31-2.52 (4H, m) , 2.60-2.72 (IH, m) , 2.62 (4/5 x 3H, s), 2.78 (1/5 x 3H, s), 2.98-3.17 (2H, m) , 3.25-3.76 (5H, m) , 4.21 (1/5 x 2H, ABq, Δ=0.22, J=17Hz) , 4.30 (2/5 x IH, d, J=15Hz), 4.59 (2/5 x IH, d, J=15Hz) , 5.00-5.18 (2H, a), 7.10-7.85 (12H, a), 8.11-8.31 (2H, m) , 8.48 (IH, s) (35) MASS (m/z) : 661 (M+H) + NMR (CDCI3, δ) : 2.30 (3H, s) , 2.30-2.53 (4H, m) , 2.53-2.72 (IH, m) , 2.65 (3/4 x 3H, s) , 2.79 (1/4 x 3H, s), 2.96-3.16 (2H, m) , 3.25-3.76 (5H, m) , 4.08 (1/4 x IH, d, J=17Hz), 4.32 (3/4 x IH, d, J=15Hz) , 4.34 (1/4 x IH, d, J=17Hz) , 4.58 (3/4 x IH, d, J=15Hz), 4.95-5.12 (2H, m) , 7.10-7.97 (12H, a), 8.05-8.30 (2H, m) , 8.49 (IH, s) (36) MASS (m/z) : 631 (M+H) + NMR (CDCI3, δ) : 2.54-2.70 (IH, m) , 2.66 (4/5 x 3H, s) , 2.73 (1/5 x 3H, s) , 2.91-3.15 (2H, a) , 3.15- 3.32 (IH, a), 3.32-3.76 (8H, a), 4.18 (1/5 x 2H, ABq, Δ=0.24, J=17Hz) , 4.41 (4/5 x 2H, ABq, Δ=0.15, J=15Hz), 5.00-5.20 (2H, a), 6.92-8.20 (15K, a), 9.74 (1/5 κ IH, s), 9.80 (4/5 κ IH, s) (37) MASS (a/z) : 632 (M+H) + NMR (CDCI3, δ) : 2.58-2.72 (IH, a), 2.63 (4/5 κ 3H, s), 2.75 (1/5 x 3H, s) , 2.94-3.20 (2H, a), 3.22- 3.80 (9H, m), 4.19 (1/5 x 2H, ABq, Δ=0.24, J=17Hz) , 4.42 (4/5 x 2H, ABq, Δ=0.22, J=15Hz) , 5.01-5.13 (2H, m) , 7.08-7.77 (13H, a), 8.02-8.26 (2H, m) (38) MASS (m/z) : 648 (M+H) + NMR (CDCI3, δ) : 2.52-2.70 (IH, m) , 2.66 (4/5 x 3H, s), 2.77 (1/5 x 3H, s) , 2.93-3.18 (2H, m) , 3.22- 3.82 (9H, m) , 4.06 (1/5 x IH, d, J=17Hz) , 4.32 (1/5 x IH, d, J=17Hz), 4.42 (2/5 x 2H, ABq, Δ=0.18, J=15Hz), 4.97-5.15 (2H, m) , 7.08-7.52 (9H, m) , 7.65-7.93 (4H, m) , 8.03-8.21 (2H, m) (39) MASS (m/z) : 597 (M+H) + NMR (CDCI3, δ) : 2.55-2.70 (IH, a), 2.68 (4/5 x 3H, s) , 2.79 (1/5 x 3H, s) , 2.98-3.06 (2H, a) , 3.22-3.33 (IH, a), 3.40-3.78 (8H, m) , 4.09 (1/5 x IH, d, J=17Hz), 4.36 (1/5 x IH, d, J=17Hz) , 4.48 (4/5 x 2H, ABq, Δ=0.15, J=15Hz) , 5.03-5.18 (2H, a), 6.95- 7.48 (11H, a), 7.63-7.78 (2H, a) , 8.00-8.12 (IH, a), 8.30-8.55 (2H, a), 9.33 (1/5 κ IH, br s), 9.51 (4/5 κ IH, br s) (40) MASS (m/z) : 598 (M+H) + NMR (CDCI3, δ) : 2.57-2.72 (IH, a), 2.62 (3/4 κ 3H, s), 2.77 (1/4 κ 3H, s) , 2.95-3.18 (2H, a) , 3.22- 3.81 ( 9H, a ) , 4.09 ( 1/4 κ IH, d, J=17Hz), 4.31 ( 3/4 κ IH, d, J=15Hz ) , 4.34 (1/4 κ IH, d, J=17Hz ) , 4.61 ( 3/4 κ IH, d, J=15Hz) , 5.02-5.19 (2H, a ) , 7.10-7. 7 6 ( 13H, a ) , 8.13-8.25 (IH, m) , 8.30 (1/4 κ IH, s ) , 8.38 ( 3/4 x IK, s), 8.46-8.55 (IH, m ) ( 41 ) MASS (m/z) : 611 (M + H) + NMR ( CDC1 3 , δ ) : 2.31 (3H, s) , 2.31-2.52 (4H, m ) , 2.6 0 - 2.73 ( IH, m ) , 2.62 (3/4 x 3H, s) , 2.77 ( 1/4 x 3K, s ) , 2.98-3.18 ( 2H, m) , 3.27-3.77 (5H, m) , 4.22 ( 1/4 x 2H, ABq, Δ=0.22, J=17Hz) , 4.29 (3/4 x IH, d, J=15Hz ) , 4.62 ( 3/4 x IH, d, J=15Hz) , 5.03-5.20 ( 2H, m ) , 7.12-7.78 (13H, m) , 8.16-8.25 (IH, m ) , 8.28 ( 1/4 x IH, s ) , 8.38 (3/4 x IH, s), 8.48-8.55 ( IH, ( 42 ) MASS (m/z) : 623 (M+H) + NMR ( CDCI3, δ ) : 1.07 (3H, t, J=7Hz) , 2.28-2.52 ( 6H, a ) , 2.61 ( 2/3 x 3H, s) , 2.61-2.76 (IK, a), 2.81 ( 1/3 x 3H, s ) , 2.92-3.11 (2H, a), 3.18-3.35 ( IH, a ) , 3.35-3.75 (4H, a), 4.26 (2/3 x IH, d, J=15Hz ) , 4.27 ( 1/3 κ 2H, ABq, Δ=0.22, J=17Hz) , 4.68 ( 2/3 κ IH, d, J=15Hz ) , 5.04-5.22 (2H, a), 6.92-8.12 ( 17H, m ) , 9.68 (1/3 x IH, s), 9.72 (2/3 x IH, s ) ( 43 ) MASS (m/z) : 624 (M+H) + NMR ( CDCI3, δ ) : 1.07 (3H, t, J=7Hz), 2.32-2.54 ( 6H, m ) , 2.58 ( 2/3 x 3H, s) , 2.58-2.70 (IH, a), 2.80 ( 1/3 κ 3H, s ) , 2.94-3.14 (2H, m) , 3.24-3.74 ( 5H, m ) , 4.24 ( 1/3 κ 2H, ABq, Δ=0.22, J=17H Z ) , 4.28 ( 2/3 x IH, d, J=15Hz ) , 4.63 (2/3 x IH, d, J=15Hz) , 5. 0 0- 5.29 ( 2H, m ) , 6.90-7.74 (16H, m) , 8.15-8.27 ( IH, a ) ( 44 ) MASS (a/z) : 640 (M + H) + NMR ( CDCI3, δ ) : 1.08 (3H, t, J=7Hz) , 2.32-2.58 ( 6H, m) , 2.58-2.70 (IH, m) , 2.62 (2/3 x 3H, s) , 2.32 (1/3 κ 3H, s), 2.93-3.13 (2H, a), 3.24-3.75 (5H, a), 4.28 (1/3 κ 2H, ABq, Δ=0.22, J=17HZ) , 4.32 (2/3 κ IH, d, J=15Hz), 4.65 (2/3 x IH, d, J=15Hz), 4.95- 5.18 (2H, a), 6.92-8.20 (17H, m) (45) MASS (m/z) : 640 (M " * * +l) NMR (CDC1 3 , δ) : 2.29 (3H, s), 2.42 (4H, m) , 2.57 (3H x 2/3, s), 2.66 (IH, dd, J=6, 16Hz) , 2.77 (3H κ 1/3, s), 3.04 (2H, m) , 3.33 (IH, m) , 3.49 (2H, m) , 3.67 (2H, a), 3.77 (3H, s), 4.02 (IK κ 1/3, d, J=16Hz), 4.21 (IH κ 2/3, d, J=15Hz) , 4.29 (IH κ 1/3, d, J=16Hz), 4.57 (IH x 2/3, d, J=15Hz) , 5.06- 5.19 (2H, m) , 6.80 (2H, d, J=8Hz) , 6.87-7.02 (2H, a), 7.17-7.21 (5H, m) , 7.31 (IH, t, J=8Hz) , 7.44 (IH, t, J=8Hz), 7.51 (IH, s), 7.56 (IH, d, J=8Hz) , 7.64-7.72 (2H, a), 8.22 (IH, m) (46) MASS (ESI) (m/z) : 640 (M+H) + NMR (CDCI3, δ) : 2.27 (3H, s) , 2.29 (3H, s), 2.23-2.52 (4H, m) , 2.55-2.68 (IH, m) , 2.61 (3 x 2/3H, s), 2.80 (3 x 1/3H, s), 2.97-3.10 (2H, a), 3.28-3.38 (IH, a), 3.42-3.58 (2H, m) , 3.62-3.72 (2H, m) , 4.09 (2 x 1/4H, d, J=17Hz), 4.27 (2 x 1/4K, d, J=15Hz), 4.33 (2 x 1/4H, d, J=17Hz) , 4.60 (2 x 1/4H, d, J=15Hz), 4.99-5.15 (2H, m) , 6.89 (2 κ 1/3H, d, J=8Hz), 6.98 (2 x 2/3H, d, J=8Hz) , 7.07 (2H, a, J=8Hz), 7.12-7.20 (5H, a) , 7.38-7.48 (2H, m) , 7.71 (IH, t, J=8Hz), 7.80-7.88 (3H, a), 8.12 (IH, d, J=8Hz) (47) MASS (ESI) (m/z) : 623 (M+H) ÷ NMR (CDCI3, δ) : 2.21 (3H, s), 2.27 (3H, s) , 2.28-2.40 (4H, m) , 2.56 (3 x 2/3H, s), 2.62-2.78 (IH, m) , 2.80 (3 x 1/3H, s), 2.93-3.08 (2H, m) , 3.18-3.27 96/16981 - 581 - (IH, m) , 3.35-3.48 (2H, m) , 3.53-3.70 (2H, m, , 4.13 (2 x 1/6H, d, J=17Hz), 4.20 (2 x 1/3H, d, J=15Hz) , 4.31 (2 x 1/6H, d, J=17Hz) , 4.68 (2 x 1/3H, a, J=15Hz), 5.12-5.30 (2H, m) , 6.86 (2 x 1/3H, d, J=8Hz), 6.93 (2 x 2/3H, d, J=8Hz) , 6.98-7.12 (9H, m) , 7.22 (IH, t, J=8Hz), 7.44 (IH, d, J=8Hz) , 7.63 (IH, d, J=8Hz), 8.01-8.11 (2H, m) (48) MASS (ESI) (m/z) : 624 (M+H) + NMR (CDC1 3 , δ) : 2.29 (3H, s) , 2.31 (3H, s) , 2.33-2.52 (4H, m) , 2.58 (3 x 2/3H, s) , 2.61-2.71 (IH, m) , 2.79 (3 x 1/3H, s) , 2.98-3.12 (2H, m) , 3.28-3.38 (IH, m) , 3.42-3.57 (2H, a), 3.62-3.72 (2H, m) , 4.08 (2 x 1/4H, d, J=17Hz), 4.23 (2 x 1/4H, d, J=15Hz) , 4.31 (2 x 1/4H, d, J=17Hz) , 4.61 (2 x 1/4H, d, J=15Hz), 5.03-5.18 (2H, m) , 6.86 (2 x 1/3H, d, J=8Hz), 6.97 (2 x 2/3H, d, J=8Hz) , 7.09 (2H, d, J=8Hz), 7.12-7.22 (5H, m) , 7.29 (IH, t, J=8Hz) , 7.43 (IH, t, J=8Hz), 7.49 (IH, s) , 7.58 (IH, d, J=8Hz), 7.67 (2H, q, J=8Hz) , 8.20-8.23 (IH, m) (49) MASS (m/z) : 550 (M + +l) NMR (CDCI3, δ) : 2.29 (3H, s) , 2.39 (4H, a), 2.57-2.72 (IH, m) , 2.89 (3H x 1/3, s) , 2.99 (3H x 2/3, s) , 3.38-3.51 (3H, m) , 3.54-3.70 (3H, m) , 3.78 (IH, dd, J=5, 11Hz), 3.87-3.98 (IH, a), 4.44 (IH x 2/3, d, J=15Hz), 4.63 (2H x 1/3, s) , 4.67 (IH x 2/3, d, J=15Hz), 5.03 (IK, m) , 5.09 (IH x 1/3, m) , 5.16 (IH x 2/3, m) , 7.16-7.19 (2H, m) , 7.25-7.37 (4H, m) , 7.44 (IH, t, J=8Hz), 7.53 (IH, s), 7.58 (IH, d, J=8Hz), 7.67 (IH, d, J=8Hz), 7.74 (IK, d, J=8Hz) , 8.06 (IH, m) (50) MASS (m/z) : 576 (M + +l) NMR (CDCI3, δ) : 0.79 (3H x 1/3, d, J=7Hz) , 0.83 (3H x 1/3, d, J=7Hz) , 0.93 (3H x 2/3, d, J=7Hz) , 0.96 (3H κ 2/3, d, J=7Hz), 1.38-1.49 (IH, a), 1.58-1.75 (2H, a), 2.27 (3H, s) , 2.38 (4H, a), 2.65 (IH, a), 2.89 (3H κ 1/3, s), 2.97 (3H κ 2/3, s), 3.29 (IH, dd, J=3, 16Hz) , 3.46 (2H, a), 3.65 (2H, m) , 4.36 (IH κ 2/3, d, J=15Hz) , 4.60 (IH κ 1/3, d, J=15Hz), 4.65 (IH x 1/3, d, J=15Hz), 4.73 (IH x 2/3, d, J=15Hz), 4.96 (IH, m) , 5.11 (IH, m) , 7.16-7.36 (5H, m) , 7.41 (2H, t, J=8Hz) , 7.48 (IH, s), 7.53 (IH, d, J=8Hz), 7.59-7.73 (2H, m) , 8.24 (IH, d, J=8Hz) (51) MASS (m/z) : 678 (M + +l) NMR (CDC1 3 , δ) : 2.30 (3H, s), 2.42 (4H, m) , 2.64 (3H x 3/4, s), 2.67 (IH, dd, J=7, 16Hz) , 2.80 (3H x 1/4, s), 2.96-3.15 (2H, m) , 3.34 (IH, dd, J=3, 16Hz), 3.49 (2H, m) , 3.67 (2H, m) , 4.27 (IH κ 1/4, d, J=16Hz), 4.34 (IH κ 1/4, d, J=16Hz) , 4.36 (IH κ 3/4, d, J=15Hz), 4.66 (IH x 3/4, d, J=15Hz) , 5.02- 5.18 (2H, m) , 6.99-7.21 (7H, m) , 7.30 (IH, t, J=8Hz), 7.44 (IH, t, J=8Hz), 7.51-7.62 (4H, a), 7.67-7.71 (2H, m) , 8.21 (IH, t, J=8Hz) (52) MASS (m/z) : 677 (M + +l) NMR (CDCI3, δ) : 2.24 (3H, s) , 2.30-2.39 (4H, a), 2.63 (3H x 3/4, s) , 2.71 (IH, dd, J=5, 16Hz) , 2.78 (3H κ 1/4, s), 2.93-3.12 (2H, a), 3.25 (IH, dd, J=3, 16Hz), 3.43 (2H, a), 3.62 (2H, a), 4.27 (IH x 3/4, d, J=15Hz), 4.32 (2H x 1/4, s), 4.67 {IH κ 3/4, a, J=15Hz), 5.06-5.25 (2H, a), 6.96-7.28 (10H, a), 7.43-7.49 (3H, a), 7.65 (IH, d, J=8Hz) , 8.03 (IH, d, J=7Hz), 8.10 (IH, d, J=7Hz) (53) MASS (m/z) : 610 (M + +l) NMR (CDCI3, δ) : 2.28 (3H, s), 2.37-2.40 (4H, m) , 6/16981 - 583 - 2.52 (IK, dd, J=7, 16Hz) , 2.64 (3H κ 2/3, s), 2.88 (3H κ 1/3, s), 2.97-3.09 (2H, m) , 3.17 (IH κ 1/3, dd, J=3, 16Hz), 3.28 (IH x 2/3, dd, J=3, 16Hz), 3.37-3.48 (2H, m) , 3.56-3.74 (2H, a), 4.28 (IH x 2/3, d, J=15Hz), 4.29 (IH x 1/3, d, J=15Hz) , 4.41 (IH x 1/3, d, J=15Hz), 4.72 (IH x 2/3, d, J=15Hz), 4.94 (IH x 1/3, dt, J=4, 7Hz), 5.10 (IK x 2/3, dt, J=4, 7Hz), 5.19 (IH, dt, J=7, 7Hz) , 7.02 (IH, d, J=7Hz), 7.07-7.32 (10H, a) , 7.42 (IH, t, J=8Hz) , 7.48-7.55 (2H, m) , 7.66 (IH, d, J=8Hz) , 7.84 (IH κ 2/3, d, J=8Hz), 7.92 (IH x 1/3, d, J=8Hz) , 8.00 (IH x 1/3, d, J=8Hz), 8.16 (IH x 2/3, d, J=8Hz) (54) MASS (m/z) : 610 (M + +l) NMR (CDC1 3 , δ) : 2.27 (3H, s) , 2.37-2.43 (4H, m) , 2.58 (3H x 2/3, s), 2.66 (IH, dd, J=7, 15Hz), 2.79 (3H x 1/3, s), 3.04 (2H, m) , 3.29 (IH, dt, J=4, 15Hz) , 3.47 (2H, a), 3.65 (2H, m) , 4.14 (IH x 1/3, d, J=15Hz), 4.26 (IH x 2/3, d, J=15Hz) , 4.33 (IH x 1/3, d, J=15Hz), 4.63 (IH x 2/3, d, J=15Hz) , 5.02- 5.16 (2H, m) , 6.92-7.05 (2H, m) , 7.15 (5H, m) , 7.23-7.30 (4H, a), 7.42 (IH, t, J=8Hz) , 7.48 (IH, s), 7.54 (IH, d, J=8Hz), 7.64-7.74 (2H, a), 8.22 (IH, m) (55) MASS (m/z) : 610 (M + +l) NMR (CDC1 3 , δ) : 2.28 (3H, s), 2.37-2.40 (4H, m) , 2.52 (IH, dd, J=7, 16Hz), 2.64 (3H x 2/3, s) , 2.88 (3H κ 1/3, s), 2.97-3.09 (2H, m) , 3.17 (IH κ 1/3, dd, J=3, 16Hz), 3.28 (IH x 2/3, dd, J=3, 16Hz), 3.37- 3.48 (2H, a), 3.56-3.74 (2H, m) , 4.28 (IH x 2/3, d, J=15Hz), 4.29 (IH x 1/3, d, J=15Hz) , 4.41 (IH x 1/3, d, J=15Hz), 4.72 (IH x 2/3, d, J=15Hz) , 4.94 (IH x 1/3, dt, J=4, 7Hz), 5.10 (IH x 2/3, dt, J=4, 7Hz), 5.19 (IH, dt, J=7, 7Hz) , 7.02 (IH, d, J=7Hz) , 7.07-7.32 (10H, a), 7.42 (IH, t, J=8Kz) , 7.48-7.55 (2H, a), 7.66 (IH, d, J=8Hz) , 7.84 (IH x 2/3, d, J=8Hz), 7.92 (IH x 1/3, d, J=8Hz) , 8.00 {IH x 1/3, d, J=8Hz), 8.16 (IH x 2/3, d, J=8Hz) (56) MASS (FAB) (m/z) : 598 (M+H) + NMR (CDC1 3 , δ) : 2.67 (3 x 2/3H, s), 2.68-2.74 (IH, a), 2.83 (3 x 1/3H, s) , 2.98-3.12 (2H, a), 3.20- 3.31 (IH, m) , 3.39-3.53 (2H, m) , 3.60-3.75 (6H, m) , 4.13-4.42 (2 x 2/3H, m) , 4.63 (2 x 1/3H, d, J=15Hz), 5.07-5.20 (2H, m) , 6.99-7.08 (2H, m) , 7.12-7.33 (9H, m) , 7.49 (IH, s) , 7.67 (IH, t, J=8Hz), 8.03 (IH, d, J=8Hz) , 8.23 (IH, d, J=8Hz) , 8.48 (IH, d, J=5Hz) (57) MASS (FAB) (m/z) : 643 (M+H) + NMR (CDC1 3 , δ) : 2.59-2.70 (IH, m) , 2.65 (3 x 2/3H, s), 2.82 (3 x 1/3H, s) , 2.98-3.07 (2H, m) , 3.21- 3.33 (IH, m) , 3.40-3.53 (2H, m) , 3.62-3.75 (6K, m) , 4.11-4.46 (2 x 2/3H, m) , 4.62 (2 x 1/3H, d, J=15Hz), 5.02-5.17 (2H, m) , 7.01-7.35 (10H, m) , 7.63 (IH, s), 7.67 (IH, d, J=8Hz) , 8.40 (IH, d, J=8Hz), 8.90 (IH, s), 9.38 (IH, s) (58) MASS (FAB) (m/z) : 645 (M+H) + NMR (CDC1 3 , δ) : 2.53-2.63 (IH, ) , 2.67 (3 x 2/3H, s), 2.83 (3 x 1/3H, s) , 2.97-3.11 (2H, a), 3.30 (IH, t, J=15Hz), 3.42-3.59 (2H, m) , 3.62-3.80 (6H, m) , 4.13-4.45 (2 x 2/3H, a), 4.22 (2H, s), 4.63 (2 x 1/3H, d, J=15Hz), 5.08-5.18 (2H, m) , 7.00-7.32 (11H, m) , 7.35 (IH, t, J=8Hz) , 7.47 (IK, t, J=8Hz) , 7.53-7.62 (2H, m) , 7.70-7.83 (IH, m) , 7.93 (IK, d, J=8Hz), 8.06-8.11 (IH, m) (59) MASS (FAB) (m/z) : 627 (M+H) + NMR (CDC1 3 , δ) : 2.31 (3H, s), 2.36-2.49 (4H, a,, 2.62 (3 x 2/3H, s), 2.66-2.78 (IH, a), 2.81 (3 κ 1/3H, s), 2.98-3.12 (2H, m) , 3.28-3.37 (IH, m) , 3.42-3.55 (2H, a), 3.66-3.71 (2H, a), 4.13-4.40 (2 x 2/3H, m) , 4.63 (2 x 1/3H, d, J=15Hz) , 5.02-5.20 (2H, m) , 6.97-7.08 (2H, m) , 7.16-7.22 (5H, m) , 7.26-7.31 (3H, m) , 7.48-7.73 (3H, a), 7.98 (IH, a, J=8Hz), 8.15 (IH, d, J=8Hz), 8.80-8.84 (IH, m) (60) MASS (FAB) (m/z) : 644 (M+H) + NMR (CDC1 3 , δ) : 2.29 (3H, s), 2.36-2.49 (4H, s), 2.60 (3 x 2/3H, s), 2.58-2.70 (IH, m) , 2.82 (3 x I/3H, s), 2.97-3.11 (2H, m) , 3.31 (IH, t, J=15Hz) , 3.42- 3.58 (2H, m) , 3.66-3.72 (2H, m) , 4.10-4.39 (2 x 2/3H, m) , 4.65 (2 x 1/3H, d, J=15Hz) , 5.01-5.18 (2H, a), 6.97-7.08 (2H, m) , 7.12-7.21 (5H, a), 7.23-7.30 (3H, m) , 7.39-7.52 (3H, m) , 7.65 (IH, s) , 7.72 (IH, d, J=8Hz), 8.27 (IH, d, J=8Hz) (61) MASS (FAB) (m/z) : 640 (M+H) + NMR (CDC1 3 , δ) : 2.27 (3H, s), 2.33-2.49 (4H, m) , 2.58-2.71 (IH, m) , 2.59 (3 x 2/3H, s), 2.80 (3 x 1/3H, s), 2.98-3.12 (2H, m) , 3.29 (IH, t, J=15Hz) , 3.42-3.55 (2H, m) , 3.63-3.70 (2H, a), 3.84 (3H, s), 4.08-4.38 (2 x 2/3H, m) , 4.65 (2 x 1/3H, d, J=15Hz), 5.02-5.18 (2H, m) , 6.94-7.08 (4H, m) , 7.12-7.21 (5H, a), 7.23-7.30 (3H, a), 7.43 (IH, s), 7.45 (IH, d, J=8Hz), 7.65 (1 x 1/3H, d, J=8Hz), 7.71 (1 x 2/3H, d, J=8Hz), 8.15-8.20 (IH, m) (62) MASS (FAB) (m/z) : 688 (M+H) + NMR (CDCI3, δ) : 2.30 (3H, s), 2.36-2.50 (4H, a), 2.58-2.70 (IH, a), 2.62 (3 x 2/3H, s) , 2.82 (3 x 1/3H, s), 2.98-3.12 (2H, m) , 3.32 (IH, t, J=15Hz), 3.42-3.57 (2H, m) , 3.63-3.71 (2H, m) , 4.11-4.39 (2 κ 2/3H, m) , 4.65 (2 κ 1/3H, d, J=15Hz), 5.00-5.13 (2H, m) , 6.97-7.08 (2H, m) , 7.13-7.21 (4H, m) , 7.23-7.32 (4H, m) , 7.40-7.53 (2H, m) , 7.63-7.96 (2H, m) , 8.20-3.22 (2H, m) (63) MASS (FAB) (m/z) : 640 (M+H) + NMR (CDC1 3 , δ) : 2.29 (3H, s), 2.35-2.47 (4H, m) , 2.61 (3 κ 2/3H, s), 2.71 (IH, dd, J=15, 8Hz), 2.83 (3 κ 1/3H, s), 2.97-3.11 (2H, m) , 3.19-3.29 (IH, m) , 3.40-3.55 (2H, m) , 3.63-3.72 (2H, m) , 4.02 (3K, s), 4.17-4.40 (2 x 2/3H, m) , 4.67 (2 x 1/3H, d, J=15Hz), 5.02-5.15 (2H, m) , 6.90 (IH, d, J=8Hz) , 6.97 (IH, d, J=8Hz), 7.07 (IH, d, J=8Hz), 7.12-7.21 (6H, m) , 7.22-7.31 (4H, m) , 7.48 (IH, s), 7.68 (1 x 1/3H, d, J=8Hz), 7.75 (1 κ 2/3H, d, J=8Hz) , 8.11 (IH, t, J=8Hz) (64) M7ASS (FAB) (m/z) : 563 (M+H) + NMR (CDCI3, δ) : 2.50-2.71 (IH, m) , 2.62 (3 κ 2/3H, s), 2.82 (3 κ 1/3H, s), 2.99-3.06 (2H, a), 3.28 (IH, t, J=15Hz), 3.40-3.58 (2H, a), 3.62-3.79 (6H, a), 4.12-4.42 (2 κ 2/3H, a), 4.65 (2 κ 1/3H, d, J=15Hz) , 4.95-5.13 (2H, m) , 6.98-7.33 (11H, a) , 7.51-7.71 (3H, a), 7.90 (IH, t, J=8Hz) (65) MASS (FAB) (a/z) : 547 (M+H ) + NMR (CDCI3, δ) : 2.51-2.58 (IH, m) , 2.59 (3 κ 2/3H, s), 2.82 (3 κ 1/3H, s) , 3.00-3.10 (2H, m) , 3.29 (IH, t, J=15Hz), 3.40-3.55 (2H, m) , 3.63-3.76 (6H, a) , 4.09-4.39 (2 κ 2/3K, a) , 4.64 (2 κ 1/3H, a, J=15Hz), 4.98-5.17 (2H, a), 6.51-6.54 (IH, a), 6.93-7.32 (11H, a) , 7.51 (IH, s), 7.58 (IK, dd, J=18, 8Hz), 7.99 (IH, d, J=8Hz) (66) MASS (FAB) (m/z) : 558 (M+H) + NMR (CDCI3, δ) : 2.59 (3 κ 2/3H, s) , 2.61-2.72 (IH, a), 2.77 (3 x 1/3H, s), 2.99-3.05 (2H, a), 3.22- 3.33 (IH, a), 3.41-3.55 (2H, a), 3.62-3.72 (6K, a), 4.12-4.45 (2 x 2/3H, m) , 4.63 (2 x 1/3H, d, J=15Hz), 5.02-5.18 (2H, a), 6.92-7.22 (7H, a), 7.23-7.31 (3H, m) , 7.42-7.56 (2H, a), 7.88 (IH, t, J=8Hz), 8.20 (IH, d, J=8Hz), 8.62 (IH, d, J=5Hz), 9.18 (IH, d, J=8Hz) (67) MASS (FAB) (m/z) : 556 (M+H) + NMR (CDCI3, δ) : 2.49-2.68 (IH, m) , 2.65 (3 κ 2/3H, s), 2.82 (3 x 1/3H, s) , 2.98-3.05 (2H, m) , 3.29 (IH, t, J=15Hz), 3.41-3.59 (2H, m) , 3.61-3.78 (6H, m), 4.12-4.42 (2 x 2/3H, ) , 4.65 (2 x 1/3H, d, J=15Hz), 5.00-5.13 (2H, m) , 6.99-7.23 (7H, m) , 7.25-7.32 (3H, m) , 7.43-7.57 (3H, m) , 7.62-7.72 (IH, m) , 7.85 (2H, d, J=8Hz) , 8.07 (IH, t, J=8Hz) (68) MASS (FAB) (m/z) : 495 (M+H) + NMR (CDCI3, δ) : 2.03 (3K, d, J=5Hz) , 2.43-2.55 (IH, a), 2.58 (3 x 2/3H, s) , 2.82 (3 x 1/3H, s) , 3.01 (2H, t, J=8Hz), 3.18 (IH, t, J=8Hz) , 3.38-3.51 (2H, a), 3.58-3.63 (2H, m) , 3.67-3.75 (4H, m) , 4.08 (2 κ 1/8H, d, J=15Hz), 4.28-4.38 (2 κ 4/8H, m) , 4.63 (2 x 3/8H, d, J=15Hz), 4.78-4.90 (IH, m) , 5.01-5.12 (IH, m) , 6.97 (IH, d, J=8Hz) , 7.05-7.31 (10K, m) , 7.53 (IH, t, J=8Hz) (69) MASS (FAB) (m/z) : 608 (M+H) + NMR (CDCI3, δ) : 2.60 (3 x 2/3H, s), 2.68-2.88 (IK, a), 2.80 (3 x 1/3H, s) , 3.05 (2H, t, J=8Hz), 3.12- 3.33 (IH, a), 3.41-3.52 (2H, m) , 3.62-3.73 ( 6n f a), 4.15-4.33 (2 x 2/3H, m) , 4.65 (2 x 1/3H, d, J=15Hz), 5.10-5.21 (2H, m) , 6.96-7.08 (2H, m) , 7.12-7.21 (5H, ) , 7.23-7.31 (4H, m) , 7.58-7.68 (2H, m) , 7.80 (IH, t, J=8Hz) , 7.90 (IH, d, J=8Hz), 8.21-3.35 (3H, m) (70) MASS (FAB) (m/z) : 546 (M+H) + NMR (CDC1 3 , δ) : 2.50-2.62 (IH, m) , 2.61 (3 x 2/3H, s), 2.82 (3 x 1/3H, s) , 2.96-3.08 (2H, a), 3.20- 3.33 (IH, m) , 3.43-3.50 (2H, a), 3.60-3.75 (6K, a), 4.11-4.40 (2 x 2/3H, m) , 4.67 (2 x 1/3H, d, J-15HZ), 4.98-5.15 (2H, a), 6.13-6.17 (IH, a), 6.67-6.71 (IH, m) , 6.93-7.10 (3H, m) , 7.12-7.32 (8H, m) , 7.58-7.70 (2H, a), 9.48 (IH, br s) (71) M7ASS (FAB) (m/z) : 607 (M+H) ÷ NMR (CDCI3, δ) : 2.62 (3 x 2/3H, s) , 2.67-2.75 (IH, a), 2.82 (3 x 1/3H, s) , 3.02-3.09 (2H, m) , 3.29- 3.78 (9H, m) , 4.08-4.43 (2 x 2/3H, a), 4.63 (2 x 1/3H, d, J=15Hz), 5.08-5.22 (2H, m) , 7.00-7.33 (7H, m) , 7.25-7.32 (3H, m) , 7.43-7.96 (8H, a), 8.40 (IH, d, J=8Hz) (72) MASS (FAB) (m/z) : 607 (M+H) + NMR (CDCI3, δ) : 2.56-2.70 (IH, m) , 2.65 (3 x 2/3H, S ), 2.83 (3 x 1/3H, s), 2.93-3.12 (2H, a), 3.31 (IH, t, J=15Hz), 3.43-3.58 (2H, m) , 3.62-3.80 (6H, m) , 4.15-4.45 (2 x 2/3H, a), 4.64 (2 x 1/3H, d, J=15Hz), 5.08-5.19 (2H, m) , 7.01-7.22 (8H, a), 7.23-7.43 (2H, a), 7.52-7.62 (2K, m) , 7.73-7.83 (IH, m) , 7.89-7.92 (3H, a), 7.98 (IH, d, J=8Hz), 8.22 (IH, d, J=8Hz), 8.39 (IH, s) (73) MASS (FAB) (a/z) : 614 (M+H) ÷ NMR (CDCI3, δ) : 263 (3 x 2/3H, s) , 2.64-2.78 (IH, m) , 2.81 (3 x 1/3H, s), 2.97-3.12 (2H, m) , 3.22-3.32 (IH, m) , 3.40-3.55 (2H, a), 3.60-3.76 (6H, a), 4.12-4.39 (2 x 2/3H, a), 4.63 (2 x 1/3H, d. 96/16981 - 589 - J=15Hz), 5.01-5.18 (2H, m) , 6.97-7.20 (7H, m) , 7.23-7.30 (3H, m) , 7.47-7.71 (3H, a), 7.97 (IH, d, J=8H∑), 8.15 (IH, d, J=8Hz) , 8.82 (IH, d, J=8Hz) (74) MASS (FAB) (m/z) : 659 (M+H) + NMR (CDC1 3 , δ) : 2.53-2.62 (IH, m) , 2.69 (2H, s) , 2.82 (IH, s), 2.94-3.11 (2H, m) , 3.26 (IH, t, J=15Hz) , 3.42-3.58 (2H, m) , 3.62-3.78 (6H, m) , 4.12-4.48 (2 x 2/3H, m) , 4.64 (2 x 1/3H, d, J=15Hz), 5.01-5.15 (2H, m) , 7.01-7.22 (7H, m) , 7.23-7.40 (5H, m) , 7.52-7.60 (2H, m) , 7.70 (IH, d, J=8Hz) , 7.78 (IH, d, J=8Hz), 7.99-8.05 (2H, m) , 8.12 (IH, d, J=8Hz) (75) MASS (FAB) (m/z) : 598 (M+H) + NMR (CDC1 3 , δ) : 2.60 (3 x 2/3H, s) , 2.52-2.72 (IH, a) , 2.80 (3 x 1/3H, s) , 2.94-3.10 (2K, m) , 3.28 (IH, t, J=15Hz), 3.40-3.52 (2H, m) , 3.62-3.76 (6H, m) , 4.12-4.42 (2 x 2/3H, m) , 4.62 (2 x 1/3H, d, J=15Hz), 5.01-5.16 (2H, m) , 6.98-7.18 (7H, m) , 7.22-7.32 (3H, m) , 7.41-7.52 (2H, ) , 7.65 (IH, d, J=8Hz), 7.72 (IH, d, J=8Hz), 7.85 (IH, d, J=8Hz), 8.82 (IH, d, J=8Hz) (76) MASS (FAB) (m/z) : 645 (M+H) + NMR (CDC1 3 , δ) : 2.28-2.42 (IH, m) , 2.53 (3 x 2/3H, s), 2.81 (3 x 1/3H, s) , 2.82-3.01 (3H, m) , 3.27- 3.38 (2H, m) , 3.43-3.70 (6H, m) , 4.03-4.35 (2 x 2/3H, m) , 4.62 (2 x 1/3H, d, J=15Hz) , 4.75-4.88 (2H, m) , 4.93-5.00 (IH, m) , 6.90-6.98 (IH, a), 7.03-7.30 (12H, m) , 7.32-7.55 (4H, m) , 7.70-7.81 (3H, m) (77) MASS (FAB) (m/z) : 597 (M+H) + NMR (CDC1 3 , δ) : 2.65 (3 x 2/3H, s) , 2.83 (3 x 1/3K, s), 2.81-3.18 (4H, m) , 3.40-3.47 (2H, m) , 3.55-3.65 (6H, m) , 4.28 (2 κ 2/3H, t, J=15Hz) , 4.75 (2 κ 1/3H, d, J=15Hz), 5.20-5.30 (IH, m) , 5.46-5.61 (IH, m) , 6.93-7.11 (7H, m) , 7.21-7.32 (5H, m) , 7.46-7.52 (IH, m) , 7.78-7.83 (IH, m) , 8.40-8.49 (IH, m) , 8.63-8.72 (IH, m) (78) MASS (FAB) (m/z) : 615 (M+H) + NMR (CDC1 3 , δ) : 2.53 (3 x 2/3H, s) , 2.75 (3 x 1/3H, s), 2.80-2.92 (IH, m) , 3.00-3.13 (2H, m) , 3.25 (IH, dd, J=15, 4Hz), 3.43-3.51 (2H, m) , 3.60-3.69 (6H, m) , 3.99-4.30 (2 x 2/3H, m) , 4.58 (2 x 1/3H, d, J=15Hz), 4.81-4.92 (IH, m) , 5.13-5.20 (IH, m) , 6.83-6.97 (2H, m) , 7.08-7.23 (10H, m) , 7.35 (IH, d, J=8Hz), 7.83-7.90 (IH, a), 8.17 (IH, d, J=8Hz) (79) MASS (FAB) (a/z) : 608 (M+H) + NMR (CDC1 3 , δ) : 2.60-2.73 (IH, a), 2.63 (3 κ 2/3H, s), 2.81 (3 κ 1/3H, s), 3.00-3.08 (2H, a), 3.30 (IH, t, J=15Hz), 3.41-3.56 (2H, a), 3.60-3.78 (6H, a), 4.09-4.47 (2 x 2/3H, m) , 4.63 (2 x 1/3H, d, J=15Hz), 5.08-5.20 (2H, m) , 7.00-7.33 (10H, a), 7.43-7.52 (IH, m) , 7.67-7.83 (2H, m) , 7.88-8.03 (IH, m) , 8.20 (IH, d, J=8Hz) , 8.31 (IH, d, J=8Hz) , 8.58 (IH, s), 8.82-9.00 (IH, m) (80) MASS (FAB) (m/z) : 609 (M+H) + NMR (CDC1 3 , δ) : 2.63 (3 κ 2/3H, s), 2.81 (3 κ 1/3H, s), 2.68-2.80 (IH, a), 3.01-3.08 (2H, m) , 3.23-3.35 (IH, m) , 3.40-3.57 (2H, a), 3.63-3.75 (6H, a) , 4.10-4.42 (2 x 2/3H, a), 4.63 (2 x 1/3H, d, J=15Hz), 5.11-5.22 (2H, m) , 6.99-7.22 (6H, m) , 7.24-7.32 (4H, m) , 7.62-7.72 (IH, m) , 7.83-7.92 (2H, m) , 8.12 (2H, t, J=8Hz) , 9.11-9.17 (IH, m) , 9.64 (IH, s) (81) MASS (FAB) (m/z) : 610 (M+H) + NMR (CDC1 3 , δ) : 2.55-2.67 (IH, a), 2.61 (3 x 2/3H, s), 2.81 (3 x 1/3H, s), 2.99-3.06 (2H, a), 3.27 (IH, t, J=15Hz), 3.40-3.58 (2H, m) , 3.62-3.77 (6H, m) , 4.03 (3H, s) , 4.12-4.42 (2 x 2/3H, a), 4.63 (2 x 1/3H, d, J=15Hz), 4.99-5.17 (2H, m) , 6.98-7.41 (14H, m) , 7.67 (2H, q, J=8Hz) , 8.01 (IH, t, J=8Hz) (82) MASS (FAB) (m/z) : 740 (M-rH) + NMR (CDC1 3 , δ) : 1.23 (3H, t, J=8Hz) , 2.52-2.71 (5H, m) , 2.62 (3 x 2/3H, s) , 2.79 (3 x 1/3H, s), 2.97- 3.14 (2H, m) , 3.22 (2H, s) , 3.28-3.39 (IH, m) , 3.47-3.62 (2H, ) , 3.68-3.78 (2H, m) , 3.91 (3H, s), 4.18 (2H, q, J=8Hz) , 4.30-4.38 (2 x 2/3H, m) , 4.70 (2 x 1/3H, d, J=15Hz), 5.03-5.19 (2H, a), 6.97 (2 x 1/3H, d, J=8Hz), 7.08 (2 x 2/3H, d, J=8Hz) , 7.13- 7.23 (5H, m) , 7.30 (IH, t, J=8Hz) , 7.43 (IH, t, J=8Hz), 7.49 (IH, s), 7.53-7.63 (IH, m) , 7.69 (2H, t, J=8Hz), 7.92 (2H, d, J=8Hz) , 8.20 (IH, t, J=8Hz) (83) MASS (FAB) (m/z) : 774 (M+H) + NMR (CDCI3, δ) : 1.25 (3H, t, J=8Hz) , 2.52-2.69 (5H, m), 2.62 (3 x 2/3H, s) , 2.79 (3 x 1/3H, s), 2.97- 3.11 (2H, m) , 3.20 (2H, s) , 3.31 (IK, t, J=8Hz) , 3.43-3.60 (2H, m) , 3.68-3.77 (2H, ) , 3.91 (3H, s), 4.13 (2H, q, J=8Hz) , 4.22-4.38 (2 x 2/3H, m) , 4.69 (2 x 1/3H, d, J=16Hz), 5.01-5.18 (2H, ) , 6.98 (2 x 1/3H, d, J=8HZ), 7.08 (2 x 2/3H, d, J=8Hz) , 7.12- 7.24 (5H, m) , 7.40 (2H, t, J=8Hz) 7.50 (IH, d, J=8Kz), 7.60-7.70 (2H, m) , 7.92 (2H, d, J=8Hz) , 8.23 (IH, t, J=8Hz) (84) MASS (FAB) (m/z) : 756 (M+H) + NMR (CDCI3, δ) : 1.25 (3H, t, J=8Hz) , 2.57-2.68 (5H, m) , 2.63 (3 x 2/3H, s) , 2.80 (3 x 1/3H, s), 2.97- 3.11 (2H, m), 3.22 (2H, s), 3.32 (IK, t, J=8Hz) , 3.47-3.63 (2H, m) , 3.68-3.75 (2H, m) , 3.90 (3K, s), 4.18 (2H, q, J=8Hz) , 4.22-4.41 (2 x 2/3H, a), 4.70 (2 x 1/3H, d, J=15Hz), 5.00-5.18 <2H, a), 7.00 (2 x 1/3H, d, J=8Hz), 7.09 (2 x 2/3H, d, J=8Hz) , 7.11- 7.23 (5H, m) , 7.38-7.47 (2H, a), 7.69 (1 x 1/3H, d, J=8Hz), 7.73 (1 x 2/3H, d, J=8Hz) , 7.80-7.δ9 (3H, m), 7.93 (2H, d, J=8Hz) , 8.10-8.15 (IH, m) (85) MASS (FAB) (m/z) : 739 (M+H) + NMR (CDC1 3 , δ) : 1.21 (3H, t, J=8Hz) , 2.43-2.58 (4H, a), 2.63 (3 x 2/3H, s), 2.67-2.74 (IH, a), 2.80 (3 x 1/3H, s), 2.92-3.10 (2H, m) , 3.16 (2H, s) , 3.21 (IH, t, J=8Hz), 3.40-3.52 (2H, m) , 3.58-3.73 (2H, m), 3.90 (3H, s) , 4.14 (2H, q, J=8Hz) , 4.28 (2 x 1/2H, d, J=8Hz), 4.73 (2 x 1/2H, d, J=15Hz) , 5.08- 5.28 (2H, m), 6.92-7.16 (8H, m) , 7.27 (2H, t, J=8Hz), 7.43 (IH, d, J=8Hz), 7.63 (IH, d, J=8Hz) , 7.89 (2H, d, J-8HZ), 8.01-8.10 (2H, m) (86) MASS (FAB) (m/z) : 716 (M+H) + NMR (CDCI3, δ) : 1.23 (3H, t, J=8Hz) , 2.53-2.70 (5H, a), 2.62 (3 x 2/3H, s) , 2.81 (3 x 1/3H, s), 2.97- 3.11 (2H, m), 3.23 (2H, s) , 3.31 (IH, t, J=15Hz), 3.43-3.60 (2H, m) , 3.68-3.73 (2H, m) , 4.11-4.38 (2 x 2/3H, m), 4.18 (2H, q, J=8Hz) , 4.65 (2 x 1/3H, d, J=8Hz), 5.02-5.17 (2H, m) . 6.97 (2 x 1/3H, d, J=8Hz), 7.04 (2 x 2/3H, d, J=8Hz) , 7.11-7.21 (5H, a), 7.23-7.30 (3H, m) , 7.37-7.51 (3H, m) , 7.63 (IK, s), 7.64 (1 x 1/3H, d, J=8Hz) , 7.71 (1 x 2/3H, d, J=8Hz) , 8.21-8.27 (IH, m) (87) MASS (FAB) (m/z) : 698 (M+H) + NMR (CDCI3, δ) : 1.26 (3H, t, J=8Hz) , 2.56-2.69 (5H, m), 2.63 (3 x 2/3H, s) , 2.83 (3 x 1/3H, s), 2.97- 3.12 (2H, m) , 3.12 (2H, s) , 3.31 (IH, t, J=15Hz) , 3.48-3.62 (2H, a), 3.68-3.72 (2H, a), 4.17 (2H, q, J=8Hz), 4.20-4.41 (2 x 2/3H, m) , 4.65 (2 x 1/3H, d, J=15Hz), 4.98-5.13 (2H, ) , 6.98 (2 x 1/3K, d, J=8Hz), 7.08 (2 x 2/3H, d, J=8Hz) , 7.12-7.32 (8K, m) , 7.37-7.46 (2H, m) , 7.70 (1 x 1/3H, d, J=8Hz) , 7.73 (1 x 2/3H, d, J=8Hz) , 7.80-7.86 (3H, a), 3.13 (IH, d, J=8Hz) (88) MASS (FAB) (m/z) : 655 (M+H) ÷ NMR (CDC1 3 , δ) : 2.31 (3H, s) , 2.37-2.52 (4H, m) , 2.58-2.70 (IH, m) , 2.59 (3 x 2/3H, s), 2.81 (3 x 1/3H, s), 2.98-3.10 (2H, ) , 3.35 (IH, t, J=15Hz), 3.43-3.58 (2H, a), 3.67-3.72 (2H, a), 4.07-4.39 (2 x 2/3H, a), 4.63 (2 x 1/3H, d, J=15Hz) , 5.02-5.17 (2H, a), 6.97 (2 x 1/3H, d, J=8Hz), 7.07 (2 x 2/3H, d, J=8Hz), 7.12-7.22 (6H, m) , 7.24-7.32 (3H, m) , 7.63 (IH, s), 7.65-7.72 (2H, m) , 8.35-8.40 (IH, a), 8.62 (IH, s) (89) MASS (FAB) (m/z) : 653 (M+H) + NMR (CDC1 3 , δ) : 2.29 (3H, s) , 2.38-2.50 (4H, m) , 2.61 (3 x 2/3H, s), 2.58-2.70 (IH, m) , 2.81 (3 x 1/3K, s), 2.98 (6H, s), 3.02-3.08 (2H, m) , 3.25-3.35 (IH, m) , 3.42-3.58 (2H, m) , 3.64-3.72 (2H, m) , 4.13-4.38 (2 x 2/3H, m) , 4.65 (2 x 1/3H, d, J=15Hz) , 5.00- 5.16 (2H, ) , 6.89-7.08 (5H, m) , 7.13-7.22 (5H, a), 7.28-7.32 (2H, m) , 7.38-7.46 (2H, m) , 7.63 (1 x 1/3H, d, J=8Hz), 7.70 (1 x 2/3H, d, J=8Hz) , 8.10- 8.13 (IH, a) (90) MASS (FAB) (m/z) : 702 (M+H) + NMR (CDCI3, δ) : 2.31 (3H, s) , 2.38-2.50 (4H, m) , 2.60-2.72 (IK, m) , 2.65 (3 x 2/3H, s) , 2.82 (3 x 1/3H, s), 3.00-3.12 (2H, m) , 3.30-3.40 (IH, a). 3.45-3.58 (2H, m) , 3.63-3.72 (2H, m) , 3.93 (3K, s), 4.20-4.40 (2 x 2/3H, a), 4.69 (2 κ 1/3H, d, J=15Hz), 5.02-5.22 (2H, m) , 7.00 (2 x 1/3H, d, J=8Hz), 7.10 (2 x 2/3H, d, J=8Hz) , 7.14-7.32 (5H, a), 7.38-7.53 (3H, a), 7.60-7.72 (2H, a), 7.90-8.00 (2H, a), 8.22-8.30 (IH, a) (91) MASS (FAB) (m/z) : 684 (M+H) + NMR (CDC1 3 , δ) : 2.28 (3H, s) , 2.32-2.50 (4H, m) , 2.58-2.70 (IH, m) , 2.66 (3 x 2/3H, s), 2.81 (3 x 1/3H, s), 2.97-3.11 (2H, m) , 3.31 (IK, t, J=15Hz) , 3.44-3.58 (2H, ) , 3.62-3.70 (2H, m) , 3.90 (3H, s), 4.23-4.41 (2 x 2/3H, m) , 4.69 (2 x 1/3H, d, J=15Hz), 5.00-5.18 (2H, m) , 7.01 (2 x 1/3H, d, J=8Hz), 7.09 (2 x 2/3H, d, J=8Hz) , 7.12-7.22 (5H, m) , 7.38-7.47 (2H, m) , 7.70-7.88 (4H, m) , 7.92 (2H, d, J=8Hz), 8.12-8.18 (IH, m) (92) MASS (FAB) (m/z) : 667 (M+H) + NMR (CDCI3, δ) : 2.20 (3H, s) , 2.27-2.42 (4H, m) , 2.62 (3 x 2/3H, s), 2.67-2.76 (IH, m) , 2.79 (3 x 1/3H, s), 2.93-3.10 (2H, a), 3.22 (IH, dd, J=15, 5Hz) , 3.32-3.47 (2H, a), 3.52-3.70 (2H, m) , 3.90 (3H, s) , 4.22 (2 x 1/3H, d, J=15Hz) , 4.29 (2 x 1/3H, d, J=18Hz), 4.72 (2 x 1/3H, d, J=15Hz) , 5.09-5.30 (2H, m) , 6.92-7.03 (4H, a), 7.04-7.18 (4H, m) , 7.22 (2H, t, J=8Hz) , 7.42 (IH, d, J=8Hz), 7.66 (IH, d, J=8H Z ), 7.90 (2H, d, J=8Hz) , 8.07-8.19 (2H, m) Example 11 The following object compounds were obtained according to a similar manner to that of Example 3. (1) MASS (m/z) : 667 (M+H) + NMR (CDCI3, δ) : 2.34 (6H, s) , 2.42-2.78 (9H, m) , 2.61 (2/3 x 3H, s) , 2.81 (1/3 x 3H, s) , 2.93-3.15 (2H, m) , 3.22-3.40 (IH, m) , 3.40-3.75 (4H, m) , 4.25 (1/3 x 2H, ABq, Δ=0.18, J=17Hz) , 4.29 (2/3 x IH, d, J=15Hz), 4.65 (2/3 x IH, d, J=15Hz) , 5.00-5.22 (2H, m) , 6.85-7.78 (16H, m) , 8.15-8.25 (IH, m) (2) MASS (m/z) : 696 (M + +l) NMR (CDC1 3 , δ) : 1.45 (9H, s) , 2.62 (3H x 2/3, s), 2.67 (IH, m) , 2.82 (3H x 1/3, s) , 3.04 (2H, m) , 3.28 (IH, m) , 3.44 (6H, m) , 3.62 (2H, m) , 4.14 (IH x 1/3, d, J=16Hz), 4.29 (IH x 2/3, d, J=15Hz) , 4.37 (IH x 1/3, d, J=16Hz), 4.63 (IH x 2/3, d, J=15Hz) , 5.11 (2H, m) , 6.96-7.33 (11H, ) , 7.44 (IH, t, J=8Hz), 7.50 (IH, s), 7.56 (IH, d, J=8Hz) , 7.67 (2H, m), 8.19 (IH, d, J=8Hz) (3) MASS (FAB) (m/z) : 600 (M+H) + NMR (DMSO-d 6 , δ) : 2.55-2.67 (2H, m) , 2.74 (3 x 1/3H, S), 2.82 (3 x 2/3H, s) , 2.84-3.03 (2H, m) , 3.42 (2H, t, J=5Hz), 3.64-3.75 (IH, m) , 4.37 (2 x 1/3H, d, J=15Hz), 4.53 (2 x 2/3H, d, J=15Hz) , 4.57-4.63 (2H, m) , 4.80-5.01 (2H, a), 7.03-7.10 (4H, m) , 7.13-7.30 (9H, a), 7.45 (IH, d, J=8Hz) , 7.63 (2H, t, J=8Hz), 8.32 (1 x 2/3H, d, J=8Hz) , 8.39 (1 x 1/3H, d, J=8Hz), 8.49 (IH, t, J=8Hz) (4) MASS (FAB) (m/z) : 653 (M+H) + NMR (CDCI3, δ) : 1.66-1.73 (2H, m) , 2.37-2.50 (4H, m) , 2.55 (2H, t, J=5Hz), 2.60 (3 x 2/3H, s) , 2.59-2.72 (IH, m) , 2.81 (3 x 1/3H, s) , 3.02 (2H, d, J=8Hz) , 3.18-3.27 (IH, m) , 3.40-3.47 (2H, m) , 3.59-3.65 (2H, m), 3.76 (2H, t, J=5Hz) , 4.18-4.38 (2 x 2/3H, m) , 4.69 (2 x 1/3H, d, J=15Hz) , 5.11-5.22 (2H, m) , 6.96-7.17 (13H, a) , 7.43 (IH, d, J=8Hz), 7.63 (IH, d, J=8Hz), 7.93-8.08 (2H, a) ( 5 ) MASS ( FAB) (m/ z ) : 682 (M+H) + NMR (CDC1 3 , δ) : 1.23 (3H, t, J=8Hz) , 2.52-2.66 (4H, m) , 2.58 (3 x 2/3H, s) , 2.67 (IH, dd, J=15, 8Hz) , 2.81 (3 x 1/3H, s), 2.97-3.11 (2H, a) , 3.20 (2H, S), 3.31 (IH, t, J=15Hz), 3.47-3.62 (2H, m) , 3.70- 3.74 (2H, m) , 4.18 (2H, q, J=8Hz) , 4.20-4.38 (2 x 2/3H, m) , 4.66 (2 x 1/3H, d, J=15Hz) , 5.02-5.18 (2H, m) , 6.96 (2 x 1/3H, d, J=8Hz) , 7.06 (2 x 2/3H, d, J=8Hz), 7.14-7.21 (6H, m) , 7.25-7.32 (3H, m) , 7.43 (IH, t, J=8Hz), 7.50 (IH, s), 7.57 (IH, d, J=8Hz), 7.63-7.72 (2H, a) , 8.18-8.22 (IH, m) (6) MASS (FAB) (m/z) : 631 (M+H) + NMR (CDC1 3 , δ) : 2.68-2.80 (IH, m) , 2.70 (3 x 2/3H, s), 2.84 (3 x 1/3H, s) , 2.90-3.08 (3H, a) , 3.70- 3.83 (6H, a), 4.28 (2 x 1/3H, d, J=15Hz) , 4.43-4.68 (2 x 2/3H, a), 4.54 (3H, br s) , 5.03-5.19 (2H, m) , 7.02-7.05 (4H, a) , 7.09-7.16 (4H, a), 7.23-7.33 (4H, a), 7.39 (IH, t, J=8Hz) , 7.46 (2H, t, J=8Hz) , 7.62 (IH, d, J=8Hz) , 7.92 (1 x 1/3H, d, J=8Hz) , 8.00 (1 x 2/3H, d, J=8Hz) , 8.14 (IH, d, J=8Hz) (7) MASS (FAB) (a/z) : 630 (M+H) + NMR (CDC1 3 , δ) : 2.68-2.75 (IH, a), 2.77 (3 x 2/3H, s), 2.84-3.08 (3H, m) , 2.92 (3 x 1/3H, s) , 3.65- 3.77 (6H, m) , 4.24-4.52 (2 x 2/3H, m) , 4.81 (2 x 1/3H, d, J=15Hz), 5.10-5.40 (2H, m) , 6.96-7.14 (11H, m) , 7.23-7.33 (3H, a), 7.43 (IH, d, J=8Hz) , 7.64 (IH, d, J=8Hz), 7.92 (IH, t, J=8Hz) , 8.27 (1 x 1/3H, d, J=8Hz), 8.37 (1 x 2/3H, d, J=8Hz) (8) MASS (FAB) (m/z) : 601 (M+H) + NMR (CDCI3, δ) : 2.67 (3 x 2/3H, s) , 2.62-2.81 (2H, a), 2.81 (3 x 1/3H, s) , 2.88-3.07 (3H, a), 3.75- 3.90 (4H, a), 3.99-4.08 (IH, a), 4.19-4.47 (2 x 2/3H, m) , 4.21 (IH, br s), 4.33 (IH, br s), 4.70 (2 x 1/3H, d, J=15Hz), 5.02-5.10 (IH, m) , 5.12-5.21 (IH, a), 7.00 (3H, t, J=8Hz) , 7.09-7.15 (3H, m) , 7.21-7.27 (4H, m) , 7.30-7.49 (4H, m) , 7.57 (IH, t, J=8Hz), 8.03 (1 x 1/3H, d, J=8Hz) , 8.12 (1 x 2/3H, d, J=8Hz), 8.21-8.23 (IH, m) (9) MASS (ESI) (m/z) : 510 (M+l) NMR (CDC1 3 , δ) : 1.99 (IH, dd, J=25, 8Hz) , 2.61 (IH, dd, J=25, 8Hz), 2.80-3.12 (4H, m) , 2.86 (3 x 2/3H, s), 2.92 (3 x 1/3H, s) , 3.05 (3H, s) , 3.49 (2H, d, J=8Hz), 3.51-3.72 (IH, m) , 4.00 (IH, q, J=8Hz) , 4.22-4.34 (2H, m) , 4.52-4.70 (3H, a) , 5.20-5.28 (2H, a), 6.58 (IH, d, J=8Hz) , 7.07 (2H, d, J=8Hz) , 7.16-7.32 (7H, a), 7.40-7.66 (7H, a) Example 12 To a solution of Starting Coapound (107 ag) in dichloroaethane (5 al) was added (benzo[b] furan-2- yl)isocyanate (50 ag) at rooa teaperature and stirred for 1 hour. Purification by column chromatography (silica gel, chloroform-methanol) afforded Object Compound (140 mg) as white powders. MASS (m/z) : 625 (M+H) + NMR (CDC1 3 , δ) : 2.28 (3H, s) , 2.30-2.48 (4H, ) , 2.55 (2/3 x 3H, s), 2.65-2.82 (IH, m) , 2.78 (1/3 x 3H, s), 2.95-3.15 (2H, m) , 3.22-3.72 (4H, m) , 4.14 (2/3 X IH, d, J=15HZ), 4.22 (1/3 x 2H, ABq, Δ=0.16, J=17Hz), 4.65 (2/3 x IH, d, J=15Hz) , 4.78-4.95 (IH, m) , 5.05-5.22 (IH, m) , 6.44 (IH, s), 6.82-7.82 (16H, m) , 8.35-8.55 (2H, a) Example 13 Starting Coapound (387 ag) and benzo[b]furan-2- carboxaldehyde (99 ag) were dissolved in benzene (10 al) and heated to reflux for 2 hours. After the mixture was allowed to cool to room temperature, the solvent was evaporated and the remaining solid was redissolved in methanol (1 mi) . To this solution was added sodium cyanoborohydride (45 mg) at room temperature, and added some drops of hydrogen chloriae- methanol to adjust the solution to about pH 4. The reaction mixture was stirred at the room temperature for 2 days. The mixture was evaporated, added aqueous sodium hydrogen carbonate, and eκtracted three times with chloroform. The organic layer was washed with brine and dried over magnesium sulfate. Evaporation of the solvent followed by subjecting to column chromatography (silica gel, chloroform-methanol) gave Object Compound (248 mg) as a viscous oil. MASS (m/z) : 596 (M+H) + NMR (CDC1 3 , δ) : 2.25 (3H, s) , 2.25-2.78 (7K, m) , 2.68 (2/3 κ 3H, s), 2.85 (1/3 x 3H, s), 2.90-3.15 (2H, m) , 3.25-3.68 (4H, m) , 3.83 (2/3 x 2H, s), 3.90 (1/3 κ 2H, ABq, Δ=0.12, J=17Hz) , 4.35 (2/3 κ IH, d, J=15Hz), 4.38 (1/3 κ 2H, s), 4.70 (2/3 κ IH, d, J=15Hz), 5.05-5.22 (IH, m) , 6.55 (1/3 κ IH, s) , 6.60 (2/3 x IH, s), 6.93-7.56 (15H, a), 3.02-8.22 (IH, m) Example 14 Starting Compound (53 mg) was dissolved in N,N- dimethylformamide (1 ml) . Pyridinium chloride (98 mg) was added to the solution, and the mixture was stirred at room temperature for 2.5 hours. The solvent was evaporated, and the remaining oil was dissolved in ethyl acetate. The solution was washed twice with aqueous sodium hydrogen carbonate and dried over magnesium sulfate. Evaporation of the solvent followed by subjecting to column chromatography (silica gel, chloroform-methanol) afforded Object Compound (24 mg) as white powder. MASS (m/z) : 586 (M+H) " NMR (CDCI3, δ) : 2.58-3.20 (3H, m) , 2.88 (1/3 κ 3K, s), 3.01 (2/3 x 3H, s), 3.28-3.80 (9H, m) , 4.27 (2/3 x IH, d, J=15H∑), 4.62 (1/3 x 2H, ABq, Δ=0.09, J=17Hz), 4.80 (2/3 κ IH, d, J=15Hz) , 4.98-5.35 (2H, m) , 6.45-8.22 (15H, a), 8.65 (IH, br s) Example 15 Starting Coapound (347 mg) was dissolved in a mixture of 15% aqueous sodium hydroκide (I ml) and ethanol (2 ml), and the solution was stirred at room temperature for 1 hour. The solution was acidified by adding 6N hydrochloric acid and extracted three times with chloroform. The organic layer was dried over sodium sulfate. Purification by column chromatography (silica gel, chloroform-methanol) gave Object Compound (151 mg) as white powder. MASS (m/z) : 640 (M+H) + NMR (CDCI3, δ) : 2.55-2.70 (IH, m) , 2.73 (2/3 x 3H, s), 2.88 (1/3 κ 3H, s), 2.92-3.75 (11H, m) , 4.22 (1/3 κ IH, d, J=17Kz), 4.28 (2/3 κ IH, d, J=15Hz) , 4.55 (1/3 x IH, d, J=17Hz) , 4.62 (2/3 x IH, d, J=15Hz), 5.02-5.35 (2H, m) , 6.75-8.45 (17H, m) Example 16 Starting Compound (155 mg) , N- (2-chloroethyl) - dimethylamine hydrochloride (62 mg) , and potassium carbonate were mixed in N,N-dimethylformamide (0.5 ml) and heated to 50°C for 8 hours. The reaction mixture was diluted with ethyl acetate, washed twice with aqueous sodium hydrogencarbonate, twice with aqueous sodium hydroxide, once with brine, and dried over magnesium sulfate. Purification by column chromatography (chloroform-methanol) gave Object Compound (32 mg) as white powder. MASS (m/z) : 684 (M+H) + NMR (CDCI3, δ) : 2.34 (6H, S) , 2.58 (2/3 x 3H, s), 2.58-2.80 (3H, m) , 2.78 (1/3 x 3H, s) , 2.95-3.12 96/16981 - 600 - ( 2H, m ) , 3.23-3.39 (IH, a) , 3.39-3.80 ( 8H, m ) , 4.00-4.10 ( 2H, m), 4.02 (1/3 κ IK, d, J=17Hz ) , 4.22 ( 2/3 x IH, d, J=15HZ), 4.31 (1/3 x IK, d , J=17Hz ) , 4.59 ( 2/3 x IH, d, J=15Hz), 5.02-5.20 ( 2H, m ) , 6.68-7.75 (15H, a), 8.15-8.26 ( IH, m ) Tr.y m lp 17 To a solution of Starting Compound ( 92 mg ) in dichloromethane ( 0.5 ml) was added lodomethane ( 100 mg ) at room temperature and stirred for 12 hours. Ether was added to the mixture, and pale-yellow precipitate formed was removed by filtration and dried in vacuo to give Ob j ect Compound (103 mg) . MASS (m/z) : 624 (M-I )+ NMR ( CDC1 3 , δ ) : 2.70-2.88 (IH, m ) , 2.83 ( 3H, s ) , 2.90-3.25 ( 3H, m) , 3.25-4.18 (14H, m ) , 4.45 ( 2/3 x 2H, ABq, Δ =0.05, J=15Hz) , 4.47 ( 1/3 κ 2H, ABq, Δ =0.18, J=17H Z) , 4.98-5.25 (2H, m) , 7.00-8.05 ( 17H, m) Eyam l 18 The following object compounds were obtained accord i ng to a similar manner to that of Preparation 10. (1) MA SS (FAB) (m/z) : 613 ( M + H ) + NMR ( CDCl 3 -DMSO-d 6 , δ) : 2.57-2.70 ( IH, m ) , 2. 7 2 ( 3 κ 1/3H, s ) 2.82 ( 3 x 2/3H, s) , 2.83-3.05 ( 3H, m ) , 3 38-3.45 ( 4H, m) , 3.49-3.53 (2H, m ) , 3.5 7 -3.60 ( 2H, m ) , 4.38-4.52 (2H, m) , 4.82-5.02 ( 2H, m ) , 5.29 ( 2H, 5) . 7.02-7.32 (11H, m) , 7.38 ( IH, s ) , 7.85 ( IH, s ) , 8.27-8.37 (IH, m) , 8.56-8. 6 4 ( IH, m ) ( 2) MASS (FAB) (m/z) : 625 ( M + H ) NMR ( CDCI3, δ ) : 2.29 (3H, s) , 2.33-2.49 ( 4H, m ) , 2.58-2.70 ( IH, m) , 2.63 (3 x 2/3H, s ) , 2.81 ( 3 x 1/3H, s), 2.97-3.11 (2H, a), 3.25-3.35 (IH, a) , 3.42-3.54 (2H, m) , 3.61-3.70 (2H, a), 4.08-4.38 (2 x 2/3H, a), 4.63 (2 x 1/3H, d, J=15Hz) , 5.01-5.18 (2H, m) , 6.81 (IH, dd, J=8, 2Hz) , 6.87 (IH, d, J=2Hz), 6.95 (2 x 1/3H, d, J=8Hz) , 7.06 (2 x 2/3H, d, J=8Hz), 7.12-7.22 (5H, a), 7.22-7.28 (3H, a), 7.30-7.33 (2H, a), 7.62-7.75 (IH, a), 8.10-8.15 (IH, a) Example 19 To an ethanol (5 ml) solution of Starting Compound (488 mg) was added ethanol (5 ml) solution of citric acid (169 mg) at room temperature. The mixture was concentrated to about 2 ml, and diluted with 300 ml of water. The water was removed by freeze dryer to give Object Compound (569 mg) as white powders. NMR (D 2 0, δ) : 2.65 (4H, ABq, Δ=0.12, J=16HZ) , 2.5-3.5 (18H, m) , 3.8-5.0 (4H, m) , 6.8-7.7 (17H, m) Example 20 The following object compounds were obtained according to a similar manner to that of Example 19. (1) NMR (D 2 0, δ) : 2.65 (6H, ABq, Δ=0.12, J=16Hz) , 2.5-3.5 (18H, m) , 3.8-4.9 (4H, m) , 6.6-7.6 (17H, m) (2) NMR (D 2 0, δ) : 2.73 (8H, ABq, Δ=0.12, J=16Hz) , 2.4-3.6 (18H, m) , 3.8-5.0 (4H, a), 6.5-7.5 (17H, m) (3) MASS (FAB) (m/z) : 668 NMR (CD 3 OD, δ) : 2.72-2.78 (5H, a), 2.83-2.87 (5E, ' a), 2.89-3.10 (6H, m) , 3.12-3.18 (2H, m) , 3.77-3.85 (3H, ) , 3.89 (3H, S), 4.48 (2 x 1/2H, d, J=15Hz) , 4.63 (2 x 1/2H, d, J=15Hz) , 4.98-5.15 (3H, m) , 7.12-7.24 (7H, ) , 7.33 (IH, t, J=8Hz) , 7.48 (IH, t , J=8Hz ) , 7 . 52 ( IH , s ) , 7 . 60 ( IH, d, J=8Hz ) , 7 . 73 ( IH, d, J=8Hz ) , 7 . 92 ( 2H, d, J=8Hz ) Example 21 The following object compound was obtained according to a similar manner to that of Preparation 3, 4 or 8. MASS (m/z) : 596 (M + +l) NMR (CDC1 3 , δ) : 2.61 (3H x 2/3, s) , 2.67 (IH, m) , 2.81 (3H κ 1/3, s), 2.86 (4H, m) , 3.05 (2H, m) , 3.31 (IH, m) , 3.44 (2H, m) , 3.63 (2H, a), 4.15 (IH κ 1/3, d, J=16Hz), 4.29 (IH κ 2/3, d, J=15Hz) , 4.35 (IH κ 1/3, d, J=16Hz), 4.64 (IH κ 2/3, d, J=15Hz) , 5.10 (2H, m) , 6.96 (2H x 1/3, a), 7.05 (2H x 2/3, m) , 7.17 (5H, s), 7.25-7.33 (5H, a), 7.43 (IH, t, J=8Hz), 7.50 (IH, s), 7.57 (IH, d, J=8Hz) , 7.66- 7.74 (2H, a) , 8.22 (IH, m) Example 22 To a solution of Starting Compound (1.0 g) in methanol (10 ml) was added dropwise 10% hydrochloric acid - methanol solution (1 ml) . Evaporation of solvent gave Object Compound (1.06 g) . NMR (CDC1 3 , δ) : 2.56 (3H κ 2/3, s) , 2.70 (3H x 1/3, s), 2.78 (2H, m) , 2.86 (3H x 1/3, s) , 2.93 (3H x 2/3, s), 3.00-3.24 (4H, a), 3.35-3.57 (3H, a), 3.65-3.91 (IH, a), 4.02-4.05 (IH, a), 4.38 (IH, d, J=15Hz), 4.55 (IH, d, J=15Hz), 4.63-4.75 (IK, a), 5.06 (IH, a), 5.06 (IH x 1/3, a), 5.28 (IH x 2/3, a), 7.05-7.33 (11H, a), 7.40-7.58 (4H, a), 7.67 (IH, d, J=8Hz), 7.76 (IH, t, J=4Hz) Example 3 The following object compound was obtained according to a similar manner to that of Preparation 10. MASS (FAB) (m/z) : 629 (M+H) " 96/16981 - 603 - NMR (CDCI3, δ) : 2.59-2 AC (IH, mj , 2.67 (3 x 2/3H, s), 2.81 (3 κ 1/3H, s), 3.04-3.14 !2H, mi , 3.39 (IH, dd, J=15, 5Hz), 3.44-3.51 (2H, a) , 3.60-3.78 (6H, m) , 4.11-4.42 [ 2 κ 2/3H, m) , 4.68 (2 x 1/3H, d, J=15Hz), 5.08-5.15 ( IH, a;, 5.23-5.32 (IK, ) , 6.93-7.03 (2H, m; , ".18-7.36 (9H, a) , ".51 (IH, a, J=8Hz), 7.71 (IK, t, J=8Hz), 7.95 ;1K, s'. , 3.22 (IH, d, J=8Hz) Example 24 The crude Object compound was obtained according to a similar manner to that of Exaaple 1. About 3C g of the product was obtained, and it was recrystallized from ethanol- water (2:1) to give 23.47 g of white crystals. ap : 92-93°C MASS : m/z 562 (M+H) + NMR (CDCI3, δ) : 2.59 (4/5 κ 3H, s), 2.77 (1/5 x 3H, s), 2.91 (2H, d, J=7Hz), 3.32 (IK, dd, J=14 and 7Hz), 3.47 (IH, dd, J=14 and 4Hz) , 4.11 (1/5 κ IH, a, J=16Hz), 4.27 (4/5 κ IH, d, J=15Hz) , 4.29 (1/5 x IH, d, J=16Hz), 4.60 (4/5 x IH, a, J=15Hz) , 5.02- 5.13 (2H, m) , 7.08-7.37 (10H, ) , 7.43 (IH, t, J=8Hz), 7.48 (IH, s), 7.55-7.69 (3H, a) , 8.18 (IH, a), 8.26 (1/5 x IH, d, J=2Hz), 8.3" (4/5 κ IH, d, J=2Hz), 8.51 (IH, a, J=4Hz) , 8.58 (IH, a, J=4Hz), 8.65 (IH, d, J=7Hz) Example 25 Object compounds were obtained according tc a similar manner to that of Eκampie 1 cr 24. (1) MASS : m/z 578 (M + AL) NMR (CDCI3, δ) : 2.60 (3H κ 3/4, s), 2.76 (3H κ 1/4, S), 2.87 (2H, d, J=7Hz) , 3.27 (IH, a), 3.42 (IH, 6981 - 604 - a) , 4.12 (IH x 1/4, d, J=I6Hz > , 4.29 (IH x 3/4, a, J=I5Hz), 4.32 (IH x 1/4, d, =16Hz " ι , 4.53 (IH x 3/4, d, J=l5Hz) , 4.97-5.13 .'2H, m, , ".09-7.29 (3H, a), 7.35- "* .45 (3H, a, , ".63 (IH, t, J=8Hz, , A 85- 7.83 (3H, m) , S.1C (IH κ 3/4, d, =5Hz) , 6.12 ;iH : 1/4, d, J=8Hz), Q J"5 / π, s 51 ; IH, a) , 3.57 IH, m) , 3.69 (IH, a =8H= \ 2 ) MASS : m/z 561 (M T +1; NMR (CDCI 3 , δ) : 2.64 (3H κ 3/4, s;, 2.31 (3H x 1/4, s), 2.82-3.05 (2H, a,, 3.2" (2H, a) , 4.1" (IH κ 1/4, d, J=l6Hz), 4.24 flH x 1/4, d, J=16Hz, , 4.36 (IH x 3/4, d, J=15Hz) , 4.53 (iH x 3/4, a, J=15Hz), 5.17 (IH, q, J=7Hz), 5.35 ( IH x 3/4, q, J=7Hz) , 5.44 (IH x 1/4, q, J=7Hz), 7.03-7.32 ' 12H, a! , 7.38-7.49 (2H, a) , 7.67 (IH, d, J=8Hz) , 8.22-3.71 (5H, a) MASS : a/z 599 (MAI) NMR (CDCI3, δ) : 2.51 (3H x 2/3, s;, 2.78 (3H x 1/3, s) , 2.89 (2H, a) , 3.26 (IH, a), 3.43 (IH x 2/3, a) , 3.47 (IH x 1/3, a) , 4.17 (2H x 1/3, s), 4.21 (IH κ 2/3, d, J=15Hz), 4.56 (IH κ 2/3, d, J=15Hz), 4.96- 5.08 (2H, m) , 6.81 (IH, d, J=8Hz) , 6.92 (IH, m) , 6.99-7.12 (8H, m) , 7.16 (IH, t, J=8Hz) , 7.24-7.32 (5H, ) , 7.35-7.50 (4H, a) , 7.64 (IH, d, J=3Hz) , 7.73 (IH, m) , 8.25 (IH x 2/3, br s), 8.35 (IH x 1/3, br s) 4) MASS : m/z 598 (M τ +1) NMR (CDCI3, δ) : 2.4ό(3H x 2/3, s), 2.8C (3H κ 1/3, s), 2.88-3.02 (2K, a), 3.21-3.37 (2H, m) , 3.75 (IH x 1/3, d, J=16Hz), 4.15 (IH x 2/3, a, J=15Hz) , 4.19 (IH κ 1/3, d, J=16Hz), 4.77 (IK κ 2/2, d, J=15Hz), 5.19 (IK, m) , 5.62-5.73 (IK, m) , 6.76 (IH, a) , /16981 - 605 - 6.90-7.26 (18H, a) , 7.47 ; IH, a, J= Hz; , ~ . ~ Ξ- ~ .6~ (3H, a) , 8.92 (IH, d, J=3Hz) (5) MASS : a/z 550 (M + ÷l) NMR (CDC1 3 , δ) : 2.65 (3H x 2/3, s), 2.83 (3H x 1/3, s), 2.93-3.02 (2H, a) , 3.12-3.31 (IH, a), 4.22 (IH κ 1/3, a, J=16Hz), 4.39 (IH x 1/3, a, J=16Hz, , 4.44 (IH x 2/3, a, J=15Hz), 4.58 {IK x 2/3, d, J=15Hz) , 4.95-5.13 (2H, a), 6.81 (IH, s), 7.01-7.08 (3H, a) , 7.13 (4H, s), 7.24-7.28 (5H, a) , 7.3: (IH, t, J=8Hz), 7.45-7.52 (3H, a), 7.62 (IH, br s), 7.96 (IH, br s), 8.20 (IH x 1/3, a, J=8Hz ' , 3.3C 'IK x 2/3, d, J=8Hz) (6) MASS : a/z 549 (M + AL) NMR (CDC1 3 , δ) : 2.67 (3H x 2/3, s), 2.91 (3H κ 1/3, s), 2.93-3.03 (2H, a), 3.16 (2H, a), 4.30 (IH x 2/3, d, J=15Hz), 4.31 (2H x 1/3, s), 4.80 (IH x 2/3, d, J=15Hz), 5.26 (IH, m) , 5.53 (IH, m) , 6.65 (IH, s), 6.90-7.1C (10H, m) , 7.19-7.27 (OH, a}, 7.45 (IH, a, J=8Hz), 7.62 (IH, d, J=8Hz), 7.6^ (IH, m) , 8.95 (IH, br s) (7) MASS : m/z 561 (M ÷ +l) NMR (CDCI3, δ) : 2.57 (3H x 2/3, s) , 2.80 (3H x 1/3, s), 2.87-2.98 (2H, a), 3.23-3.49 (2H, a) , 4.13 (IH x 1/3, d, J=16Hz), 4.28 (IH x 2/3, a, J=15Hz), 4.31 (IH x 1/3, d, J=16Hz), 4.60 (IH κ 2/3, a, J=15Hz 1 , 5.03-5.20 (2H, a), 6.92-7.31 (13K, a) , 7.38-7.67 (5H, a) , 8.17 (IH κ 2/3, d, J=SHz) , 8.33 (IH κ 1/3, a, J=8Kz), 8.52-8.62 (2H, a) (8) MASS : a/z 595 (M + ) NMR (CDCI3, δ) : 2.64 (3H x 5/6, s) , 2.75 (3H x 1/6, s) , 2.79-2.97 (2H, a) , 3.34 (2H, a) , 4.11 (IH x 1/6, d, J=I6Hz), 4.24 (IH x 1/6, a, J=lόHz , 4.34 (IH κ 5/6, d, J=15Hz) , 4.47 (IH κ 5/6, d, J=15Hz), 5.10-5.23 (2H, a), 7.02-7.26 (I2H, a , 7.44 (IH, dd, J=3, 10Hz), ".53 (IH, t, J=8Hz) , A 68 (IH, d, J=8Hz) , 3.08-3.33 (2H, a), 8.52 (2H, a, (9) MASS : a/z 612 (M + ) NMR (CDC1 3 , δ) : 2.62 (3H x 4/5, s), 2.74 (3H x l/5, s), 2.87 (2H, d, J=7Hz), 3.29 (IH, A , 3.43 (IH, a) , 4.10 (IH x 1/5, a, J=iόHz ; , 4.22 CH x 1/5, a, A16HZ), 4.27 (IH x 4/5, d, J=15Hz, , 4.52 (IH x 4/5, d, J=15Hz), 5.01 (IH, a, , 5.08 (IH, a) , 7.05- 7.33 (9H, a), 7.38-7.47 (2H, a), 7.63 (IH, a), 7.87-7.90 (3H, a), 8.07-S.24 (2H, a), 8.5 "* (IH, a), δ.6 "7 (IH x 1/5, d, J=8H∑), 8.73 (IH x 4/5, a, J=8Hz) (10) MASS : m/z 596 (M + ) NMR (CDCI3, δ) : 2.62 (3H x 5/6, s) , 2. A (3H κ 1/6, s), 2.91 (2H, d, J=7Hz) , 3.32 (IH, a), 3.45 (IH, a), 4.12 (IH κ 1/6, a, J=16Hz), 4.22 (IH κ 1/6, d, J=16H∑), 4.25 (IH κ 5/6, d, J=15Hz), 4.52 (IH κ 5/6, d, J=15Hz), 5.04-5.15 (2H, m) , 7.08-7.32 (10H, m) , 7.44 (IH, m) , 7.49 (IH, s), "7 .55 (IH, t, J=8Hz), 7.62-7.69 (2H, a), 5.03 (IH x 1/6, a) , 8.14 (IH x 5/6, aj , 8.22 {IK, d, J=8Hz' , 3.58-3.68 (2K, a) (11) MASS : a/z 578 (M + +l) NMR (CDCI3, δ) : 2.17 (3H x 3/4, s), 2.82 (3H x 1/4, s), 2.91-3.02 (2H, a), 3.20-3.47 (2H, a) , 4.16-4.55 (2H, m) , 4.93-5.22 (2H, a), 6.73-6.87 (2H, a) , 7.05-7.22 (6H, a), 7.37-7.45 (2H, a ) , A59-7.65 (IH, a), 7.84-7.88 (3H, a), 8.05-8.25 (IH, a), 8.33-8.71 (4H, a) (12) MASS : a/z 579 ( ' - l ) NMR (CDCI 3 , δ.- : 2.67 V 3H x 2/3, s), 2.61 :3H κ 1/3, s), 2.88-3.06 (2H, a, , 3.17-3.52 (2H, a), 4.21 (IH x 1/4, a, J=15Kz) , 4.37 (IH 1/4, a, J=15Hz), 4.35 (IH x 3/4, d, J=15Kz), 4.52 (IH x 3/4, a, J=15Hz) , 4.96-5.27 (2K, a), 6.74-6.86 (2K, a) , 7.03-7.25 (6H, m) , 7.46-7.64 (3H, m) , A 95 (IH, ai , 3.11-9.20 (5H, a) (13) MASS : 562 (MAD NMR (CDCI3, δ) : 2.68 (3H x 3/4, s) , 2.81 (3H κ 1/4, s), 2.88-3.05 (2H, a,, 3.13-3.48 (2H, m- , 4.22 (IH κ 1/4, d, J=15Hz), 4.34 (IH κ 3/4, a, J=15Hz), 4.35 (IH κ 1/4, d, J=15Hz), 4.53 (IH κ 3/4, d, J=15Hz), 4.94-5.25 (2H, a), 6.73-6.76 (2H κ 1/4, a), 6.86- 6.88 (2H x 3/4, a), 7.03-7.22 ( 6 ' ή, a) , 7.26-7.32 (2H, a), " 7.40-7.68 (5H, m) , 8.15-8.65 (5K, a) (14) MASS : a/z 561 (M ÷ AL) NMR (CDCI3, δ) : 2.67 (3H x 3/4, s), 2.83 (3H x 1/4, s), 2.77-3.06 (2H, a), 3.22-3.44 (2H, a), 4.13 (IH κ 1/4, d, J=15Hz), 4.25 (IH κ 3/4, a, J=15Hz), 4.42 (IH κ 1/4, d, J=15Hz), 4.63 (IH κ 3/4, d, J=15Hz), 4.98-5.40 (2H, a), 6.68-6.72 (2H x 1/4, a), 6.82- 6.84 (2H x 3/4, a), 6.97-7.23 (10H, a) , 7.37-7.53 (2H, a), 7.66-7.69 (IH, a), 8.24-8.62 (5H, a) (15) MASS : m/z 560 (M + A) NMR (CDCI3, δ) : 2.63 (3H x 3/4, s), 2.87 (3H x 1/4, s), 2.90-3.01 (2H, a), 3.32-3.37 (2H, a), 4.17 (IH κ 1/4, d, J=15Hz), 4.26 (IH x 3/4, a, J=15Hz), 4.72 (IH x 1/4, d, J=15Hz), 4.74 (IH x 3/4, a, J=15Hz) , 5.21 (IK, a), 5.46 (IH, a), 6.88-7.24 (15H, a), 7.37-7.48 (2H, a), 7.17-8.25 (IH, a), 8.40-8.61 (2H, a) Example 26 The following object compounds were obtained according to a similar manner to that of Eκample 1 or 24. (1) MASS : 530 (M+l) NMR (CDCI3, δ) : 2.15 (3 κ 1/3H, s), 2.17 (3 x 2/3H, s), 2.67 (3 x 2/3H, s) , 2.91 (3 x 1/3H, s) , 2.82- 3.13 (4H, m) , 4.12 (2 κ 1/6H, d, J=16Hz), 4.39 (2 κ 1/6H, d, J=16Hz), 4.41 (2 x 1/3H, d, J=15Hz': , 4.63 (2 κ 1/3H, d, J=15Hz), 4.78-4.88 (IH, a) , 5.17-5.23 (IH, a), 6.99-7.57 (16H, a), 7.70 (IH, d, J=8Hz) (2) MASS : 529 (M+l) NMR (CDCI3, δ) : 2.17 (3H, s) , 2.72 (3 κ 2/3H, s) , 2.98 (3 κ 1/3H, s) , 2.95-3.10 (4H, a) , 4.19 (2 κ 1/6H, d, J=16Hz) , 4.39 (2 κ 1/6H, d, J=16Hz) , 4.52 (2 κ 1/3H, d, J=15Hz) , 4.80 (2 κ 1/3H, d, J=15Hz) , 5.38-5.49 (IH, a), 5.60-5.70 (IH, a) , 6.97-7.18 (9H, a) , 7.21-7.33 (5H, a) , 7.51 (IH, d, J=8Hz) , 7.68 (IH, d, J=8Hz) , 9.10 (1 κ 1/3H, a, J=8Hz) , 9.15 (1 κ 2/3H, d, J=8Hz) (3) MASS : 535 (M+l) NMR (CDCI3, δ) : 2.73 (3 x 2/3H, s) , 2.80 (3 x I/3H, s), 2.99-3.16 (2H, a), 3.72-3.82 (IH, a) , 4.07-4.23 (2H, m) , 4.42 (2 κ 1/2H, d, J=15Hz) , 4.53 (2 κ 1/2H, d, J=15Hz), 4.82-4.90 (IH, m) , 5.11-5.20 (IH, m) , 7.09-7.31 (7H, m) , 7.32-7.45 (2H, m) , 7.50 (IH, d, J=8Hz), 7.51 (IH, s) , 7.57 (IH, t, J=8H=, , 7.63 (IH, d, J=8Hz) , 7.79 (IH, d, J=8Kz) , 8.15 (1 x 1/3H, s) , 8.20 (1 x 2/3H, s) (4) MASS : 551 (M+l) NMR (CDCI3, δ) : 2.69 (3 x 2/3H, s) , 2.78 (3 x 1/3K, s) , 2.98-3.14 (2H, m) , 3.73-3.82 (IH, m) , 4.06-4.14 (IH, m) , 4.18 (IH, t, J=8Hz), 4.00 (2 x 1/6H, d, J=16Hz), 4.41 (2 κ 1/6H, d, J=16Hz) , 4.38 (2 κ 1/3H, d, J=15Hz), 4.51 (2 x 1/3H, d, J=15Hz) , 4.80- 4.87 (IH, m) , 5.09-5.18 (IH, m) , 7.07-7.30 (6H, m) , 7.31-7.43 (4H, m) , 7.73-7.87 (4H, m) , 8.12 (1 x 1/3H, s) , 8.17 (1 x 2/3H, s) (5) MASS : 534 (M+l) NMR (CDC1 3 , δ) : 2.91 (3 x 1/4H, s) , 2.93 (3 x 3/4H, s), 3.01-3.25 (2H, m) , 3.91-4.08 (2H, m) , 4.09 (2 x 1/8H, d, J=16Hz), 4.30 (2 x 1/8H, d, J=16Hz) , 4.35 (2 x 3/8H*, d, J=15Hz), 4.65 (2 x 3/8H, d, J=15Hz) , 5.20-5.38 (2H, m) , 5.40-5.50 (1 x 1/4H, m) , 5.57- 5.73 (1 x 3/4H, m) , 6.81 (IH, d, J=8Hz) , 7.00 (IH, s) , 7.09-7.31 (9H, m) , 7.42 (IH, d, J=8Hz) , 7.68 (IH, d, J=8Hz) , 8.08 (1 x 1/4H, s) , 8.13 (1 x 3/4H, s) , 9.19 (IH, d, J=8Hz) (6) MASS : 758 (M+l) NMR (CDCI3, δ) : 2.61 (3 x 2/3H, s), 2.62-2.68 (IH, m) , 2.80 (3 x 1/3H, s) , 2.82-2.91 (IH, m) , 2.93- 3.04 (2H, m) , 4.20-4.30 (IH, m) , 4.12 (2 x 1/4H, d, J=16Hz), 4.22 (2 x 1/4H, d, J=16Hz) , 4.31 (2 x 1/4H, d, J=15Hz), 4.60 (2 x 1/4H, d, J=15Hz) , 5.11 (IH, q, J=15Hz), 6.69-7.71 (32H, m) (7) MASS : 774 (M+l) NMR (CDCI3, δ) : 2.58-2.63 (IH, m) , 2.61 (3 x 2/3H, s) , 2.77 (3 x 1/3H, s) , 2.81-3.06 (3H, m) , 4.10- 4.32 (IH, m) , 4.10 (2 x 1/4H, d, J=16Hz) , 4.22 (2 x 1/4H, d, J=16Hz) , 4.30 (2 x 1/4H, d, J=15Hz), 4.59 (2 x 1/4H, d, J=15Hz), 5.10 (IH, q, J=8Hz) , 6.59 (IH, t, J=8Hz), 6.78 (1 x 1/3H, d, J=8Hz) , 6.86 (1 x 2/3H, d, J=8Hz) , 6.90-7.20 (19H, a) , 7.39-7.46 (8H, m) , 7.68 (IH, d, J=8Hz) , 7.83 (2H, t, J=8Hz) (3) MASS : 5" (M-D NMR (CDC1 3 , δ) : 2.51-2.69 (2H. m; , 2. "2 (3 κ 2/3H, s), 2.90-3.06 (2H, ni , 2.98 (3 x i/?K, s- , 4.25 (2 x 1/3H, s) , 4.39 (2 x 1/3H, α, J=15H=) , 4.38 2 x 1/3H, a, J=15Hz), 5.22-5.37 ;2H, a , 6X8 (IH, d, J=3Hz) , 6.87-6.93 (2H, a), 6.9i- ~ .i (I3H, a , 7.20-A 40 (3H, m) , 7.51 (IH, d, J=3H:; , ".A 1 IH, d, J=8Hz) , 3.63 (IH, t, =8Hz) (9) MASS : 551 (M+D NMR (CDCI3, δ) : 2.82 (3 x 2/3H, s) , 2.91 (3 x I/3H, s), 3.01-3.2C (2H, a;, 3.73-3.3 " (IH, a' , " -4.19 (IH, a) , 4.32 (2 κ 1/6H, d, J=16Hzl , 4.63 (2 x 1/6H, d, J=16Hz) , 4.67 (2 κ 1/3H, a, J=15Hz, , 4.71 (2 κ 1/3H, d, J=15Hz), 4.61 (IH, fcr s) , 4.85-4.98 (IH, a), 5.17-5.33 (IH, a), 7.03-7.20 (5H, mi , 7.27 (IH, t, J=8Hz), 7.36-7.80 (8H, a), 7.33-7.94 (2H, a) , 3.08 (1 κ 2/3H, d, J=8Hz), 3.10 (1 κ 1/3H, a, J=3Hz) , 8.77 (IH, s) (10) MASS : 550 (M+l) NMR (CDCI3, δ) : 3.0C (3H, s), 3.04-3.2C (IH, ai , 3.20-3.32 (IH, m) , 3.93-4.13 (2H, a, , 4.22 (2 κ 1/6H, d, J=16Hz), 4.52 (2 x 1/3H, d, J=15Hz , 4.60 (2 x 1/6H, d, J=16Hz) , 4.92 (2 x 1/3K, d, =15HZ) , 5.30-5.50 (IH, m) , 5.58-5.77 (IH, a) , 6.58 (1 κ 1/4H, s), 6.73 (1 x 3/4H, ≤), 7.0C-7.32 (8H, ir.) , 7.33-7.49 (6K, mi , A 96 (IH, a, , 3.64 'IH, s), 9.23 (IH, a, : 8Hz) (11) MASS (a/z! : 590 (MAl) NMR (CDCI3, δ) : 2.90 (3H x 1/4, s) , 3.02 (3H x 3/4, s), 3.14 (IH, m) , 3.2S (IH, a) , 3.7C (IH, , . 3.92 (IK, a), 4.21-4.69 (4H, a) , 4.90 (IH, a), 5.22 (IH, a), 5.54 (IH, a), 6.92-7.2 " (14H, a), " .33- " .42 (2H, mj , 7.66 (IH, a, J=8Hz), 6.32-3.33 (2H, m) ;i2) MASS (m/z) : 589 (M ~ -i, NMR (CDC1 3 , δ) : 2.65 ( H x 2/3, s.' , 2.9C (3H x 1/3, S), 3.05 (2H, a), 3.77 (IH, a), 3.92 (IH, A , 4.14 (IH x 1/3, d, J=15Hz), 4.28 (IH x 2/3, d, J=15Hz), 4.38 (IH κ 1/3, a, J=15Hz), 4. ^ (IH, d, J=I5Hz), 4.54 (IH, d, J=15Hzϊ, 4.81 (IH x 2/3, d, J=15Hz), 5.34 (IH, q, J=7Hz), 5.47 (IH, a), c.92 (IH, a), 7.00 (IH, d, J=2Hz) , 7.06-^.33 (17K, a), 7.4" (IH, a, J=8Hz), 7.63 (IH, d, J=8H∑) , 3.64 (IH, a, J=8Hz) (13) MASS (a/z) : 500 (MAI) NMR (CDC1 3 , δ) : 2.94 (3K x 3/4, s;, 2.95 (3H x 1/4, s) , 3.11 (IH, dd, J=5, 12Hz) , 3.24 (IH, dd, J=7, 12Hz), 2.98 (2H, a), 4.36 (IH x 1/4, a, J=15Hz), 4.39 (IH κ 3/4, a, J=15Hz) , 4.48 (IK κ 1/4, a, J=15Hz), 4.79 (IH κ 3/4, a, J=15Kz) , 5.33 (IH, a), 5.57 (IH, a), 6.96 (2H, a), A 08-7.22 (9H, m , 7.47 (IH, d, J=8Hz) , 7.65 (IH, d, J=3Hz), 8.32 (IH, da, J=2, 6Hz), 8.36 (IH, d, J=2Hz), 9.05 (IH x 1/4, d, J=8Hz), 9.12 (IH x 3/4, a, J=6Hz; (14) MASS : 501 (M + +l) NMR (CDCI3, δ) : 2.77 (3H x 3/4, s), 2.85 (3H x 1/4, s), 3.06 (2H, a), 3.77 (IH, dd, J=7, 12Hz), 4.12 (IH, a), 4.25 (IH x 1/4, a, J=15Hz), 4.43 (IH κ 1/4, a, J=15Hz), 4.4" (IH x 3/4, d, J=15H∑) , 4.57 (IH x 3/4, d, J=15Hz) , 4.83 (IH, a; , 5.16 (IH, q, J=7Hz), 7.14 (4H, s), 7.18-7.72 (10H, a), 8.39 (IH x 1/4, d, J=2Hz), 8.42 (IH x 3/4, a, J=2Hz), 8.51 (IH, a) (15) MASS (a/z) : 517 (M ' +l) NMR (CDCI3, δ) : 2.77 (3H κ 3/4, s), 2.87 (3H κ 1/4, s), 3.04 (2H, m) , 3.72 (IH, m) , 3.89 (IH, m) , 4.13 (IH, a), 4.48 (IH x 3/4, d, J=15Hz) , 4.49 (IH x 1/4, d, J=15Hz), 4.52 (IH x 1/4, d, J=15Hz) , 4.58 (IH x 3/4, d, J=15Hz), 4.72 (IH, a), 5.12 (IH, q, J=7Hz), 7.11-7.51 (11H, m) , 7.80-7.87 (3H, a), 8.42 (IH x 1/4, d, J=2Hz), 8.45 (IH x 3/4, d, J=2Hz), 8.53 (IH, a) (16) MASS (m/z) : 518 (M + +l) NMR (CDC1 3 , δ) : 2.80 (3H x 4/5, s) , 2.88 (3H x 1/5, s), 2.97-3.15 (2H, a), 3.80 (IH, t, J=7Hz) , 4.08- 4.20 (2H, a), 4.34 (IH κ 1/5, d, J=15Hz) , 4.41 (IH x 1/5, d, J=15Hz), 4.46 (IH x 4/5, d, J=15Hz) , 4.55 (IH x 4/5, d, J=15Hz), 4.71-4.82 (IH, m) , 5.07 (IH x 1/5, q, J=7Hz), 5.22 (IH x 4/5, q, J=7Hz) , 6.64- 6.97 (2H, m) , 7.08-7.21 (5H, m) , 7.46-7.62 (3H, m) , 7.95 (IH, d, J=8Hz), 8.07 (IH, d, J=8Hz) , 8.04-8.32 (IH, m) , 8.49-8.52 (2H, m) (17) MASS (m/z) : 517 (M + +l) NMR (CDCI3, δ) : 2.77 (3H x 3/4, s), 2.85 (3H x 1/4, s), 2.95-3.14 (2H, m) , 3.72-3.81 (IH, m) , 4.08 (IH, dt, J=4, 12Hz), 4.27 (IH x 1/4, d, J=15Hz) , 4.37 (IH x 1/4, d, J=15Hz), 4.42 (IH x 3/4, d, J=15Hz) , 4.53 (IH x 3/4, d, J=15Hz) , 4.73-4.85 (IH, a), 5.05 (IH x 1/4, q, J=7Hz), 5.18 (IH x 3/4, q, J=7Hz) , 6.90-6.93 (2H, a), 7.07-7.21 (5H, a), 7.33-7.42 (3H, m) , 7.77-7.87 (4H, m) , 8.46-8.50 (2H, m) (18) MASS (m/z) : 500 (M + +l) NMR (CDCI3, δ) : 2.73 (3H x 3/4, s) , 2.89 (3H x 1/4, s), 2.97-3.17 (2H, m) , 3.83-4.02 (2H, m) , 4.10 (IH x 1/4, d, J=15Hz), 4.20 (IH x 1/4, d, J=15Hz) , 4.37 (IH x 3/4, d, J=15Hz), 4.57 (IH x 3/4, d, J=15Hz) , 5.10-5.18 (IH x 1/4, a), 5.35-5.42 (IH x 3/4, a). 5.50-5.57 (IH, a), 6.71 " (2H x 1/4, a, A^Hz , 6.33 (2H κ 3/4, d, J=7Hz) , 7.06-7.23 (8H, a), 7.37 (IH, d, J=8Hz), 7.56 (IH, d, J=8Hz) , 7.63 ( IH, a, J=8Hz), 8.37-8.40 (2H, a), 8.97-9.02 ; IH, a (19) MASS (a/z) : 501 (M τ +1) NMR (CDC1 3 , δ) : 2.80 (3H κ 3/4, s), 2.83 ,3H x 1/4, s), 2.95-3.15 (2H, a), 3.71-3.78 (IH, a), 4.11 (IH, dt, J=4, 12Hz), 4.35 (IH x 1/4, a, J=15Hz, , 4.40 (IH κ 1/4, d, J=15Hz) , 4.46 (IH κ 3/4, d, J=I5Hz), 4.56 (IH κ 3/4, d, J=15Hz), 4.72-4.65 (IH, a;, 5.06 (IH κ 1/4, q, J=7H∑), 5.21 (IH x 3/4, q, J="Hzi , 6.92-6.97 (2H, a), 7.07-7.21 (5H, a), 7.28- " .78 (7H, a) , 8.50-8.53 (2H, a) (20) MASS (a/z) : 525 (M + +l) NMR (CDCI3, δ) : 0.96 (6H, d, J=6Hz) , 1.54-1.80 (3H, a), 2.70 (3H x 1/3, s), 2.79 (3H κ 2/3, s) , 2.95- 3.11 (2H, a), 4.47 (IH κ 1/3, d, J=15Hz), 4.55 (IH κ 2/3, d, J=15Hz), 4.63 (IH κ 1/3, d, A15Hz), 4.73 (IH κ 2/3, d, J=15Hz), 5.42 (2H, a), 6.92-7.15 6H, a), 7.18-7.32 (4H, a), 7.51-7.66 (IH, a; (21) MASS (a/z) : 559 (M + +l) NMR (CDCI3, δ) : 2.69 (3H κ 2/3, s), 2.95 (3H κ 1/3, s) , 3.00 (2H, a), 3.21 (2H, t, J=7Hz), 4.22 (2H κ 1/3, s), 4.32 (IH κ 2/3, d, J=15Hz), 4.91 (IH x 2/3, d, J=15Hz), 5.31 (IH, a), 5.76 (IH, a; , 6.92- 7.15 (14H, a), 7.20-7.31 (5H, a), 7.43 (IH, a, J=3Hz), 7.68 (IH, d, J=8Hz) , 8.94 (IK, a, J=3K∑) (22) MASS (a/z) : 660 (M + +l) NMR (CDCI3, δ) : 1.60-1.70 (2H, a), 1.80-1.93 (2H, a), 2.72 (3H x 1/3, s), 2.78 (3H x 2/3, s), 2.96-3.24 (4H, a), 4.23 {IH κ 1/3, d, J=15Hz), 4.42 (IH κ 2/3, d, J=15Hz), 4.63 ( IH x A3, d, =15Hz , 4 (IH κ 2/3, d, , 5.02 ,2H, ≤, , 5.32-5.42 (2H m) , ό.9 ~ -l.l ~ '10H, ai , ".21- " .31 .'9K, > , 7.47 i IH, d, J=8Hz', 7.66 ■ IH, dd, J=2, 8H= , 3.81 IK, br si (23) MASS (m/z, : 543 (MτKι NMR (CDC1 3 , δ) : 2.08 ' 3K, s), 2.10-2.32 ,2H, a , 2.57-2.63 (2H, a), 2. " 2 (3 x 2/3H, s , 3.05 '3 x 1/3H, s) , 3.00-3.0" (2H, a), 4.1c 2 x 1/4H, a, , 4.50 (2 y 1/4H, d, J=15Kz), 4.89 (2 x 1/4H, a, J=I5Hz , 5.34- 5.48 (IH, a), 5.52-5.63 (IK, a) , 6.93- "* .18 (9H, a) , "* .19-".37 (5H, a), 7.49 V 1H, a, J=8Hz , 7.69 (IH, d, J=8Hz), 9.08 (IH, t, J=8Hz) (24) MASS (a/z) : 560 (M-rH) NMR (CDC1 3 , δ) : 2.02-2.26 (2H, ; , 2.11 (3H, s), 2.57-2.63 (2H, a), 2.68 (3 x 2/3K, si , 2.69 (3 x 1/3H, s) , 2.99-3.12 (2H, a), 4.17 -2 x 1/4H, d, J=16Hz) , 4.41 (2 x 1/4H, d, J=16Hz), 4.42 (2 x 1/4H, a, J=15Hz), 4.62 (2 x 1/4H, a, J=15Hz , 4.90- 5.01 (IH, a), 5.17-5.27 (IH, a), 7.02-7.43 (13H, m) , 7.59 (IH, t, J=8Hz), A7S-".8 "? (3K, a) (25) MASS (m/z) : 544 (M-^H- NMR (CDCI3, δ) : 2.C8 (3E, d, J=3Kz;, 2.10-2.28 '2H, a) , 2.53-2.63 (2H, a) , 2.68 (3 x 2/3H, s) , 2.92 X x 1/3H, s) , 2.98-3.12 (2H, a) , 4.19 '2 x 1/4H, a, J=16Hz), 4.40 (2 κ 1/4H, a, , 4.46 (2 κ 1/4K, d, J=15Hz), 4.63 (2 κ 1/4H, d, J=15Hz), 4.89- 5. CO (IH, a) , 5.18-5.23 'IH, a) , ".02-7.18 (7H, a) , 7.24-7.31 (4H, a) . A 39-".54 ^5K, a; , 7.69 ;iκ, a, J=8Hz) [26. MASS (a/z) : 500 (MA > NMR (CDCi-3, δi : 2. "3 (3 κ 2/3H, ≤, , 2.91 ;3 x 1/3H, s), 2.95-3.13 !2H, a. , 3.62-3.33 (2H, a) , 3.35 ( IH, t, J=8Hz), 4.03-4.1 " (IH, a), 4.27-4.56 (2 x 2/3H, a), 4.69 (2 x 1/3H, d, J=15Hzi, 4.72-4.79 (IH, m) , 5.12-5.22 (IH, a) , " .04-7.13 ;6K, a) , 7.26-7. S "7 (3H, m, , 7. C (2H, t, J=8Hz, , " .50 (IH, s,, A 52 (2H, t, J=8Hz. , 7.62 (IH, d, J=8Hz ' , (27) MASS (a/z) : 515 (MM) NMR (CDCI 3 , δ) : 2.50 (3H x 3/4, si , 2.53 (3H x 1/4, ≤) , 2.75 (3H x 3/4, si , 2.52 ; 3H x 1/4, s), 3.00- 3.15 (2H, m) , 3.81 (IH, a) , 4.10 (IH, a) , 4.05-4.14 (2H x 1/4, a) , 4.44 (IH x 3/4, d, J=15Hz) , 4.50 (IH x 3/4, a, J=15Hz), 4.79 (IH, br s), 4.94 (IH, a), 5.18 (IH, a), 7.C0-7.13 (6H, a), 7.25-7.66 (7H, a), 7.88 (IH x 1/4, d, J=8Hz) , 7.96 (IH x 3/4, d, J=8Hz), 8.28 (IH, d, J=2Hz) (28) MASS (a/z; : 514 (M + A) NMR (CDCI3, δ) : 2.41 (3H x 6/7, s), 2.53 (3H x 1/7, s) , 2.93 (3H, s), 3.10 (IH, dd, J=5, 12Hz) , 3.26 (IH, dd, J=7, 12Hz) , 3.97 (2H, a) , 4.28 (IH x 6/7, d, J=15Hz), 4.28 (IH x 1/7, d, J=i6Hz ' , 4.37 (IH x 1/7, d, J=16Hz), 4.78 (IH κ 6/7, d, J=15Hz) , 5.32 (IH, a), 5.64 (IH, a), 6.69 (IH, d, J=8Hz) , 6.88 (IH x 1/7, s), 6.92 (IH x 6/7, s), 7.04-7.25 (9H, a), 7.48 (IH, d, J=8Hz), 7.61 (IH κ 1/7, d, J=8Hz), 7.65 (IF. x 6/7, d, J=5Hz), 3.22 (IH, s; , 9.22 (IK x 1/7, d, J=8Hz) , 9.28 (IH κ 6/ " , a, J=8Kz) (29) MASS (a/z) : 513 (M~ l) NMR (CDC1 3 , δ) : 1.21 (3H x 1/3, a, J=7Hz), 1.24 (3H κ 2/3, d, J=7Hz), 2.76 (3H x 2/3, s) , 2.97 (3H x 1/3, s), 3.00-3.14 (2H, a), 3.92-4.83 (4r., a) , 5.26-5.41 (2H, a) , 7.C2-7.14 (8H, a) , " .16-7.31 (5K, m. , 7.38-".49 (2H, a), 7.65 (IH, a, J=8Hz > , 3.85 (IH κ 1/3, a, J=8Hzi , 3.93 (IH x 2/3, a, J=3Hz • (30) MASS (a/z) : 514 (M ~ -i ' NMR (CDC1 3 , δ) : 1.16 (3H x 1/3, a, , 1.21 ( 3H x 2/3, a, J=7KZ), 2.76 ,3H x 2/3, s>, 2.93 ( 3H x 1/3, si, 2.95-3.13 (2H, a) , 3.8^-3.97 (IH, ) , 4.28-4.75 (4H, a), 5.16 (IH, a) , ".05-7.16 [6r., _-. , ".21-7.32 (5H, a), A41-A69 (5H, a) NMR (CDC1 3 , δ) : 2.42 (3 κ 2/3H, s), 2.50 (3 x 1/5H, s) , 2.82-3.08 (2H, a), 3.23-3.42 (2H, a) , 3.47 (2 x I/3H, d, J=15H∑) , 3.70 (2 κ 1/6H, d, J=I6Hz, , 4.09 (2 κ I/6H, d, J=16Hz), 4.70 (2 κ 1/3H, a, J=15Hz), 5.10-5.30 (IH, a) , 5.80-6.00 (IH, a), 6.71-6.80 (2 x 1/3H, a), 6.83-6.92 (2 κ 2/3H, a), 6.93-7.30 (14H, a), 7.31-7.73 (7H, a) , 8.97 1H, d, J=3Hz) (32) MASS : 610 (M+l) NMR (CDC1 3 , δ) : 2.49 (3 x 2/2H, s), 2.63 (2 κ 1/3H, s), 2.85-3.05 (2H, a), 3.22-3.48 (2H, m, , 3.98 (2 κ 1/3H, d, J=15Hz), 4.07 (2 x 1/3H, si , 4.58 (2 x 1/3H, d, J=15Hz), 5.01-5.22 (2H, a) , 6.82-7.55 (19H, a) , 7.60-A7C (5H, a) (33 ' ι MASS : 564 (M+l) NMR (CDCI3, δ) : 2.51 (3 κ 1/4H, s) , 2.52 (3 x 3/4H, s), 2.72 (3 x 3/4H, s), 2.33 (3 κ 1/4H, si , 2.91- 3.08 (2H, a) , 3.10-3.26 (2H, a), 4.18 (2 κ 1/8H, a, J=16Hz), 4.29 (2 κ 1/8H, d, J=16Hz) , 4.30 (2 x 3/8H, d, J=15Hz), 4.72 (2 x 3/8H, d, J=15Hz) , 5.20- 5.35 (IK, a) , 5.42-5.6C (IH, a) , 6.69 (1 κ 3/4H, s), 6.72 (1 κ 1/4H, s) , 6.90-7.20 (8H, a), ".20- 7.30 (2H, m) , 7.32-7.58 (3H, a), 7.62 (IH, a, J=8H∑), 8.15 (1 κ 1/4H, s) , 8.21 (1 x 3/4H, s) , 8.92 (1 x 3/4H, d, J=8H∑), 9.00 (1 κ 1/4H, a, J=8H∑) (34) MASS : 565 (M+l) NMR (CDC1 3 , δ) : 2.53 (3H, s), 2.60 (3 x 3/4H, s) , 2.78 (3 κ 1/4H, s) , 2.90-3.07 (2H, a), 3.08-3.33 (2H, a), 3.99 (2 κ 1/8H, a, J=I6Hz), 4.31 (2 κ 1/3H, a, J=16Hz), 4.39 (2 κ 3/8K, d, J=15Hz, , 4.49 (2 κ 3/8H, d, J=15Hz), 4.95-5.18 (2H, a), 6.82 (IH, s), 7.00-7.30 (3H, a) , 7.39 (IH, t, J=8Hz) , 7.43-7.58 (3H, a), 7.62 (IH, d, J=8Hz), 8.00 ( IH, br s) , 8.20 (1 x 1/4H, s), 8.28 (1 x 3/4H, s), 8.36 (IH, br s) (35) MASS : 574 (M+l) NMR (CDCI3, δ) : 2.60-3.40 (4H, a), 2.71 (3H, s), 2.91 (3H, s), 4.32-4.60 (2 κ 2/3H, a) , 4.67 (2 κ 1/3H, s), 4.90-5.48 (2H, a), 6.85-7.48 (19H, a) , 7.49- 7.75 (2H, a) (36) MASS : 573 (M+l) NMR (CDCI3, δ) : 2.72 (3 x 2/3H, s) , 2.91 (3 x 1/3H, s), 2.85-3.14 (3H, a), 3.15-3.50 (IH, a), 3.29 (3 x 1/3H, s), 3.40 (3 x 2/3H, s) , 4.29 (2 x 1/3H, a, J=15H∑), 4.33 (2 x 1/6H, d, J=16Hz) , 4.61 (2 x 1/6H, d, J=16Hz), 4.79 (2 x 1/3H, a, J=15Hz; , 5.13- 5.30 (IH, a), 4.48-4.58 (1 x 1/2H, a), 4.60-4.72 (1 κ 1/2H, a), 6.70-6.82 (IH, m) , 6.85-7.20 (12H, a), 7.21-7.40 (5H, m) , 7.40-7.60 (IK, m) , 7.60-".72 (IH, m) , 8.07-8.17 (1 κ 1/2H, m) , 8.30-8.42 (1 κ 1/2H, m) (37) MASS : 612 (M+l) NMR (CDCI3, δ) : 2.67 (3 κ 4/5H, s) , 2.83 (3 κ 1/5K, si, 2.88-3.08 <'2H, a), 3.22-3.50 ZH, m. , 4.32 '2 κ 1/6H, d, J=16Hz) , 4.48 (2 x 1/3H, a, J=15Hz, , 4.51 (2 x I/6H, a, J=16Hz) , 4.78 (2 x 1/3H, a, J=15Hz) , 5.0A5.23 (2K, a), " .CO- " .21 ;6H, a , A22-A32 (2H, a), 7.40-7.80 ., 5H, m, , 7.91 , IH, s , 5.10 (IH, a, , 5.2 (1 x 3/4H, a, , 6.52-3.70 '2H, a. , 6. 2 ;IH, a, J=2Hz) (38) MASS : 610 (MAL) NMR (CDC1 3 , δ) : 2.63 (3 x 2/3H, s) , 2. =0-3.10 (2H, a) , 2.89 (3 x 1/3H, s) , 3.30-3.43 IH, m, , 4.36 (2 x 1/6H, a, J=16Hz), 4.43 (2 x 1/όH, a, J=16Hz), 4.59 (2 x 1/3H, d, A15Hz), 4.70 ;2 x 1/3H, d, =15Hz), 5.14-5.22 (IH, m) , 5.23-5.49 (IH, a! , 6.92-7.30 (11H, a), 7.32-7.53 (3H, a, , 7.62-7.8C (3H, m) , 7.90 (IH, s), 8.03-8.23 (IK, m) , 8.33-3.52 (2H, m) , 8.60 (1 x 1/4H, s), 3.72 . 1 x 3/4H, s) (39) MASS : 552 (M+l) NMR (CDC1 3 , δ) : 2.99-3.26 (2H, m) , 3.00 (3H, s) , 3.70- 3.83 (IH, m), 4.01-4.18 (IH, m) , 4.25 (IH, br s) , 4.79 (2 x 1/2H, a, J=15Hz) , 4.87-4.93 (IK, a), 4.97 (2 x 1/2H, a, J=15Hz), 5.20-5.38 (IH, a) , 7.03-7.20 (5H, a), 7.23-7.30 (IH, a), 7.40 (IH, t, J=8Hz) , 7.43 (IH, d, J=8Hz) , ~ .50 (IH, s) , ".53 (IK, a, J=8Hz) , 7.63 (IH, a, J=8Hzi , 7.7I-A81 ;3H, mi , 7.9 "* -8.05 (IK, a), 8.06-3.1" ( IH, a, , 8.30 (IH, s> (40) MASS : 551 (M+l) NMR (CDC1 3 , δ) : 3.04-3.30 (2H, a) , 3.C5 (3H, si , 3.90-4.08 (2K, m) , 4.49 (2 x 1/6K, a, -J=16HZ; , 4.62 (2 x 1/6H, d, J=16Hz), 4.79 (2 x 1/2H, a, J=15Hz ) , 4.99 (2 κ 1/3H, d, J=15Hz ' ι , 5.20 (IH, br sj , 5.27- 5.50 (IH, a), 5.60-5.73 (IH, a), 6 5 II κ 1/4K, s) , 6.81 (1 x 3/4H, s), 6.94-7.10 <'4H, mi, A12- 7.22 ( 4-ή, mi, 7.31 'IH, d, J=8Hzi, 7.42-A73 (4K, a), ^ . 9r2 (IK, a, J=6Hz) , 8.ci (1 x 1/4K, s), 6.69 (1 x 3/4H, s), 9. IS (IH, d, =8Hzi (41) MASS : 613 (M+l) NMR (CDC1 3 , c; : 2.80 ' 3 x 3/4H, s), 2.89-3. OC (2H, a) , 2.94 (3 x 1/4H, s), 3.22-3.5C (2H, a), 4.60 (2 x 1/3H, d, J=15Hz! , 4.59 (2 x 1/6H, a, J=16Kz'. , 4.69 (2 x 1/6H, a, J=16Hz) , 4.93 (2 x 1/3H, a, J=15Hz), 5.00-5.30 (2H, a), 6.99-7.20 (6H, a), 7.22-7.32 (2H, a), 7.42 (IH, t, J=8Hz) , 7.47 (IH, 5) , 7.52-7.70 (3H, a) , 7.72-7.80 (2H, a), 7.94-8.03 (IK, a) , 8.07-8.13 (IH, a), 3.27-8.39 (IH, ai , 3.49-8.63 (2H, a), 8.63 (1 κ 1/4H, s), 8.73 (1 κ 3/4H, s) (42) MASS : 612 (M+li NMR (CDC1 3 , δ) : 2.80-3.12 (2H, a), 2.85 (3 x 3/4, s), 2.93 (3 x 1/4H, s), 3.26-3. 0 (2H, a), 4.57 (2 x 1/6H, d, J=16Hz), 4.70 (2 κ 1/6H, a, J=16Hz), 4.71 (2 x 1/3K, a, J=15Hz), 4.89 (2 x 1/3H, a, J=15Hz), 5.19-5.41 (2H, a) , 6.90-7.23 (10H, a) , 7.33-7.50 (2H, m) , 7.63-7.80 (3H, ) , 7.97-8.03 (IH, a), 8.07-8.15 (IH, a), 8.22 (1 x 1/4H, d, J=8Hz ' , 3.33 (1 x 3/4H, d, J=8Hzi , 8.41 (1 x 3/4H, a, J=8Hz) , 3.50 (IH, a, J=5Hz), 8.61 (1 κ I/4H, s), 8.63 (1 κ 1/4H, a, J=3Hz), 3.70 (1 x 3/4H, s) (43) MASS : 602 (M+l) NMR (CDCI3, δ) : 2.87 (3 κ 4/SH, s), 2.94 (3 κ 1/4K, s), 2.92-3.33 (4H, a), 4.68 (2 κ 1/5H, s), 4.77 (2 κ 2/5K, d, J=15Hz), 4.83 (2 κ 2/5H, d, J=15Hz), 4.92-5.30 (2H, a), 6.82 (IH, s), 7.00-7.20 (5H, m) , 7.20-7.31 (2K, t, J=8Hz) , 7.33 (IK, t, J=8Kzi , 7.44-7.59 (3H, a), 7.62 (IK, a, J=5Hzi, 7.70-7.82 (2H, a) , 7.84-8.18 (2H, a) , 3.22-6.40 (IH, m; , 6.3" (IH, s) NMR (CDC1 3 , 5) : 2.78-3.30 ,4H,. ~. ) .. 2.9C (3 x 4/5H, s) , 3.01 (3 x 1/5H, s ] , 4.57 (2 x 1/6H, d, J=16Hz) , 4.78 (2 x 1/6H, d, J=16Hz), 4.80 (2 x 1/3H, a, J=15Hz), 4.88 (2 x I/3K, a, J=15Hz) , 5.22-5.60 (2H, ' a) , 6.69 (1 x 4/5H, s) , 6.71 (1 κ 1/5H, s) , 6.85- 7.2C (8H, a), 7.30-7.49 (2H, a) , 7.Ξ7 (IH, t, J=8HZ] , 7.62-7.82 (3H, a) , A 92-8.02 (IH, mi , 8.03- 8.12 (IH, a), 8.59 (1 κ 1/5H, s), 8.67 (1 x 4/5H, s) , 8.90-9.13 (IH, a) (45) MASS : 577 (M+i) NMR (CDC1 3 , δ) : 1.82 (IH, br ≤;, 2.97 (3 x 1/4H, s), 2.99 (3 x 3/4H, s), 3.07-3.19 ( IH, a), 3.20-3.30 (IH, a), 3.90-4.19 (2H, a) , 4.42 (2 κ 1/3H, a, 4.50 (2 κ 1/6H, d, J=16Hz) , 4.60 (2 κ 1/6H, d, J=16Hz) , 4.80 (2 κ 1/3H, d, J=15Hzi , 5.30- 5.40 (IH, a), 5.56-5.70 (IH, a) , 6.51 (1 κ 1/4H, s) , 6.71 (1 κ 3/4H, s), 7.C3-7.40 (9H, a) , 7.50 (IH, d, J=8Hz), 7.59 (IH, d, J=8Hz), 7.73 (IH, d, J=8Kz) , 7.80 (IH, t, J=8Hz), 8.08 (IH, a, J=8Hz) , 8.25-8.49 (2H, a), 8.6" (1 x 1/4K, a, 6.72 (I x 3/4H, d, J=2Kz), 9.10 (1 x I/4H, d, =3Hz, , 9.17 (1 x 3/4H, a, J=8Hz) (46) MASS : 578 (M+l) NMR (CDC1 3 , δ) : 1.92 (IH, br s), 2.75 (3 x 3/4H, s), 2.88 (3 κ 1/4H, s), 2.98-3.13 (2K, a), 3.70-3.32 (IH, a), 4.07-4.20 (IH, a), 4.23 (2 x 1/ β H, d, J=16Hz), 4.50 (2 x 1/3H, a, J=15Hz) , 4.55 (2 x 1/6H, d, =16Hz), 4.68 (2 x 1/3H, a, J=15Hz ' , 4.73- 4.90 (IH, a), 5.12-5.28 (IH, a , " .13- " .36 A-i, m 7.42 (IH, t, J=8Kz] , 7.4 ** - " .7C { 6K, - , , " .51 (IH, t, J=6H∑), 8.27-S.4C (2H, a, , 8.49 .1 x 1/4H, si, 8.51 (1 κ 3/4, si , 5.62-8.65 (IH, a (47) MASS : 636 (M+l) NMR (CDC1 3 , δ) : 2.68 (3 x 4/5H, s,' , 2. " 9-2.10 (2H, a), 2.83 (3 x 1/5H, s), 3.30-3.47 2H, a< , 4.19 (2 κ 1/6H∑, d, J=16Hz) , 4.3C 2 x 1/6H, d, =16HZ) , 4.43 (2 κ 1/3H, d, J=I5Hz,, 4.57 , 2 x 1/3H, a, J=15H∑), 5.11-5.28 (IH, a), 5.29-5.48 (IH, x) , 6.90-7.14 (8H, a) , A15-7.30 (2H, a,, 7.31-A52 (4H, m) , 7.52-7.60 (IH, a, , 7.67 (IH, d, J=8Kz) , 8.22-8.38 (2H, a.) , 3.40-8.53 (3H, __, . , 8.60-3.72 (IH, m) , 9.10-9.22 (IH, a) (48) MASS : 639 (M+l) NMR (CDCI3, δ) : 2.61 (3 κ 4/5H, s), 2.80 (3 κ 1/5H, s), 2.83-3.09 (2H, a), 3.28-3.50 (2H, a), 4.19 (2 κ 1/6H, d, , 4.40 (2 x 1/3H, d, J=15Hz>, 4.58 (2 x 1/3H, d, J=15Hz), 5.02-5.22 (2H, a), 7.05-7.33 (3H, a,, ~ .35-7.50 (4H, a), 7.51-7.70 (5H, a), 8.22 (IH, a, J=8Hz) , 8.28 (IH, d, J=8Hz), 3.38 (1 x 1/5H, s), 8.45 (1 x 4/5H, s), 8.56 (IH, a, J=2Kz) , 8.61 (IH, d, J=4Hz), 9.18 (IK, s) (49) MASS : 578 (M+l) NMR (CDCI3, δ) : 2.8C (3 x 3/4H, s), 2.69 (3 x 1/4K, s), 3.00-3.19 (2H, a) , 3. " 2-3.82 (IH, a, , 4.08-4.20 (IH, a), 4.21-4.33 , IH, a;, 4.13 (2 x 1/6K, a, J=16Hz), 4.24 (2 x 1/6H, d, J=16H∑i , 4.33 (2 x 1/3H, d, J=15Hz) , 4.59 (2 x 1/3H, a, J=15K=, , 4.78- 4.90 (IH, a), 5.12-5.26 (IH, a), A 11-7.22 (5H, a), 7.23-7.33 (IH, a,', 7.35-7.47 (3H, a), 7. 8-".60 (3H, m) , 7.62-7.73 (3H, a), 8.30 (IH, t, J=7Hz), 8.49 (1 x 1/4H, s), 8.51 (1 κ 3/4H, s), 8.65 (IH, br s) , 9.17 (IH, br s) (50) MASS (a/z) : 781 (M + +l) NMR (CDC1 3 , δ) : 1.30-1.57 (2H, a), 1.98 (2H, a), 2.18 (3H, s), 2.65 (3H, s), 2.78 (2H, a), 2.85 (6H, s), 3.04-3.23 (2H, a), 3.72-3.90 (2H, a), 3.85 (3H, s) , 4.88-4.93 (2H, a), 5.36 (IH, a), 6.42 (IH, a), 6.57 (IH, s), 7.03 (2H, d, J=8Hz) , 7.14-7.32 (9H, a), 7.41 (IH, t, J=8Hz), 7.47 (IH, s), 7.52 (IH, d, J=8Hz), 7.67 (IH, d, J=8Hz) (51) MASS (m/z) : 561 (M + +l) NMR (CDCI3, δ) : 2.60 (3H x 3/4, s), 2.82 (3H x 1/4, s), 2.99 (2H, d, J=7Hz), 3.20 (2H, m) , 4.12 (IH x 1/4, d, J=16Hz), 4.23 (IH x 1/4, d, J=16Hz) , 4.34 (IH x 3/4, d, J=15Hz), 4.62 (IH x 3/4, d, J=15Hz) , 5.03 (IH, m) , 5.11 (IH, m) , 7.09-7.15 (5H, a), 7.19-7.32 (9H, m) , 7.36-7.46 (2H, m) , 7.52 (IH, d, J=8Hz) , 7.53 (IH, s), 7.67 (IH, d, J=8Hz), 8.30 (IH x 1/4, br s), 8.41 (IH x 3/4, br s), 8.53 (IH, br s) (52) MASS (m/z) : 560 (M + +l) NMR (CDCI3, δ) : 2.69 (3H x 3/4, s) , 2.88 (3H x 1/4, s), 3.00 (2H, m) , 3.20 (2H, m) , 4.14 (IH κ 1/4, d, J=16Hz), 4.25 (IH x 1/4, d, J=16Hz) , 4.28 (IH x 3/4, d, J=15Hz), 4.85 (IH x 3/4, d, J=15Hz) , 5.30 (IH, m) , 5.73 (IH, a), 7.02-7.17 (14K, m) , 7.20- 7.31 (3H, m) , 7.45 (IH, d, J=8Hz) , 7.67 (IH, d, J=8Hz), 8.29 (IH x 1/4, br s), 8.43 (IH x 3/4, br s), 8.55 (IH, m) , 8.88 (IH x 3/4, d, J=7Hz), 9.03 (IH x 1/4, d, J=7Hz) (53) MASS (m/z) : 562 (M + +l) NMR (CDCA, δ: -.. O. (3rn κ i/4. '3H 74, s) , 2.96 (2H, a; , 3. A (2H, m) , 4.06 ; IH x J=16H∑), 4.27 (IH x 1/4, a, J=16Hz) , 4.35 (IH x 3/4, d, J=15Hz; , 4.62 (IH x 3/4, a, J=15Hz, , 5.07 (2H, a) , 7.04-7.17 (7H, a) , 7.20-7.51 I6ii, r.] , 7.6: (IH, d, J=8Hz), 6.30-3.53 . ' 4H, a; (54) MASS (a/z) : 561 (M~Vl, NMR (CDC1 3 , δi : 2.65 (3H x 3/4, ε,, 2.94 '3K x 1/4, s), 2.98 (2H, a) , 3.20 (2K, a) , 4.07 (IH x 1/4, a, J=I6Hz) , 4.22 (IH x 1/4, a, J=16Hz) , 4.30 (IH x 3/4, d, J=15Hz) , 4.89 (IH x 3/4, α, J=15Hz) , 5.29 (IK, σ, =7Hz) , 5.63 (IH, q, J=7Hz) , 7.0 "" -7.15 (10H, a), 7.21-A 44 (4K, a), 7.67 ( IH, a, J=3Hz) , 8.32-8.57 (4H, a) , 3.91 (IH x 3/4, d, =8H∑i , 9.03 (IK x 1/4, d, J=8Hz) (55) MASS (a/z) : 567 (M + +l) NMR (CDCI3, δ) : 2.80 (3H κ 3/4, s) , 2.88 (3H κ 1/4, s) , 3.08 (2H, a) , 3.76 (IH, a) , 4.07-4.18 (2H, a) , 4.24 (IH x 1/4, a, J=16Hz), 4.53 (IH x 3/4, d, J=15Hz) , 4.53 (IH κ 1/4, a, J=16Hz) , 4.62 (IH x 3/4, d, J=15Hz) , 4.82 (IH, a), 5.21 (IH, q, J=7Hz) , 7.15-7.32 (7H, a), 7.42 (IH, t, J=8Hz) , ~ .49-7.71 (7H, a) , 8.10 (IK, s) , 8.55 (IH x 3/4, s) , 3.56 (IK κ 1/4, s) (56) MASS (a/z λ : 566 (M~-l) NMR (CDCI3, δ) : 2.70 (3H κ 3/4, s) , 2.83 (3H x 1/4, s) , 3.09 (2H, a) , 3.97 (2H, a), 4.C1 (IH κ 1/4, d, J=I6Hz), 4.27 (IH κ 1/4, d, J=16H∑) , 4.45 (IH κ 3/4, d, J=15Hz), 4.60 (IK x 3/4, d, J=15Hz, , 5.36 (IH, a) , 5.61 (IH, m) , 6.90-7.22 (11H, m) , A37- 7.46 (3H, m) , 7.55 (IK x 3/4, d, J=SHz) , 7.62 (IH, d, J=8Hz), 7.75 (IH κ 1/4, d, J=8Hz;, 8.02 (IH κ 1/4, s), 8.06 (IH x 3/4, s), 8.46 (IH x 3/4, s), 8.61 (IH x 1/4, s), 9.00 (IH x 3/4, d, J=8H∑), 9.11 (IH κ 1/4, d, J=8Hz) (57) MASS (m/z) : 559 (M+l) + NMR (CDC1 3 , δ) : 2.04-2.21 (2H, m) , 2.12 (3H, s) , 2.52 (3H, s), 2.61 (2H, m) , 2.67 (3H κ 4/5, s) , 2.81 (3H κ 1/5, s), 3.02 (2H, d, J=7.0Kz), 4.40 (IH, d, J=14.5H∑), 4.54 (IK, d, J=14.5Hz), 4.84 (IH, m) , 5.09-5.26 (IH, m) , 6.98-7.08 (IH, a), 7.09-7.56 (12H, a), 7.69 (IH, d, J=7.5Hz), 8.24 (IH x 1/5, d, J=1.5Hz), 8.33 (IH x 4/5, d, J=1.5Hz) (58) MASS (m/z) : 553 (M+l) + NMR (CDCI3, δ) : 2.10 (3H, s), 2.19 (2H, m) , 2.51-2.68 (2H, m) , 2.56 (3H κ 1/4, s), 2.58 (3H κ 3/4, s), 2.76 (3H x 3/4, s) , 2.98 (3H x 1/4, s), 3.03 (2H, d, J=7.5Hz), 4.53 (IH, d, J=14.5Hz), 4.68 (IH, d, J=14.5Hz), 5.29-5.49 (2H, a), 6.98-7.03 (IH, a), 7.04-7.19 (9H, m) , 7.22-7.37 (2H, m) , 7.49 (IH, d, J=7.5Hz), 7.70 (IH, d, J=7.5Hz), 8.26 (IH κ 1/4, d, J=1.5Hz), 8.37 (IH x 3/4, d, J=1.5Hz), 8.64 (IH, br d, J=7.5Hz) (59) MASS (m/z) : 545 (M+l) ÷ NMR (CDCI3, δ) : 2.06-2.21 (2H, m) , 2.13 (3H, s), 2.63 (2H, m) , 2.70 (3H x 3/4, s), 3.86 (3H x 1/4, s), 3.03 (2H, d, J=7.5Hz), 4.11 (IH x 1/4, d, J=14.5Hz), 4.39 (IH κ 1/4, d, J=14.5H∑), 4.42 (IH κ 3/4, d, J=14.5Hz), 4.61 (IH x 3/4, d, J=14.5Hz), 4.87 (IH, m) , 5.13 (IH, m) , 7.03-7.35 (9H, m) , 7.40-7.58 (4H, m) , 7.70 (IH, d, J=7.5Hz), 8.36 (IH x 1/4, d, J=1.5Hz), 8.44 (IH x 3/4, d, J=1.5Hz), 8.55 (IH, m) (60) MASS (m/z) : 544 (M+l) + NMR (CDC1 3 , δ) : 2.10 (3H, s) , 2.20 (2H, m) , 2.63 (2H, m) , 2.77 (3H x 3/4, s) , 2.99 (3H x 1/4, s) , 3.03 (2H, d, J=7.5Hz), 4.18 (IH x 1/4, d, J=14.5Hz), 4.52 (IH x 1/4, d, J=14.5Hz), 4.53 (IH x 3/4, d, J=14.5Hz), 4.77 (IH x 3/4, d, J=14.5Hz), 5.39 (2H, m) , 7.01 (IH, m) , 7.06-7.19 (7H, m) , 7.20-7.34 (4H, m) , 7.40-7.51 (2H, m) , 7.70 (IH, d, J=7.5Hz), 8.35 (IH x 1/4, s), 8.48 (IH x 3/4, s) , 8.53-8.68 (IH, m) (61) MASS (m/z) : 594 (M+l) + NMR (CDCI3, δ) : 2.08 (3H x 1/4, s) , 2.10 (3H x 3/4, s), 2.11-2.29 (2H, m) , 2.54-2.69 (2H, m) , 2.83 (3K x 3/4, s), 3.02 (3H x 1/4, s), 3.07 (2H, s) , 4.37 (IH x 1/4, d, J=14.5Hz), 4.60 (IH x 1/4, d, J=14.5Hz), 4.72 (IH x 3/4, d, J=14.5Hz), 4.91 (IH x 3/4, d, J=14.5Hz), 5.30-5.43 (2H, m) , 6.97-7.20 (8H, a), 7.20-7.30 (IH, m) , 7.43-7.62 (3H, m) , 7.65-7.83 (13/4H, m) , 7.98 (IH x 3/4, s), 8.09-8.19 (IH, m) , 8.52 (IH, d, J=7.5Hz), 8.68 (IH κ 1/4, d, J=1.5Hz), 8.82 (IH κ 3/4, d, J=1.5Hz) (62) MASS (m/z) : 595 (M+l) + NMR (CDCI3, δ) : 2.07-2.26 (2H, m) , 2.11 (3H, s), 2.53-2.69 (2H, m) , 2.73 (3H κ 4/5, s), 2.91 (3H κ 1/5, s), 3.02-3.10 (2H, m) , 4.30 (IH x 1/5, d, J=14.5H∑), 4.60 (IH x 1/5, d, J=14.5Hz), 4.62 (IH κ 4/5, d, J=14.5Hz), 4.78 (IH x 4/5, d, J=14.5Hz), 4.88 (IH, m) , 5.18 (IH, m) , 7.04-7.20 (6H, ) , 7.23-7.37 (2H, m) , 7.45 (IH, t, J=7.5Hz), 7.49-7.62 (3H, m) , 7.66-7.86 (16/5H, m) , 7.99 (IH x 4/5, s) , 8.13 (IH, d, J=7.5Hz), 8.70 (IH x 1/5, d, J=1.5Hz), 8.80 (IH x 4/5, d, J=1.5Hz) (63) MASS (m/z) : 596 (M+l) + NMR (CDC1 3 , δ) : 2.03-2.22 (2H, a), 2.11 (3H, s), 2.52-2.67 (2H, m) , 2.92 (3H x 4/5, s) , 3.00 (3H x 1/5, s), 3.08 (2H, t, J=7.5Hz), 4.73 (IH, d, J=14.5Hz), 4.79-4.90 (IH, m) , 4.96 (IH, d, J=14.5Hz), 5.16-5.28 (IH, m) , 7.02-7.17 (6H, m) , 7.21-7.36 (2H, m) , 7.43 (IH, t, J=7.5Hz), 7.48-7.57 (2H, m) , 7.69 (IH, d, J=7.5Hz), 7.73-7.81 (2H, m) , 7.99-8.06 (IK, m) , 8.10-8.15 (IH, m) , 8.73 (IH x 1/5, s) , 8.82 (IH x 4/5, s) (64) MASS (m/z) : 595 (M+l) + NMR (CDCI3, δ) : 2.08 (3H, s), 2.10-2.27 (2H, m) , 2.57-2.69 (2K, m) , 3.01 (3H κ 4/5, s), 3.03-3.10 (2H, m) , 3.15 (3H x 1/5, s) , 4.83 (IH, d, J=14.5Hz), 5.09 (IH, d, J=14.5Hz), 5.25-5.48 (2H, m) , 6.89-7.24 (10H, a), 7.33-7.40 (IH, m) , 7.62- 7.70 (IH, m) , 7.74-7.83 (2H, ) , 8.01-8.08 (IH, m) , 8.11-8.19 (IH, m) , 8.39-8.47 (IH, a), 8.69 (IH x 1/5, s) , 8.83 (IH x 4/5, s) (65) MASS (m/z) : 621 (M+l) + NMR (CDCI3, δ) : 2.07 (3H, s), 2.10-2.33 (2H, m) , 2.59-2.68 (2H, m) , 2.83 (3H x 3/4, s), 3.02 (3H κ 1/4, s), 3.04 (2H, d, J=A5Hz), 4.22 (IH κ 1/4, d, J=14.5Hz), 4.46 (IH x 1/4, d, J=14.5Hz), 4.63 (IH κ 3/4, d, J=14.5Hz), 4.75 (IH κ 3/4, a, J=14.5Hz), 5.33-5.49 (2H, m) , 6.99 (IH κ 1/4, d, J=1.5Hz) , 7.01 (IH κ 3/4, d, J=1.5Hz), 7.04-7.19 (7H, a), 7.23-7.32 (IH, m) , 7.39-7.54 (3H, ) , 7.67-7.73 (2H, a), 8.33 (IH, d, J=7.5Hz), 8.45 (IH κ 1/4, d, J=i.5Hz), 8.57 (IH κ 3/4, d, J=1.5Hz), 8.63-8.88 (2H, a), 9.21 (IH, s), 10.32 (IH, br s) (66) MASS (a/z) : 622 (M+l) **' NMR (CDCI3, δ) : 2.04-2.26 (2H, m) , 2.13 (3H, s) , 2.53-2.69 (2H, m) , 2.74 (3H x 4/5, s), 2.87 (3H x 1/5, s), 2.99-3.14 (2H, m) , 4.16 (IH x 1/5, d, J=14.5Hz), 4.44 (IK x 1/5, d, J=14.5Hz), 4.53 (IH x 4/5, d, J=14.5Hz), 4.61 (IH x 4/5, d, J=14.5Hz), 4.88 (IH, quint., J=7.5Hz), 5.17 (IH, quint., J=7.5Hz), 7.10-7.25 (6H, m) , 7.27-7.60 (7H, a), 7.66-7.74 (2H, a), 8.28-8.34 (IH, ) , 8.44 (IH x 1/5, d, J=1.5Hz), 8.54 (IH x 4/5, d, J=1.5Hz), 8.68 (IH, d, J=5.5Hz), 9.20 (IH, m) (67) MASS (m/z) : 566 (M+l) + NMR (CDCI3, δ) : 2.60 (3H x 2/3, s) , 2.87 (3H x 1/3, S), 3.00 (2H, t, J=7.5Hz), 3.37-3.46 (2H, m) , 4.06 (IH x 1/3, d, J=14.5Hz), 4.31 (IH x 1/3, d, J=14.5Hz), 4.41 (IH x 2/3, d, J=14.5Hz), 4.56 (IH x 2/3, d, J=14.5Hz), 4.85-4.99 (IH, m) , 5.10-5.21 (IH, m) , 6.83-7.21 (11H, m) , 7.22-7.33 (5H, m) , 7.43 (IH, t, J=7.5Hz), 7.49-7.57 (2H, a), 7.70 (IH, d, J=7.5Hz) (68) MASS (m/z) : 565 (M+l) + NMR (CDCI3, δ) : 2.69 (3H x 2/3, s) , 2.99 (3H κ 1/3, s), 3.03 (2H, d, J=7.5Hz), 3.49 (2H, t, J= 7.5Hz), 4.10 (IH x 1/3, d, J=14.5Hz), 4.31 (IH x 1/3, d, J=14.5Hz), 4.43 (IK κ 2/3, d, J=14.5Hz), 4.86 (IH κ 2/3, d, J=14.5H∑), 5.22-5.37 (IH, m) , 5.58-5.70 (IH, m) , 6.78-6.88 (2H, m) , 6.93-7.20 (11H, m) , 7.23-7.39 (5H, a) , 7.51 (IH, d, J=7.5Hz), 7.70 (IH, a), 8.71 (IH, br d, J=7.5Hz) (69) MASS (a/z) : 543 (M+H) + NMR (CDCI3, δ) : 2.83 (3/4 κ 3H, s), 2.91 (1/4 κ 3H, s), 2.95-3.30 (2H, m) , 3.02 (3/4 κ 6K, s), 3.06 (1/4 κ 6H, s), 3.81 (1/4 x IK, d, J=17Hz), 3.88- 4.04 (2H, a) , 4.24 (3/4 x IH, d, J=15Hz), 4.36 (1/4 κ IH, d, J=17Hz), 4.65 (3/4 κ IH, d, J=15Hz), 5.18- 5.64 (2H, a), 6.16 (3/4 κ IH, d, J=9H∑), 6.43 (1/4 κ IH, d, J=9Hz), 6.88-7.92 (13H, a), 8.88-9.12 (IH, a) , 10.00 (IH, br s) (70) MASS (m/z) : 544 (M+H) + NMR (CDC1 3 , δ) : 2.72 (2/3 x 3H, s), 2.82 (1/3 x 3H, s), 2.91-3.12 (2H, m) , 3.08 (6H, s), 3.63-3.80 (IH, m) , 3.92 (1/3 κ IH, d, J=17Hz) , 4.05-4.20 (IH, m) , 4.39 (2/3 κ 2H, ABq, Δ=0.13, J=15Hz) , 4.42 (1/3 κ IH, d, J=17Hz), 4.68-4.82 (IH, m) , 5.04-5.32 (IH, m) , 6.48 (2/3 κ IH, d, J=9Hz) , 6.50 (1/3 κ IH, d, J=9Hz), 7.06-7.73 (13H, m) , 7.94 (1/3 κ IH, d, J=2Hz), 7.98 (2/3 x IH, d, J=2Hz) (71) MASS (m/z) : 567 (M+H) + NMR (CDCI3, δ) : 2.80 (3/4 x 3H, s), 2.90 (1/4 κ 3H, s), 2.96-3.20 (2H, m) , 3.50-3.85 (IH, m) , 3.96-4.22 (IH, m) , 4.26 (1/4 x IH, d, J=17Hz) , 4.55-4.88 (IH +1/4 x IH, m) , 4.70 (3/4 x 2H, s) , 5.05-5.35 (IH, m) , 7.00-8.18 (17H, m) , 8.75 (IH, s) (72) MASS (m/z) : 641 (M+H) + NMR (CDCI3, δ) : 2.71 (3/4 κ 3H, s) , 2.88 (1/4 κ 3H, s), 2.92-3.15 (2H, m) , 3.56-3.73 (IH, m) , 3.95-4.08 (IH, m) , 4.44 (1/4 κ 2K, ABq, Δ=0.20, J=17Hz) , 4.51 (3/4 x IH, d, J=15Hz), 4.62 (2H, s), 4.72-4.90 (IH, ) , 4.82 (3/4 x IH, d, J=15Hz) , 5.10-5.32 (IH, m) , 7.00-8.15 (22H, m) , 8.64 (1/4 x IH, d, J=2Hz), 8.77 (3/4 x IH, d, J=2Hz) (73) MASS (m/z) : 549 (M+H) + NMR (CDCI3, δ) : 2.70 (2/3 x 3K, s) , 2.90-3.13 (4H, m) , 2.99 (1/3 x 3H, s), 4.21 (1/3 x 2H, ABq, __=0.09, J=17Hz), 4.40 (2/3 x IH, d, J=15Hz) , 4.89 (2/3 x IH, d, J=15Hz), 5.22-5.41 (IH, ) , 5.56-5.72 (IH, m) , 6.24 (1/3 x IH, s), 6.28 (2/3 x IH, s) , 6.87- 7.75 (18H, m) , 8.84 (IH, d, J=9Hz) , 11.48 (IH, br s (74) MASS (m/z) : 550 (M+H) + NMR (CDC1 3 , δ) : 2.63 (2/3 x 3H, s) , 2.88 (1/3 x 3H, s), 2.92-3.10 (4H, m) , 4.23 (1/3 x 2H, ABq, Δ=0.18, J=17Hz), 4.52 (2/3 x 2H, ABq, Δ=0.14, J=15Hz) , 4.83-4.98 (IH, m) , 5.09-5.22 (IH, m) , 6.27 (1/3 x IH, s), 6.31 (2/3 x IH, s) , 6.92-7.73 (19H, m) (75) MASS (m/z) : 549 (M+H) + NMR (CDCI3, δ) : 2.72 (2/3 x 3H, s) , 2.95-3.13 (2H, m), 2.97 (1/3 x 3H, s) , 3.22-3.34 (2H, m) , 4.23 (1/3 x 2H, ABq, Δ=0.16, J=17Hz) , 4.42 (2/3 x IH, d, J=15Hz), 4.83 (2/3 x IH, d, J=15Hz) , 5.23-5.40 (IH, m) , 5.61-5.77 (IH, m) , 6.04-6.22 (2H, m) , 6.90-7.74 (17H, m) , 8.88 (IH, d, J=8Hz) , 11.38 (2/3 x IH, br s) , 11.40 (1/3 x IH, br s) (76) MASS (m/z) : 550 (M+H) + NMR (CDCI3, δ) : 2.59 (2/3 x 3H, s), 2.85 (1/3 x 3H, s), 2.88-3.33 (4H, m) , 4.20 (1/3 x 2H, ABq, Δ=0.23, J=17Hz), 4.48 (2/3 x 2H, ABq, Δ=0.16, J=15Hz) , 4.90-5.07 (IH, m) , 5.07-5.25 (IH, a), 6.06-6.32 (2H, a), 6.88-7.72 (18H, m) (77) MASS : 547 (M+l) NMR (CDCI3, δ) : 2.70 (3 x 3/4H, s), 2.80 (3 κ 1/4H, s), 2.95-3.17 (2H, m) , 3.71-3.85 (IH, m) , 3.90 (3H, s), 3.98 (2 x 1/8H, d, J=16Hz), 4.05-4.19 (IH, a), 4.28 (2 x 3/8H, d, J=15Hz) , 4.41 (2 κ 1/8H, d, J=16Hz), 4.57 (2 x 3/8H, d, J=15Hz) , 4.78-4.88 (IH, a), 5.08-5.18 (1 x 3/4H, m) , 5.20-5.28 (1 κ 1/4H, a), 6.69 (1 κ 3/4K, d, J=8H∑ι , 6. A (1 x 1/4H, d, J=8Hz), 7.05-7.21 (5H, m) , 7.29-".45 (4H, a, , 7.69 (IH, d, J=7Hz), 7.76-7.89 (3K, a) , " .90-3.00 (IH, a) (78) MASS : 601 (M+l) NMR (CDC1 3 , δ) : 2.79 (3 x 3/4H, si , 2.68 (3 x 1/4H, s), 2.92-3.08 (2H, a) , 3.10-3.33 (2H, a) , 4.29 (2 κ 1/8H, d, J=16Hz) , 4.53 (2 x 1/8H, a, J=16Hzi , 4.60 (2 κ 3/8H, d, J=15Hz) , 4.71 (2 x 3/SH, d, J=15Hz) , 4.93-5.22 (2H, a), 6.32 (IH, si , " .00-7.20 (5H, a), 7.27 (IH, t, J=8Hz) , 7.39 (IH, t, J=3Hz) , 7.45-7.60 (4H, a), 7.61-7.80 (3K, a), 7.91 (IH, s) , 7.92-8.18 (IH, a), 8.09 (IH, a, J=8Hz) , 8.30-8.50 (IH, a), 8.67 (1 κ 1/4H, s), 8.71 (1 κ 3/4H, s) (79) MASS : 600 (M+l) NMR (CDCI3, δ) : 2.78 (3 κ 4/5H, s), 2.92 (3 κ 1/5H, s), 2.97-3.10 (2H, a), 3.11-3.30 (2H, a), 4.47 (2 κ 2/5H, d, J=15Hz), 4.50 (2 κ 1/5H, si , 5.00 (2 κ 2/5H, d, J=15Hz), 5.33 (IH, q, J=8Kz) , 5.43-5.60 (IK, a), 6.69 (1 κ 4/5H, s) , 6.79 (1 x 1/5H, s), 6.99 (IH, s), 7.02-7.19 (6H, a), 7.22 (IH, d, J=8Hz), 7.32-7.60 (4H, a), 7.61-7.80 (3K, a) , 7.89 (IH, s), 8.10 (IH, d, J=8Hz) , 3.61 (1 x 1/5H, s) , 8.70 (1 κ 4/5H, s) , 8.97 (1 κ 4/5H, d, J=8Hz), 9.11 (1 κ 1/5H, d, J=8Hz) (80) MASS : 628 (M+l) NMR (CDCI3, δ) : 2.70 (3 κ 4/5H, s), 2.82 (3 κ 1/5H, s) , 2.90-3.10 (2H, a), 3.11-3.36 (2H, m) , 4.12 (2 κ 1/8H, d, J=16Hz), 4.41 (2 κ 1/8H, a, J=16Hz) , 4.43 (2 κ 3/8H, d, J=15Hz) , 4.60 (2 κ 3/8H, a, J=15Hz) , 4.96-5.20 (2H, m) , 6.88 (IH, s), 7.05-7.31 (6H, m) , 7.32-7.43 (2H, m) , 7.44-7.70 (6H, a, , 7.90-8.10 (IH, a), 8.20-8.33 (2H, a), 8.40 ,'1 x 1/5H, s, , 8.47 (1 x 4/5H, s), 8.61 (IK, d, J=2Hz), 9.13 (IH, (81) MASS : 627 (M+l) NMR (CDC1 3 , δ) : 2.77 (3 κ 2/3H, s), 2.90 (3 κ 1/3K, s), 2.92-3.10 (2H, a), 3.10-3.30 (2K, a), 4.4C (2 κ 1/2H, d, J=15Hz), 4.79 .2 x 1/2H, d, J=15Hz) , 5.22- 5.37 (IH, a), 5.38-5.50 (IH, a), 6.78 (IH, s), 6.92-7.30 (8H, a), 7.32-7.80 (7H, a), 8.22 (iH, d, J=5Hz), 8.38 (1 x 1/3H, s), 8.46 (1 κ 2/3K, s) , 8.62 (IH, d, J=2H∑), 8.70-8.90 (IH, a) , 9.14 (IH, s) (82) MASS : 589 (M+l) NMR (CDC1 3 , δ) : 2.69 (3 x 2/3H, s), 2.90 (3 x 1/3H, s) , 2.95-3.05 (2H, a), 3.06-3.22 (2H, a), 2.39 (3 κ 1/3H, s), 3.40 (3χ 2/3K, s), 4.20 (2 x 1/6H, a, J=16H∑), 4.21 (2 x 1/3H, d, J=15Hz) , 4.27 (2 x 1/6H, d, J=16Hz), 4.97 (2 x 1/3H, d, J=15Hz) , 5.20- 5.40 (IH, a), 5.61-5.80 (IH, a), 6.45-5.60 (2H, a), 6.88-7.15 (10H, a), 7.16-7.40 (6H, a), 7.49 (IH, d, J=8Hz), 7.68 (IH, d, J=8Hz) , 8.95 (IH, d, J=8H∑! (83) MASS : 590 (M+l) NMR (CDCI3, δ) : 2.59 (3 x 2/3H, s), 2.85 (3 κ 1/3H, S), 2.90-3.04 (2H, a), 3.05-3.19 (2H, a) , 3.70 (3H, s), 4.12 (2 κ 1/6H, d, J=16Hz), 4.28 (2 κ 1/6K, d, J=16Hz), 4.35 (2 κ 1/3H, d, J=15Hz) , 4.63 (2 x 1/3H, d, J=15Hz), 4.92-5.03 (IH, a), 5.07-5.20 (IH, a), 6.70-6.78 (2H, a) , 6.91-7.20 (10H, a) , 7.21- 7.33 (5H, m) , 7.41 (IH, t, J=8Hz) , 7.44-7.55 (2H, a), 7.68 (IH, d, J=8Hz) (84) MASS : 613 (M+l) 981 - 632 - NMR (CDC1 3 , δ) : 2.69 (3 x 3/4H, s), 2.85 (3 x 1/4H, s), 2.90-3.07 (2H, a), 3.35-3.50 (2H, a), 4.40 (2 x 1/8H, d, J=16H∑) , 4.51 (2 x 1/3H, ri, J=16Hz' , 4.56 (2 x 3/8H, d, J=15Hz), 4.78 (2 x 3/8H, a, J=15Hz), 5.01-5.22 (IH, a), 7.03-7.21 (5H, a), 7.22-7.35 (3H, a), 7.37-7.5C (3H, a), 7.51-7.71 (4K, a) , 7.72 (1 κ 1/4H, s), 7.81 (1 κ 3/4H, 5), 7.99 (IH, t, J=8Hz), 8.22-3.33 (IH, a), 8.49-8.69 (2H, a) , 8.82 (2H, s) (85) MASS : 610 (M+l) NMR (CDCI3, δ) : 2.43 (3 κ 2/3H, s) , 2.73 (3 x 1/3H, s) , 2.80-2.97 (2H, a) , 3.42-3.60 (IH, a) , 3.66-3.80 (IH, a), 4.07 (2 x 1/6H, d, J=16H∑), 4.11 (2 κ 1/3H, d, J=15Hz), 4.17 (2 κ 1/6H, d, J=16Hz) , 4.53 (2 κ 1/3H, d, J=15H∑), 4.90-5.10 (2H, a! , 6.48-6.60 (IK, a), 6.90-7.20 (7H, a), 7.21-7.60 (12H, a), 7.61-7.78 (2H, a), 7.79-7.85 (IK, a), 8.23-3.37 (IH, a) (86) MASS : 609 (M+l) NMR (CDCI3, δ) : 2.52 (3 x 2/3H, s), 2.75-3.00 (2H, a), 2.83 (3 κ 1/3H, s), 3.08-3.30 (IH, a), 3.52- 3.68 (IH, a) , 3.95 (2 κ 1/6H, d, J=16Hz) , 4.09 (2 κ 1/3H, d, J=15Kz), 4.17 (2 x 1/6H, a, J=16Kz), 4.90 (2 κ 1/3H, d, J=15H∑ ) , 5.10-5.23 (IH, a) , 5.59-5.80 (IH, a), 6.83-7.35 (18H, a), 7.40-7.60 (3H, a) , 7.71 (IH, d, J=8Hz), 7.83 (1 κ 1/3H, a, J=8H∑), 7.92 (1 κ 2/3H, a, J=8Hz), 8.91 (IH, d, J=7Hz) (87) MASS : 550 (M+l) NMR (CDCI3, δ) : 2.71 (3 κ 4/5H, s), 2.82 (3 κ 1/5H, s), 2.89-3.08 (2H, a), 3.09-3.30 (2H, a) , 4.22 (2 x 1/lOH, d, J=16Hz) , 4.31 (2 x 1/lOH, a, J=16Hz) , 4.38 (2 x 2/5H, d, J=I5Hz), 4.70 (2 x 2/5H, d, J=15H∑) , 5.19-5.39 (IH, a), 5.42-5.59 ( IH, a) , 6.69 (1 κ 4/5H, s), 6.72 (1 κ 1/5H, s), 6.97-A30 (9H, a) , .31 (IH, d, J=8Hz), 7.39-7.59 (3H, aj , 7.62 (IH, d, J=8Hz), 8.22 (1 κ 1/5H, s), 8.33 (1 κ 4/5H, s), 8.44-3.55 (IH, a), 3.88-9.10 (IH, ai (88) MASS : 551 (M+l) NMR (CDC1 3 , δ) : 2.61 (3 κ 4/5H, s), 2.73 (3 κ 1/5H, s), 2.90-3.07 (2H, a), 3.08-3.33 (2H, a), 4.09 (2 κ I/IOH, d, J=16Hz), 4.34 (2 κ 1/lOH, d, J=16Hz) , 4.42 (2 κ 2/5H, d, J=15Hz) , 4.51 (2 κ 2/5H, d, J=15Hz), 4.95-5.15 (2H, a), 6.81 (IH, s) , 7.05-7.32 (7H, a), 7.39 (2H, t, J=8Hz), 7.47-7.60 (3H, m) , 7.62 (IH, d, J=8Hz), 8.01 (IH, d, J=5Hz) , 8.29 (2 κ 1/5H, s), 8.37 (2 κ 4/5H, s) , 8.48 (IH, d, J=3Hz) (89) MASS : 575 (M+l) NMR (CDC1 3 , δ) : 2.51 (3H, s) , 2.61 (3 κ 3/4H, s), 2.79 (3 κ 1/4H, s), 2.81-3.07 (2K, m) , 3.25-3.45 (2H, m) , 4.08 (2 x 1/8H, d, J=16Hz), 4.21 (2 x 1/8H, d, J=16Hz), 4.36 (2 κ 3/8H, d, J=15Hz) , 4.51 (2 κ 3/8H, d, J=15Hz), 5.08-5.28 (IH, m) , 5.30-5.50 (IH, m) , 6.93-7.30 (13H, m) , 7.32-7.50 (2H, m) , 7.69 (IH, d, J=8Hz), 8.18 (1 κ 1/4K, s), 8.30 (1 κ 3/4H, s), 8.22 (1 κ 1/4H, d, J=8Hz) , 8.39 (1 κ 3/4H, d, J=8Hz), 8.49 (1 x 3/4H, d, J=8Hz), 8.67 (1 x 1/4H, d, J=8Hz) (90) MASS : 576 (M+l) NMR (CDC1 3 , δ) : 2.50 (3K, s), 2.55 (3 x 3/4H, s) , 2.72 (3 x 1/4H, s), 2.78-3.02 (2H, m) , 3.22-3.38 (IH, m) , 3.38-3.50 (IH, m) , 4.01 (2 x 1/8H, d, J=16H∑), 4.22 (2 κ 3/8H, d, J=15Hz) , 4.23 (2 κ 1/8H, d, J=16Hz), 4.51 (2 x 3/8H, d, J=15Hz) , 5.00- 5.20 (2H, a), 6.98-7.37 (10H, a), 7.38-7.50 (2H, a), 7.50-7.70 (3H, a) , 8.12-8.20 (IH, a) , 3. 3 (1 x 1/4H, s), 8.22 (1 x 3/4H, s) , 8.50-3.63 (2H, a) (91) MASS : 560 (M+l) NMR (CDC1 3 , δ) : 2.78 (3 x 2/3H, si , 2.94 (3 κ I/3H, s), 2.88-3.10 (2H, a), 3.10-3.30 (2K, a), 4.29 (2 κ 1/3K, d, J=15Hz), 4.31 (2 κ I/3H, s) , 4.99 (2 κ 1/3H, d, J=15Hz), 5.17-5.40 (IH, ) , 5.70-5.9C (IH, a) , 6.84-6.94 (2H, a) , 6.95-7.15 (8H, a), 7.16-7.33 (5H, a), 7.34-7.60 (2H, a), 7.60-A70 (IH, a), 8.23 (IH, s) , 8.43 (IH, s), 8.97 (IH, d, J=8H∑) (92) MASS : 561 (M+l) NMR (CDCI3, δ) : 2.62 (3 κ 2/3H, s), 2.91 (3 κ 1/3H, s), 2.88-3.30 (4H, a), 4.26 (2 κ 1/6H, a, J=16H∑), 4.33 (2 κ 1/6H, d, J=16Hz) , 4.37 ( 2 κ 1/3H, d, J=15Hz), 4.70 (2 κ 1/3H, d, J=15Hz), 4.62-4.75 (2H, a), 6.92-7.20 (8H, a) , 7.20-7.35 (4H, a) , 7.35-7.73 (7H, a), 8.35-8.50 (2H, a) (93) MASS : 594 (M+l) NMR (CDCI3, δ) : 2.61 (3 κ 2/3H, s), 2.89 (3 κ 1/3H, s), 2.92-3.05 (2H, m) , 3.09-3.23 (2H, m) , 4.09 (2 κ 1/6H, d, J=16Hz), 4.30 (2 κ 1/6H, a, J=16Hz) , 4.39 (2 κ I/3H, d, J=15Hz) , 4.67 (2 κ 1/3H, d, J=15Hz), 4.98-5.21 (2H, m) , 6.93-7.20 (11H, m) , 7.21-7.38 (6H, a), 7.42 (IH, t, J=8Hz), 7.48-7.60 (2H, m) , 7.63 (IH, d, J=8Hz) (94) MASS : 593 (M+l) NMR (CDCI3, δ) : 2.68 (3 κ 2/3H, s), 2.88-3.04 (2H, m), 2.99 (3 κ 1/3H, s), 3.07-3.23 (2K, m) , 4.09 (2 κ 1/6H, d, J=16Hz), 4.22 (2 κ 1/6H, d, J=16H∑) , 4.25 (2 x 1/3H, d, J=15Hz) , 5.00 (2 x 1/3H, d, J=15Hz), 5.22-5.38 (IH, m) , 5.68-5.83 (IH, m) , 6.90-7.16 (13H, m) , 7.17-7.40 (5H, a), 7.49 (IH, d, J=8H∑) , 7.68 (IH, d, J=8Hz), 8.91 (IH, a, J=8Hz) (95) MASS : 572 (M+l) NMR (CDC1 3 , δ) : 2.40-3.00 (2H, m) , 2.57 (3H, s), 3.01-3.22 (IH, m) , 3.30-3.47 (IH, π) , 4.20-4.62. (IH, m) , 4.30 (2 κ 1/2H, d, J=15Hz), 4.68 (2 x I/2K, d, J=15Hz), 4.90-5.20 (2H, m) , 5.21-5.36 (IK, a), 6.80-7.37 (16H, a), 7.38-7.60 (2H, a), 7.62- 7.78 (2H, m) (96) MASS : 571 (M+l) NMR (CDCI3, δ) : 2.50-3.30 (2H, a), 2.89 (3H, s, , 2.35-2.60 (IH, a), 4.20-4.40 (IH, a) , 4.48 (2 x 1/2H, d, J=16Hz), 4.60-4.80 (IH, a), 4.76 (2 κ 1/2H, d, J=16Hz), 4.85-5.30 (2H, a), 5.45-5.60 (IH, a), 6.20-6.60 (IH, a), 6.61-7.60 (18H, a), 8.60- 8.90 (IH, a) (97) MASS : 575 (M+l) NMR (CDCI3, δ) : 2.07 (3H, s), 2.11-2.25 (2H, a), 2.50 (3H, s), 2.56-2.73 (2H, a), 2.63 (3 κ 2/3H, s), 2.80 (3 κ 1/3H, s) , 2.91-3.12 (2H, a) , 4.01 (2 x 1/6H, d, J=16Hz), 4.37 (2 x 1/6H, d, J=16Hz) , 4.38 (2 κ 1/3H, d, J=15Hz) , 4.52 (2 κ 1/3H, d, J=15Hz), 4.87-5.00 (IH, a), 5.07-5.30 (IK, a), 7.00-7.22 (6H, a), 7.23-7.50 (4H, a), 7.59 (1 κ 2/3H, d, J=8Hz), 7.67 (1 κ 1/3K, d, J=8H∑) , 7.7C- 7.90 (3H, a), 8.22 (1 κ 1/3H, s), 6.29 (1 κ 2/3H, s) Exa ple 27 The following object compound was obtained according to a similar manner to that of Example 8. MASS (m/z) : 575 (M+H) + NMR (CDC1 3 , δ) : 2.67 (2/3 x 3H, s), 2.90-3.15 (4H, m) , 2.92 (1/3 κ 3H, s), 4.28 (2/3 x IH, d, J=15Hz) , 4.38 (1/3 κ IH, d, J=17Hz) , 4.64 (1/3 κ IH, d, J=17Hz), 4.91 (2/3 κ IH, d, J=15Hz) , 5.20-5.70 (2H, m) , 6.05-7.70 (22H, m) , 8.70 (IH, s) Example 28 The following object coapound was obtained according to a similar manner to that of Preparation 10. MASS (m/z) : 499 <M + +1) NMR (CDCI3, δ) : 2.62 (3H x 2/3, s), 2.85 (3H κ 1/3 s), 2.94-3.14 (2H, m) , 3.79-4.08 (2H, m) , 4.04 (IH x 2/3, d, J=15Hz), 4.28 (IH x 1/3, d, J=15Hz) , 4.39 (IH x 1/3, d, J=15Hz), 4.92 (IH x 2/3, d, J=15Hz), 5.25-5.62 (2H, a), 6.92-7.13 (9H, a), 7.16-7.27 (3H, a), 7.42 (IH, a), 7.49-7.67 (2H, a), 8.67 (IH, m) Example 29 The following object coapounds were obtained according to a siailar aanner to that of Preparation 10. (1) MASS (a/z) : 540 (M + +l) NMR (CDCI3, δ) : 1.24-1.96 (6H, a), 2.68 (3H x 1/3, s), 2.70 (3H x 2/3, s), 2.83-3.18 (4H, a), 4.22- 4.83 (2H, m) , 5.03-5.32 (2H, m) , 6.78-7.60 (15H, m) , 8.15 (2H, m) (2) MASS (m/z) : 526 (M + +l) NMR (CDCI3, δ) : 1.92 (4H, m) , 2.72 (3H x 2/3, s) , 2.91 (3H x 1/3, s), 2.83-3.09 (4H, m) , 4.24 (IH x 2/3, d, J=15Hz), 4.47 (IH κ 2/3, d, J=15Hz) , 4.65 (IH x 1/3, d, J=15Hz), 4.85 (IH x 2/3, d, J=15Hz) , 5.2 " -5.38 (2H, ) , 5.85-7.26 (14H, a), 7.42 (IH, d, J=8Hz) , 7.55 (IH, d, J=8Hzi, 9.12 ( IH, br s, F.κample 30 The following coapounds were obtained according to a siailar aanner to that of Eκaaple 3. (1) MASS : 626 (M+l) NMR (CDC1 3 , δ) : 0.89 (4H, t, J=8Hz) , 0.99 (2H, t, . J=8Hz) , 2.29-2.56 (6H, a) , 2.62-2.83 (2H, a) , 2.75 (3 κ 2/3H, s) , 2.99 (3 κ 1/3H, s) , 3.02-3.12 (2H, a) , 3.88-4.45 (2H, a) , 4.63-4.72 (IH, a) , 4.92 (IH, dd, J=15, 8Hz) , 5.32-5.70 (2H, a) , 6.98-7.18 (9H, a) , 7.20-7.36 (5H, a) , 7.46 (IH, d, J=8Hz) , 7.68- 7.71 (IH, a) , 8.89 (1 κ 1/3K, t, J=8Hz) , 9.17 (1 κ 2/3H, d, J=8Hz) (2) MASS : 601 (M+l) NMR (CDCI3, δ) : 2.29 (6H, s), 2.67 (3 x 2/3H, s) , 2.90 (3 x 1/3H, s) , 3.00-3.10 (2H, a) , 3.22-3.23 (2H, a) , 3.28-3.39 (2H, a) , 4.21 (2 κ 1/6H, d, J=16Hz) , 4.38 (2 x 1/3H, d, J=15Hz) , 4.41 (2 x 1/6H, d, J=16Hz) , 4.70 (2 κ 1/3H, d, J=15Hzi , 4.83- 4.96 (IH, a) , 5.12-5.22 (IK, a) , 7.00-7.19 (7H, m) , 7.23-7.32 (4H, m) , 7.40-7.70 (6H, m) (3) MASS : 617 (M+l) NMR (CDCI3, δ) : 2.31 (6H, s) , 2.63 (3 κ 2/3H, s) , 2.89 (3 κ 1/3H, s) , 2.99-3.09 (2H, a) , 3.11-3.43 (4H, a) , 4.20 (2 κ 1/6K, d, J=16Hz) , 4.37 (2 κ 1/3K, d, J=15Hz) , 4.42 (2 κ 1/6H, d, J=16H∑) , 4.69 (2 κ 1/3H, d, J=15H∑), 4.72-4.80 (IK, a) , 5.10-5.22 (IH, a) , 7.00-7.20 (8H, a) , 7.21-7.35 (4H, a), 7.33-7.46 (2H, a), 7.72 (1 κ 1/3H, s) , 7.77 (1 κ 2/3H, s) , 7.83-7.88 (2H, a) (4) MASS (a/z) : 619 (M+l) NMR (CDC1 3 , δ) : 2.63 (3 κ 2/3H, s) , 2.87 (3 κ 1/3H, s) , 2.97-3.12 (2H, a) , 3.62 (2H, s) , 4.08-4.43 (2 κ 2/3H, a) , 4.32-4.41 (IH, a) , 4.48-4.58 (IH, a) , 4.65 (2 κ 1/3H, d, J=15Hz) , 5.10-5.28 (2H, a) , 6.98-7.20 (8H, a) , 7.22-7.32 (5H, a) , 7.39-7.49 (2H, a) , 7.57 (2H, t, J=8Hz) , 7.69 (IH, d, J=8Hz) , 7.71 (1 κ 2/3H, d, J=8Hz) , 7.79 (1 κ 1/3H, d, J=8Hz) , 8.42 (IH, br s) , 8.47 (IH, br s) (5) MASS (a/z) : 605 (M+l) NMR (CDCI3, δ) : 2.62 (3 κ 2/3H, s) , 2.80 (3 κ 1/3H, s) , 3.00-3.13 (2H, a), 4.08-4.40 (2 x 2/3H, a) , 4.62 (2 x 1/3H, d, J=15Hz) , 4.63-4.72 (IH, a) , 4.81-4.92 (IH, a) , 5.20-5.33 (2H, a) , 6.91-7.30 (11H, a), 7.42 (2H, t, J=7Hz) , 7.50 (2H, d, J=10Hz) , 7.66 (IH, d, J=8Hz) , 7.72-7.91 (3H, a) , 8.10 (IH, t, J=8Hz), 8.71 (IH, d, J=2Hz) (6) MASS (a/z) : 584 (M+H) + NMR (CDCI3, δ) : 2.23 (6H, s) , 2.73 (3 κ 2/3H, s) , 3.00 (3 κ 1/3H, s) , 2.98-3.10 (2H, m) , 3.13-3.22 (2H, m) , 4.20 (2 κ 1/4H, d, J=16Hz) , 4.42 (2 κ 1/4H, d, J=16Hz) , 4.43 (2 x 1/4H, d, J=15Hz), 4.94 (2 x 1/4H, d, J=15Hz) , 4.32-4.45 (IH, m) , 4.68-4.80 (IH, m) , 5.35-5.46 (IH, m) , 5.75-5.88 (IH, m) , 6.99-7.22 (10H, m) , 7.23-7.38 (4H, m) , 7.50 (IH, d, J=8Hz) , 7.70 (IH, d, J=8Hz) , 9.16 (IH, d, J=8Hz) (7) MASS (m/z) : 619 (M+l) NMR (CDCI3, δ) : 2.65 (3 x 2/3H, s) , 2.88 (3 κ 1/3H, s) , 2.99-3.12 (2H, m) , 3.61 (2H, s) , 4.10-4.42 (2 κ 2/3H, m) , 4.36-4.43 (IH, m) , 4.49-4.58 (IH, m) , 4.71 (2 κ 1/3H, d, J=15Hz) , 5.09-5.29 (2H, m) , 6.99-7.20 (9H, m) , 7.22-7.38 (4H, m) , 7.42 (2H, t, J=3Hz) , 7.52 (IH, s; , 7.57 (IH, d, J=5Hz) , 7.63- 7.73 (2H, mi , 8.45 (2H, br s) (3) MASS (a/z) : 605 (M+i) NMR (CDC1 3 , δ) : 2.62 (3 κ 2/3H, s), 2.82 (3 κ 1/3K, si , 3.07 (2H, t, J=8Kz), 4.08-4.38 (2 κ 2/3H, a), 4.61 (2 κ 1/3H, d, J=15Hz), 4.63-4.78 (2H, a), 5.22-5.31 (IH, a), 5.33-5.40 (IH, a) , 6.91-7.32 (11H, a), 7.42 (IH, t, J=8Hz), 7.52-7.61 (3H, a), 7.63 (IH, d, J=8Hz) , 7.73-7.80 (2H, a), 7.92 (1 x 2/3H, d, J=8Hz), 3.01 (1 x 1/3K, d, J=8Hz), 8.70 (2K, br s) (9) MASS (a/∑) : 619 (M+l) NMR (CDCI3, δ) : 2.59 (3 x 2/3H, s), 2.80 (3 κ 1/3H, S), 2.91 (2H, t, J=8Hz), 3.89 (2H, s) , 4.08-4.34 (2 κ 2/3H, a), 4.53-4.60 (2H, m) , 4.62 (2 x 1/3H, d, J=15Hz), 5.00-5.10 (IH, a), 5.13-5.22 (IH, a), 6.93-7.20 (13H, a), 7.40-7.48 (2H, a) , 7.52 (IH, s), 7.58-7.62 (2H, a), 7.63 (IH, d, J=8Hz) , 7.83 (IH, t, J=8Hz), 8.57 (IH, d, J=2Hz) (10) MASS (a/z) : 639 (M+l) NMR (CDCI3, δ) : 1.31-1.62 (6H, a), 2.30-2.43 (4H, a), 2.50-2.57 (2H, a), 2.60-2.71 (2H, m) , 2.63 (3 x 2/3H, s), 2.88 (3 x 1/3H, s), 2.97-3.13 (2H, a) , 4.13-4.69 (4H, a), 5.01-5.11 (IH, a) , 5.16-5.25 (IH, a), 6.98-7.20 (8H, a), 7.23-7.32 (2H, a), 7.40-7.70 (7H, a) (11) MASS (a/z) : 627 (M+li NMR (CDC1 3 , δ) : 1.00 (6H, t, J=8Hz), 2.48-2.57 (7H, a), 2.62 (3 x 2/3H, s), 2.32 (2H, t, J=8Hz), 2.89 (3 κ I/3H, s) , 3.04 (2H, t, J=6Hz), 4.05-4.69 (3H, a), 4.89-5.00 (IH, a), 5.14-5.22 (IH, a), 7.00-7.22 (8H, a), 7.25-7.36 (4H, a), 7.44 (2H, q, J=8Hz), 7.53 (IH, s), 7.56 (IH, dd, J=8, 2Hz,, 7.70 (IH, d, J=8Hz) (12) MASS (a/z) : 585 (M+l) NMR (CDC1 3 , δ) : 2.28 (6H, s), 2.68 (3 κ 2/3H, s), 2.91 (3 κ 1/3H, s), 2.97-3.12 (2H, a), 3.17 (2H, d, J=8Hz), 4.14-4.70 (4K, a), 5.09-5.27 (2H, a), 6.97- ■ 7.22 (7H, a), 7.24-7.32 (4H, a), 7.43 (IH, t, J=8Hz), 7.49-7.58 (3K, a), 7.67-7.76 (2H, a) Example 31 Starting Coapound (620 ag) was dissolved in aethylenechloride (10 al) , and the solution was ice-cooled. To this solution was added trifluoroacetic acid (5 ml) and triethylsilane (476 mg) . The mixture was stirred at this temperature for ten minutes and at ambient temperature for one hour and was concentrated under reduced pressure. The residue was dissolved in ethyl acetate and the organic layer was washed with sodium hydrogencarbonate solution and brine. After evaporation, the crude material obtained was purified on a column of silica gel eluting with chlorofora-aethanol (60:1) to give Object Coapound (380 ag) as an aaorphous solid. MASS : 516 (M+l) NMR (CDCI3, δ) : 2.72 (3 κ 2/3K, s), 2.73-2.88 (IH, a), 2.89 (3 x 1/3H, s), 2.99-3.18 (3H, a), 4.22 (2 x 1/6H, d, J=16Hz), 4.41 (2 x 1/6H, d, J=16Hz), 4.45 (2 x 1/3H, a, J=15Hz) , 4.63 (2 x 1/3H, d, J=15Hz), 4.87-4.97 (IH, a), 5.21 (IH, q, J=8Hz), 7.03-7.19 (7H, a), 7.26-7.35 (5H, a), 7.42-7.57 (4H, a) , 7.69 (IH, d, J=8Hz) Eκample 32 The following object compounds were obtained according to a similar manner to that of Example 31. (1) MASS : 532 (M+l) NMR (CDC1 3 , δ) : 2.73 (3 x 2/3H, s) , 2.78-2.90 (IH, m) , 2.90 (3 x 1/3H, s) , 2.99-3.18 (3H, m) , 4.18 (2 x 1/6H, d, J=16Hz) , 4.43 (2 x 1/6H, a, J=16Hz) , 4.45 (2 x 1/3H, d, J=15Hz), 4.61 (2 x 1/3H, d, J=15Hz) , 4.31-4.92 (IH, m) , 5.17-5.27 (IH, a) , 7.03-7.20 (7H, a) , -7.22-7.47 (7H, a) , 7.81-7.89 (3H, m) (2) MASS : 515 (M+l) NMR (CDCI3, δ) : 2.77 (3 x 2/3H, s) , 2.91-3.18 (4H, m), 3.03 (3 x 1/3H, s) , 4.13 (2 x 1/6H, a, J=16H∑) , 4.41 (2 x 1/6H, d, J=16Hz) , 4.51 (2 κ 1/3H, d, J=15Hz), 4.86 (2 x 1/3H, d, J=15Hz) , 5.37-5.52 (IH, m) , 5.63-5.73 (IH, ) , 7.00-7.20 (9H, m) , 7.22-7.40 (5H, m) , 7.49 (IH, d, J=8Hz) , 7.70 (IH, d, J=8Hz) , 9.11 (IH, t, J=8Hz) Example 3 To a stirred solution of Starting Compound (C.ll g) and triethylamine (0.05 ml) in methylene chloride (5 ml) was added dropwise acetyl chloride (0.02 g) at 0°C and the mixture was stirred at room temperature for I hour. The reaction mixture was washed with IN aqueous hydrochloric acid and 5c aqueous sodium bicarbonate, and dried. Evaporation of solvent gave a residue which was purified by column chromatography on silica gel. Elution with chloroform - 31 methanol-chloroform afforded Object Compound (0.05 g) as powder. MASS (m/z) : 582 (M ÷ +l) NMR (CDCI3, δ) : 1.41-1.94 (6H, m) , 1.84 (3H, s) , 2.80 (3H x 2/3, s), 3.02 (3H x 1/3, s), 2.97-3.11 (3H, a), 3.22-3.33 (IH, a), 4.24 (IH κ 1/3, a, J=15Hz) , 4.45 (IH x 2/3, d, J=15Hzj , 4.62 (IH x 1/3, d, J=15Hz), 4.85 (IH x 2/3, d, J=15Hz) , 5.39 (2H, m) , 6.31 (IH, m) , 6.99-7.15 (8H, m) , 7.17-7.32 (5H, m) , 7.47 (IH, d, J=8Hz), 7.67 (IH, d, J=8Hz) , 8.94 (IH, t, J=8Hz) Example 34 The following object compounds were obtained according to a similar manner to that of Example 33. (1) MASS (m/z) : 541 (M + +l) NMR (CDC1 3 , δ) : 2.02 (3H, s), 2.74 (3H x 2/3, s), 3.00 (3H x 1/3, s), 3.06 (2H, m) , 4.12 (IH x 1/3, d, J=15Hz), 4.37 (IH, m) , 4.47 (IH x 2/3, d, J=15Hz) , 4.57 (IH x 1/3, d, J=15Hz) , 4.65 (IH, dd, J=4, 12Hz), 4.88 (IH x 2/3, d, J=15Hz) , 5.37 (IH, m) , 5.70 (IH, m) , 6.96-7.20 (10H, m) , 7.25-7.32 (4H, m) , 7.49 (IH, d, J=8Hz) , 7.70 (IH, dd, J=2, 8Hz), 9.00 (IH, d, J=8Hz) (2) MASS (m/z) : 630 (M + +l) NMR (CDCI3, δ) : 1.57-2.10 (4H, m) , 2.79 (3H x 2/3, s), 2.97 (3H x 1/3, s) , 2.94-3.07 (2H, m) , 3.42- 3.49 (2H, m) , 4.27 (IH x 1/3, d, J=15Hz) , 4.38 (IH x 2/3, d, J=15Hz), 4.43 (IH x 1/3, d, J=15Hz) , 4.85 (IH x 2/3, d, J=15Hz), 5.35-5.62 (2H, m) , 6.96-7.15 (9H, m) , 7.17-7.33 (7H, m) , 7.35-7.48 (3H, m) , 7.56-7.82 (3H, m) , 9.02 (IH, t, J=8Hz) (3) MASS : 568 (M + +l) NMR (CDCI3, δ) : 1.61-1.71 (2H, m) , 1.77-1.98 (2H, m) , 1.90 (3H x 2/3, s) , 1.92 (3H x 1/3, s) , 2.81 (3H x 2/3, s), 3.02 (3H x 1/3, s) , 2.95-3.05 (2H, m) , 3.12-3.33 (2H, m) , 4.26 (IH x 1/3, d, J=15Hz) , 4.44 (IH x 1/3, d, J=15Hz), 4.46 (IH x 2/3, d, J=15Hz) , 4.88 (IK x 2/3, d, J=15Hz), 5.34-5.52 (2H, ) , 6.60 (IH, m) , 6.99-7.15 (9H, m) , 7.22-7.32 (5H, m) , 7.46 (IH, d, J=8Hz), 7.67 (IH, dd, =2, 8H∑), 9.01 (IH, t, J=8Hz) (4) MASS (m/z) : 644 (M + +l) NMR (CDC1 3 , δ) : 1.33-2.01 (6K, m) , 2.77 (3K x 2/3, s), 3.00 (3H x 1/3, s), 2.98-3.07 (2H, a), 3.21-3.48 (2H, m) , 4.26 (IH x 1/3, d, J=15Hz), 4.40 (IH x 2/3, d, J=15Hz), 4.62 (IK x 1/3, d, J=15Hz) , 4.86 (IK x 2/3, d, J=15Hz), 5.42 (2H, m) , 6.95-7.14 (8H, m) , 7.18-7.37 (8H, m) , 7.47 (IH, d, J=8Hz), 7.64- 7.77 (3H, a), 8.97 (IH, a) Exaaple 35 To a solution of Starting Coapound (243 ag) in N,N- dimethylformamide-pyridine (4:1, 5 ml) was added sulfur trioxide-pyridine complex (790 mg) at room temperature. The mixture was stirred at the temperature for 12 hours and the solvent was evaporated. To this residue was added 10 " . aqueous ammonia with ice-cooling, and the mixture was stirred for 30 minutes. The mixture was extracted three times with butanol, and the organic layer was washed with water. The solvent was evaporated, and the residue was redissolved in toluene, then evaporated to give a solid. The product was purified by column chromatography (silica gel, chloroform- methanol) to give Object Compound (191 mg) as white powders. MASS (m/z) : 499 (M-S0 3 +H ÷ ) NMR (CDCI3, δ) : 2.20-3.05 (5H, a), 3.70-5.50 (6H, a), 6.55-7.65 (17H, m) , 8.50-8.75 (IK, m) Example A The following object compound was obtained by treating Starting Compound with trifluoroacetic acid according to a similar manner to that of Preparation 3, 4, 8 or 41. MASS (m/z) : 569 (M + ÷l) NMR (CDC1 3 , δ) : 1.67 (2H, m) , 1.98 (2H, m) , 2.55 (3H κ 1/2, s), 2.58 (3H x 1/2, s), 2.66-2.78 (2H, a), 2.97 (IH, a) , 3.31 (IH, a), 3.68 (2H κ 1/2, s), 4.27-4.53 (2H κ 1/2, a), 4.99 (2H, a), 6.93-7.70 (17H, a) Example 3 ~ The following object coapounds were obtained according to a siailar aanner to that of Eκaaple 1 or 24. (1) MASS : 647 (M+l) NMR (CDCI3, δ) : 2.52-2.72 (IH, a), 2.69 (3 κ 2/3K, s), 2.80 (3 κ I/3H, s), 3.10-3.33 (3H, a), 3.37- 3.52 (2H, a), 3.53-3.80 (6H, a), 4.21 (2 κ 1/3H, d, J=15Hz), 4.23 (2 κ 1/6H, d, J=16Hz), 4.37 (2 κ 1/6H, d, J=16Hz), 4.69 (2 κ 1/3H, a, J=15H∑), 5.02- 5.30 (2H, a), 6.88 (2 x 1/3H, d, J=8Hz) , 6.93 (2 κ 2/3H, d, J=8Hz), 7.03-7.21 (3H, a) , 7.22-7.33 (3H, a), 7.34-7.57 (4H, a), 7.58-7.83 (6H, a) , 8.20 (IH, t, J=7Hz) (2) MASS : 646 (M+l) NMR (CDCI3, δ) : 2.52-2.77 (IH, a), 2.68 (3 κ 2/3H, s), 2.83 (3 κ 1/3H, s), 3.03-3.30 (3H, a), 3.30- 3.48 (2H, a), 3.49-3.72 (6H, a), 4.15 (2 κ 1/3H, d, J=15Hz), 4.30 (2 κ 1/6H, d, J=16Hz), 4.38 (2 κ 1/6H, d, J=16Hz), 4.73 (2 κ 1/3H, d, J=15H∑ 1 , 5.13- 5.38 (2H, a), 6.80-7.00 (3H, a), 7.01-7.30 (6H, ai , 7.30-7.48 (3H, a), 7.50-7.30 (5H, a), 7.94-3.20 (2H, a) (3) MASS : 610 (M+l) NMR (CDCI3, δ) : 2.50-2.72 (IH, a), 2.73-3.03 (2H, a), 2.81 (3 κ 2/3H, s), 2.87 (3 κ 1/3H, s), 3.09-3.30 (IH, a), 3.19 (3 x 1/3H, s), 3.20 (3 κ 2/3H, s), 3.31-3.70 (8H, a), 4.23 (2 κ 1/6H, a, J=16Hz), 4.50 (2 κ 1/3H, d, J=15H∑) , 4.65 (2 x 1/3H, d, J=15Hz), 4.78 (2 x 1/6K, d, J=16Hz), 5.37-5.50 (I x 1/3K, m) , 5.51-5.60 (1 x 2/3H, m) , 5.70-5.37 (IH, m) , 6.61 (1 x 2/3H, d, J=8Hz) , 6.78 (IK, s) , 6.88 (1 x 1/3H, d, J=8Hz), 6.91-7.33 (12H, m) , 7.38-7.50 (IH, m), 7.60-7.72 (IH, m) , 9.87 (IH, s) (4) MASS : 611 (M+l) NMR (CDC1 3 , δ) : 2.51-2.70 (IH, m) , 2.81 (3 κ 2/3H, s), 2.89 (3 x 1/3H, s), 2.94-3.09 (2H, m) , 3.13 (IH, t, J=8Hz), 3.22 (3H, s) , 3.30-3.42 (2H, a), 3.43-3.70 (6H, m) , 4.21 (2 x 1/6H, d, J=16Hz) , 4.51 (2 x 1/3H, d, J=15Hz), 4.67 (2 x 1/3H, d, J=15Hz) , 4.73 (2 x 1/6H, d, J=16Hz) , 5.34-5.58 (IH, m) , 5.73 (IH, q, J=5Hz), 6.54 (1 x 2/3H, d, J=8Hz) , 6.67 (1 x 1/3H, d, J=8Hz), 6.80-6.93 (IH, m) , 6.98-7.09 (2H, a), 7.11 (IH, d, J=8Hz) , 7.13-7.39 (7H, a) , 7.40-7.60 (3H, a), 7.62-7.78 (IH, a) (5) MASS : 626 (M+l) NMR (CDCI3, δ) : 2.58-2.80 (IH, a), 2.67 (3 x 2/3H, s), 2.83 (3 κ 1/3H, s), 2.89-3.02 (2H, a) , 3.10- 3.22 (IH, a), 3.30-3.48 (2H, a), 3.49-3.72 (6H, a) , 3.58 (3H, s), 4.22 (2 x 1/3H, d, J=15Hz) , 4.31 (2 x 1/6H, d, J=16Hz), 4.40 (2 x 1/6H, d, J=16Hz) , 4.75 (2 x 1/3H, d, J=15Hz) , 5.09-5.20 (IH, a) , 5.21-5.34 (IH, a), 6.61 (2H, t, J=8Hz) , 6.90-7.02 (3H, a) , 7.03-7.14 (2H, m) , 7.18-7.32 (5H, a) , 7.42 (IH, d, J=8Hz) , 7.62 (IH, d, J=8Hz) , 8.02-8.20 (2H, a) (6) MASS : 627 (M+l) NMR (CDCI3, δ) : 2.58-2.71 (IH, a), 2.68 (3 κ 1/3H, s), 2.83 (3 x 2/3H, s) , 2.88-3.08 (2H, a), 3.23- 3.38 (IH, a), 3.40-3.60 ' (2H, a), 3.61-3.80 (6H, a) , 3.70 (3H, s), 4.23 (2 κ 1/6H, a, J=16Hz, , 4.29 (2 κ 1/3H, d, J=15Hz), 4.41 (2 κ 1/6H, a, J=16Hz) , 4.69 (2 κ 1/3H, d, J=15Hz) , 5.01-5.18 (2H, a) , 6.69 (2 κ 2/3H, d, J=15Hz), 6.73 (2 κ 1/3H, a, J=15Hz) , 6.97- 7.14 (4K, a), 7.22-7.35 (5H, a), 7.43 (IH, t, J=8Hz), 7.50 (IH, si, 7.54-7.61 (IH, a) , 7.62-7.71 (IH, a) , 8.22 (IH, d, J=8Hz) (7) MASS : 569 (M+l) NMR (CDC1 3 , δ) : 2.51 (3H, s), 2.57 (3 κ 3/4H, s), 2.61-2.69 (IH, a), 2.73 (3 x 1/4H, si , 2.93 (6H, s), 2.99-3.12 (2H, a) , 3.27 (IK, dd, J=16, 5Hz), 4.09 (2 κ 1/6K, d, J=16Hz), 4.27 (2 κ 1/3K, d, J=15H∑), 4.29 (2 κ 1/6H, d, J=16Hz) , 4.51 (2 κ 1/3H, d, J=15Hz), 5.09-5.22 (2H, a), 6.99-7.29 (10H, a), 7.46 (IH, d, J=8Hz) , 7.65 (IH, d, J=8Hz), 7.99 (1 κ 3/4H, d, J=8H∑), 8.06 (I κ 1/4H, d, J=8Hz), 8.19-8.27 (2H, a) (8) MASS : 570 (M+l) NMR (CDCI3, δ) : 2.52 (3H, s) , 2.58 (3 κ 2/3H, s) , 2.61-2.70 (IH, a) , 2.73 (3 κ 1/3H, s) , 2.97 (3H, s), 3.00 (3K, s), 2.98-3.08 (2H, a) , 3.34 (IH, d, J=17Hz), 4.02 (2 x 1/6H, a, J=16Hz) , 4.27 (2 x 1/3H, d, J=15Hz), 4.31 (2 κ 1/6H, d, J=16Hz) , 4.57 (2 κ 1/3H, d, J=15Hz), 5.06-5.19 (2H, a) , 7.07 (IH, d, J=8Hz) , 7.12-7.31 (7H, a), 7.43 (IH, t, J=8Hz) , 7.51 (IH, s) , 7.58 (IH, d, J=8Hz) , 7.66 (IK, d, J=8Hz), 7.78 (1 κ 1/4H, d, J=SHz) , 7.80 (1 x 3/4H, d, J=8Hz), 8.20 (1 κ 1/4H, s) , 8.28 (1 κ 3/4K, s) , 8.32 (IH, d, J=8Hz) (9) MASS : 623 (M+l) NMR (CDCI3, δ) : 2.22 (3K, s) , 2.26 (3H, ε) , 2.25-2.42 (4H, a), 2.61 (3 x 2/3H, s) , 2.68-2.78 (IH, a), 2.82 (3 x 1/3H, s), 2.95-3.10 (2H, a), 3.19-3.30 (IK, a), 3.35-3.50 (2H, a), 3.55-3.70 (2H, m) , 4.18 (2 x 1/6H, d, J=16Hz), 4.20 (2 x 1/3H, d, J=15Hz), 4.32 (2 κ 1/6H, d, J=16Hz) , 4.68 (2 x 1/3H, d, =15Hz), 5.12-5.30 (2H, m) , 6.76-7.18 (11H, m) , 7.23 (IH, t, J=8Hz), 7.44 (IH, d, J=3Hz), 7.65 (IH, d, J=8Hz), 7.99-3.10 (2H, a) (10) MASS : 624 (M+l) NMR (CDC1 3 , δ) : 2.29 (3H, s), 2.31 (3H, s) , 2.34-2.53 (4K, a), 2.59 (3 x 2/3H, s) , 2.63-2.72 (IH, a), 2.81 (3 κ 1/3H, s), 3.00-3.10 (2H, a), 3.28-3.39 (IH, a), 3.42-3.58 (2H, a), 3.63-3.72 (2ά ' , a), 4.09 (2 x 1/6H, d, J=16Hz), 4.32 (2 x 1/6H, d, J=16Hz) , 4.27 (2 x 1/3H, d, J=15Hz) , 4.60 (2 x 1/3H, d, J=15Hz), 5.02-5.16 (2H, m) , 6.74-7.06 (3H, m) , 7.11-7.22 (6H, m) , 7.29 (IH, t, J=8Hz) , 7.43 (IH, t, J=8Hz), 7.50 (IH, s), 7.58 (IH, a, J=8Hz) , 7.68 (2 x 2/3H, d, J=8Hz), 7.72 (2 x 1/3H, d, J=8Hz) , 8.22 (IH, d, J=8Hz) (11) MASS : 623 (M+l) NMR (CDCI3, δ) : 2.13 (3 κ 1/3H, s), 2.16 (3 κ 2/3H, s), 2.23 (3H, s), 2.23-2.42 (4H, a), 2.61 (3 κ 2/3H, s), 2.59-2.74 (IH, a), 2.82 (3 x 1/3H, s), 2.99-3.09 (2H, a), 3.21 (IH, t, J=15Hz), 3.36-3.48 (2H, a), 3.52-3.71 (2H, a), 4.12 (2 x 1/6H, d, J=16Hz), 4.21 (2 x 1/6K, d, J=16Hz), 4.40 (2 x 1/3H, d, J=15Hz), 4.58 (2 x 1/3H, d, J=15Hz) , 4.98- 5.28 (2H, a), 6.75 (IH, t, J=8Hz) , 6.98 (IH, d, J=8Hz), 7.02-7.20 (9H, a), 7.23 (IH, t, J=8Hz) , 7.41 (IH, d, J=8Hz), 7.64 (IH, d, J=8Hz), 7.96-8.09 (2H, m) (12) MASS : 640 (M+l) NMR (CDC1 3 , δ) : 2.13 (3 κ 1/3H, s) , 2.14 (3 x 2/3H, s), 2.23 (3H, s) , 2.31-2.50 (4H, m; , 2.59 ( IH, dd, J=17, 8Hz), 2.63 (3 x 2/3H, s), 2.85 (3 κ 1/3H, s), 3.01-3.15 (2H, m) , 3.21-3.35 (IH, a) , 3.40-3.58 (2H, a), 3.60-3.74 (2H, a), 4.10 (2 x 1/6H, d, J=16Hz), 4.24 (2 x 1/6H, d, J=16Hz) , 4.47 (2 x 1/3H, d, J=15Hz) , 4.53 (2 x 1/3H, a, J=15H∑), 4.89- 5.20 (2H, m) , 6.80 (IH, t, J=8Hz) , 7.07-7.30 (8H, a), 7.38-7.47 (2H, a), 7.63-7.90 (4H, a), 8.11 (IH, t, J=8Hz) (13) MASS : 623 (M+l) NMR (CDCI3, δ) : 2.13 (3 x 1/3H, s), 2.15 (3 κ 2/3H, s), 2.29 (3H, s), 2.33-2.49 (4H, a) , 2.52-2.70 (IH, a), 2.62 (3 κ 2/3H, s), 2.83 (3 κ 1/3H, s), 2.99- 3.17 (2H, a), 3.30 (IH, t, J=15Hz), 3.41-3.58 (2H, m) , 3.60-3.72 (2H, m) , 4.06 (2 κ 1/6H, d, J=16Hz) , 4.22 (2 κ 1/6H, d, J=16Hz), 4.48 (2 κ 1/3H, d, J=15Hz), 4.52 (2 κ 1/3H, d, J=15Hz), 4.93-5.22 (2H, m) , 6.73 (1 κ 1/3H, d, J=8Hz) , 6.79 (1 κ 2/3H, d, J=8Hz), 7.07-7.31 (9K, a), 7.42 (IH, s), 7.49 (IH, s), 7.57 (IH, d, J=8Hz), 7.61-7.73 (2H, a) , 8.20 (IH, d, J=8Hz) (14) MASS : 598 (M+l) NMR (CDCI3, δ) : 2.60-2.73 (IH, a), 2.82 (3 κ 3/4H, s), 2.88 (3 κ 1/4H, s) , 2.92-3.12 (2H, a), 3.14- 3.26 (IH, a), 3.30-3.45 (2H, a), 3.50-3.70 (6H, a) , 4.30 (2 x 1/6H, d, J=17Hz) , 4.42 (2 x 1/3H, d, J=15Hz), 4.50 (2 κ 1/6H, d, J=17Hz), 4.60 (2 κ 1/3H, d, J=15Hz), 4.98-5.08 (2 κ 1/6K, a), 5.14- 5.26 (2 κ 5/6H, a), 6.82 (1 κ 1/4H, a, J=5Hz), 6.86 (1 κ 3/4H, d, J=5Hz) , 6.98 (IH, s) , 7.05-7.18 (6H, a), 7.27 (IH, t, J=8Hz) , 7.40 (IH, a, J=8Hz) , 7.63 (IH, d, J=5Hz), 8.00-8.10 (2H, a) , 3.53 (IH, d, J=5Hz), 9.09 (1 x 3/4H, s), 9.10 (1 κ 1/4H, ε) (15) MASS : 599 (M+l) NMR (CDC1 3 , δ) : 2.60-2.70 (IH, a), 2.82 (3 κ 3/4K, s), 2.87 (3 κ 1/4H, s), 2.98-3.13 (2H, a), 3.27- 3.33 (IH, a), 3.40-3.57 (2H, a), 3.62-3.78 (6H, a), 4.32 (2 x 1/6H, d, J=17Hz) , 4.45 (2 x 1/6H, d, J=17Hz), 4.48 (2 κ 1/3H, d, J=15Kz) , .6C (2 x 1/3H, d, J=15Hz), 4.93-5.22 (2H, a), 6.86 (1 κ 1/4H, d, J=5Hz), 6.93 (1 κ 3/4H, d, J=5Hz) , 7.15- 7.23 (5H, a), 7.30 (IH, t, J=8Hz) , 7.43 (IH, t, J=8Hz), 7.50 (IH, d, J=8Hz), 7.58 (IH, d, J=8Hz), 7.62-7.71 (2H, a), 8.18-8.22 (IK, a), 8.57-3.62 (IH, a), 9.10 (IH, s) (16) MASS : 648 (M+l) NMR (CDCI3, δ) : 2.60-2.78 (IH, a), 2.81 (3 κ 4/5H, s), 2.92 (3 κ 1/5H, s) , 2.97-3.22 (3H, a), 3.28- 3.42 (2H, a), 3.48-3.65 (6K, a), 4.67 (2 x. 1/2H, d, J=15Hz), 4.89 (2 x 1/2H, d, J=15Hz) , 5.11-5.32 (2H, a), 6.91-7.12 (7H, a), 7.20 (IH, t, J=8Hz) , 7.41 (IH, d, J=8HZ), 7.61 (IH, d, J=8Hz) , 7.70-7.78 (2H, a), 7.94-8.02 (IH, a), 8.03-8.27 (3H, a), 8.70 (1 x 1/5H, s), 8.73 (1 x 4/5H, s) (17) MASS : 649 (M+l) NMR (CDCI3, δ) : 2.58-2.73 (IH, m) , 2.82 (3 x 3/4H, s), 2.93 (3 κ 1/4H, s), 3.02-3.32 (3H, m) , 3.40- 3.55 (2K, a), 3.58-3.77 (6H, a), 4.59 (2 x 1/6E, d, J=16Hz), 4.68 (2 x 1/6H, d, J=16Hz), 4.70 (2 x 1/3H, d, J=15Hz), 4.90 (2 κ 1/3H, d, J=15Hz) , 5.03- 5.28 (2H, m) , 7.02-7.22 (5H, a), 7.29 (IH, t, J=8Hz), 7.41 (IH, t, J=8Hz), 7.48 (IH, s) , 7.56 (IH, d, J=8Hz), 7.68 (IH, d, J=8Hz) , 7.70-7.82 (3H, m) , 7.98-8.03 (IH, a) , 3.07-8.14 (IH, a) , 8.19 (IH, d, J=8H∑) , 3.70 (1 x 1/4H, s), 8.75 (1 κ 3/4H, s) (18) MASS : 647 (M+l) NMR (CDC1 3 , δ) : 2.60-2.77 (IH, a), 2.82 (3 κ 3/4H, s) , 2.93 (3 κ 1/4H, s) , 3.00-3.25 (3H, a) , 3.30- 3.45 (2H, a), 3.50-3.70 (6H, a) , 4.62 (2 x 1/3H, s), 4.67 (2 κ 1/3H, d, J=15H∑) , 4.92 (2 κ 1/3H, a, J=15Hz), 5.19-5.31 (2H, a), 6.95-7.30 (9H, a), 7.41 (IH, d, J=8Hz), 7.52 (IH, t, J=8Hz), 7.61-7.71 (2H, a) , 7.79 (IH, d, J=8Hz), 7.98-8.18 (4H, a) (19) MASS : 648 (M+l) NMR (CDCI3, δ) : 2.59-2.71 (IH, a), 2.74 (3 κ 3/4H, s), 2.89 (3 κ 1/4K, s), 3.01-3.20 (2H, a), 3.21- 3.33 (IH, a), 3.40-3.55 (2H, a), 3.60-3.80 (6H, m) , 4.60 (2 κ 1/6H, d, J=16Hz) , 4.63 (2 κ 1/6H, d, J=16Hz), 4.68 (2 κ 1/3H, d, J=15Hz), 4.89 (2 κ 1/3H, d, J=15H∑), 5.05-5.25 (2H, m) , 7.11-7.32 (7H, m) , 7.41-7.59 (4H, m) , 7.67-7.82 (4H, ) , 8.00-8.12 (2H, m) , 8.23 (IK, d, J=8Hz) (20) MASS : 647 (M+l) NMR (CDCI3, δ) : 2.63-2.80 (IH, m) , 2.71 (3 x 3/4H, s), 2.89 (3 x 1/4H, s), 2.99-3.30 (3H, m) , 3.31- 3.49 (2H, m) , 3.50-3.70 (6H, m) , 4.30 (2 x 1/6H, d, J=16Hz), 4.58 (2 κ 1/6H, d, J=16Hz), 4.69 (2 κ 2/3H, s), 5.12-5.30 (2H, ) , 6.95-7.2C (7H, a) , 7.21-7.30 (2H, ) , 7.33-7.49 (2H, m) , 7.60-7.77 (2H, m) , 7.80 (1 κ 1/4H, s), 7.88 (1 κ 3/4H, s), 8.05-8.20 (3H, m) , 8.90 (IH, a, J=2H∑) (21) MASS : 648 (M+l) NMR (CDCI3, δ) : 2.61-2.75 (IH, m) , 2. 0 (3 κ 3/4H, s), 2.86 (3 κ 1/4H, ε), 3.00-3.13 (2H, a), 3.22- 3.33 (IH, m) , 3.40-3.58 (2H, a), 3.60-3.80 !6H, a), 4.19 (2 x 1/6K, d, J=16Hz), 4.58 (2 x 1/6H, d, J=16Hz), 4.70 (2 κ 1/3H, d, J=15Hzi , 4.81 (2 κ 1/3H, d, J=15Hz), 5.03-5.22 (2H, a), 7 .10-7.60 (11H, a), 7.68 (IH, a, J=8H∑), 7. 7 1-7.32 (2H, a) , 7.83 (IH, s), 8.12 (IH, d, J=8Hz) , 3.21 (IH, t, J=8Hz), 8.89 (IH, d, J=2Hz) (22) MASS : 598 (M+l) NMR (CDCI3, δ) : 2.63-2.75 (IH, a), 2.8C (3 κ 3/4H, s), 2.83 (3 x 1/4H, s), 2.94-3.20 (3H, a), 3.30- 3.45 (2H, a), 3.50-3.67 (6H, a), 4.39 (2 x 1/6H, d, J=17Hz), 4.48 (2 κ 1/6H, d, J=17Hz), 4.49 (2 κ 1/3H, d, J=15Hz), 4.70 (2 κ 1/3H, d, J=15Hz), 5.10- 5.23 (2H, a), 6.93-6.98 (IH, a), 7.03-7.13 (6H, a), 7.22-7.28 (IH, a), 7.42 (IH, d, J=8Hz), 7.62 (IH, d, J=8Hz), 8.02-8.17 (2H, a), 8.33-5.49 (3H, a) (23) MASS : 599 (M+l) NMR (CDCI3, δ) : 2.58-2.70 (IH, a), 2.81 (3 κ 5/6H, s), 2.86 (3 x 1/6K, s), 3.00-3.18 (2H, a), 3.20- 3.31 (IH, a), 3.39-3.54 (2H, m) , 3.60-3.75 (6H, m) , 4.41 (2 x 1/3H, s), 4.48 (2 κ 1/3H, d, J=15Hz), 4.70 (2 x 1/3H, d, J=15Hz) , 5.02-5.19 (2H, a), 7.10-7.22 (6H, m) , 7.29 (IH, t, J=8Kz) , 7.42 (IH, t, J=8Hz), 7.50 (IH, s), 7.56 (IH, a, J=8H∑), 7.63- 7.78 (2H, m), 8.13-8.22 (IH, m) , 8.33-8.50 (2H, m) (24) MASS : 675 (M+l) NMR (CDCI3, δ) : 2.61-2.74 (IH, ) , 2.71 (3 x 3/4H, s), 2.81 (3 x 1/4K, s), 3.00-3.20 (2K, a) , 3.28- 3.38 (IH, a), 3.41-3.58 (2H, a) , 3.62-3.80 (6H, a), 4.15 (2 x 1/6H, d, J=16Hz) , 4.41 (2 x I/6H, a, J=16Hz), 4.42 (2 x 1/3H, d, J=15Hz) , 4.60 (2 x 1/3H, d, J=15Hz), 5.09-5.20 (2K, a) , 7.12-7.80 81 - 652 - (14H, a), 8.22 (IH, d, J=8Hz), 8.30 (IH, a, J=8H∑), 3.41 (1 κ 1/4H, s), 8.50 (1 κ 3/4H, si , 3.60-8.70 (IH, a) , 9.12-9.22 (IH, a) (25) MASS : 674 (M+l) NMR (CDC1 3 , δ) : 2.64-2.73 (IH, a), 2.65 (3 κ 3/4H, s), 2.79 (3 κ 1/4H, s), 2.98-3.27 3H, a), 3.29- 3.45 (2H, a) , 3.48-3.70 (6H, a), 4.16 (2 κ 1/6K, d, J=16Hz) , 4.33 (2 κ 1/3H, a, J=15Hz), 4.37 (2 κ 1/6H, d, J=16Hz), 4.57 (2 x 1/3H, d, J=15Hz), 5.09- 5.30 (2H, a), 6.99 (IH, ε), 7.06-7.19 (6H, a), 7.20-7.30 (IH, a), 7.33-7.48 (3H, a), 7.53-7.68 (2H, a), 8.09-8.28 (3H, a), 8.40 (1 x 1/4H, s), 8.48 (1 x 3/4H, s), 6.63 (IH, s) , 9.17 (IH, s) (26) MASS : 674 (M+l) NMR (CDCI3, δ) : 2.61-2.73 (IH, a), 2.64 (3 x 3/4H, s), 2.80 (3 κ 1/4H, s), 2.98-3.12 (2H, a), 3.13- 3.25 (IH, a), 3.30-3.48 (2H, a), 3.52-3.63 (6H, a), 4.18 (2 κ 1/6H, d, J=16Hz), 4.33 (2 κ 1/3H, d, J=15Hz), 4.40 (2 κ 1/6H, d, J=I6Hz) , 4.65 (2 κ 1/3H, d, J=15Hz), 5.11-5.30 (2H, a), 6.98-7.02 (IH, a), 7.08-7.20 (6H, a), 7.22-7.32 (2H, a) , 7.43 (2H, t, J=8Hz), 7.63 (IH, a, J=8Hz) , 7.80 (IH, t, J=8Hz), 8.02-8.20 (2H, m) , 8.30 (IH, t, J=8Hz), 8.38 (IH, d, J=8Hz), 8.47 (IH, s), 8.68 (IH, d, J=5Hz) (27) MASS : 675 (M+l) NMR (CDCI3, δ) : 2.61-2.72 (IH, m) , 2.69 (3 κ 3/4H, s), 2.81 (3 κ 1/4H, s), 3.01-3.18 (2H, m) , 3.25- 3.35 (IH, m) , 3.40-3.58 (2H, m) , 3.62-3.79 (6H, m) , 4.19 (2 κ 1/6H, d, J=16Hz), 4.38 (2 κ 1/3H, d, J=15Hz), 4.42 (2 x 1/6H, d, J=16Hz) , 4.69 (2 x 1/3H, d, J=15Hz), 5.10-5.22 (2H, a) , 7.12-7.27 (6H, 81 - 653 - m) , 7.31 (2H, t, J=8Hz), 7.43 (IH, t, J=3Hz) , 7.50- 7.60 (2H, m) , 7.67-7.85 (3K, m) , 3.21 (IH, d, J=8Hz), 8.27-8.40 (2H, a), 3.48 (IK, s), 3.6S (IK, a, J=5Hz) (28) MASS (m/z) : 548 (M + +l) NMR (CDCI 3 , δ) : 0.88-0.98 (6H, a), 2.10 (IH, a), 2.71 (IH, dd, J=6, 15Hz), 2.91 (3H x 1/4, s), 3.03 (3H κ 3/4, s), 3.22 (IH, dd, J=4, I5Hz), 3.38 (2H, a) , 3.60 ( 6H, a), 4.33 (IH x 3/4, d, J=15Hz), 4.64 (2H x 1/4, s), 4.87 (IH x 3/4, d, J=I5Hz), 4.87 (IH, a), 5.33 (IH, a), 7.02 (IH, s) , 7.12 (IH, t, J=8Hz), 7.22-7.37 (6H, a), 7.43 (IH, d, J=8Hz), 7.64 (IH, d, J=8Hz), 7.97 (IH x 1/4, d, J=7Kz), 8.07 (IH x 3/4, d, J=7Hz), 8.18 (IH, d, J=7Hz) (29) MASS (m/z) : 549 (M ÷ +l) NMR (CDCI3, δ) : 0.91-0.99 (6H, m) , 2.08 (IH, a), 2.66 • (IK, m) , 2.88 (3H x 1/4, s), 3.02 (3K x 3/4, s), 3.32 (IH, dd, J=3, 16Hz) , 3.47 (2H, a), 3.67 (6H, a), 4.35 (IH κ 3/4, d, J=15Hz) , 4.56 (IH κ 1/4, d, J=16Hz), 4.69 (IH κ 1/4, d, J=16Hz), 4.79 (IH κ 3/4, d, J=15Hz), 4.81 (IH, a), 5.15 (IH, a), 7.18- 7.37 (6H, a), 7.42 (IH, t, J=8Hz) , 7.50 (IH, s), 7.54 (IK, d, J=8Hz) , 7.65 (2H, d, J=8Hz) , 8.31 (IH, a) (30) MASS (a/z) : 602 (M ÷ +l) NMR (CDCI3, δ) : 0.62-1.21 (5H, a), 1.37-1.89 (8H, a), 2.62-2.71 (IH, m) , 2.88 (3H x 1/3, s), 2.89 (3H x 2/3, s), 3.27 (IH, dd, J=4, 15Hz) , 3.41 (2H, a), 3.62 (6H, a), 4.14 (IH x 2/3, d, J=15Hz), 4.54 (IH x 1/3, d, J=16Hz), 4.64 (IH x 1/3, a, J=16H∑), 4.80 (IH x 2/3, d, J=15Hz), 5.02 (IH, a), 5.19 (IH x 1/3, m) , 5.27 (IH x 2/3, m) , 6.90 (IH, s), 7.10- 7.38 (7H, a), 7.45 (IH, d, J=8Hz) , 7.65 (1H, d, J=8Hz), 7.77 (IH κ 1/3, d, J=7Hz) , 7.95 (IH κ 2/3, d, J=7Hz), 8.08 (IH, t, J=7Hz) (31) MASS (a/z) : 603 (M + +lj NMR (CDCI 3 , δ) : 0.62-1.25 (5H, a), 1.35-1.76 (8K, a), 2.62-2.72 (IH, a), 2.91 (3H κ 1/3, s), 2.99 (3H κ 2/3, s), 3.28 (IH, dd, J=3, 15Hz) , 3.43 (2H, a), 3.63 (6H, a), 4.37 (IH x 2/3, d, J=15Hz), 4.62 (2H x 1/3, s), 4.77 (IH x 2/3, d, J=15Hz ) , 5.02 (IH, a), 5.15 (IH, a), 7.18-7.38 (5H, a), 7.43 (IH t, J=8Hz) , 7.52 (IH, s), 7.55 (IH, d, J=8H∑) , 7.67 (2H, d, J=8Hz), 8.23 (IH, m) (32) MASS (m/z) : 695 (M + +l) NMR (CDCI3, δ) : 2.34 (3H, s) , 2.57 (4H, m) , 2.58 (3H κ 2/3, s), 2.65 (IH, dd, J=7, 16Hz), 2.78 (3H κ 1/3, s), 3.03 (2H, m) , 3.20 (4H, m) , 3.30 (IH, m) , 3.47 (2H, m) , 3.68 (6H, ) , 4.01 (IH κ 1/3, d, J=16Hz), 4.21 (IH κ 2/3, d, J=15Hz), 4.30 (IH κ 1/3, d, J=16Hz), 4.54 (IH κ 2/3, d, J=15Hz), 5.10 (2H, m) , 6.83-7.02 (4H, m) , 7.17 (5H, a), 7.32 (IH, d, J=8Hz), 7.44 (IH, t, J=8H∑), 7.51 (IH, s), 7.57 (IH, d, J=8Hz), 7.64-7.71 (2H, a) , 8.21 (IH, d, J=8Hz) (33) MASS (a/z) : 694 (M ÷ +l) NMR (CDCI3, δ) : 2.34 (3H, s), 2.57 (4K, a), 2.60 (3H κ 2/3, s), 2.72 (IH, a), 2.82 (3H x 1/3, s), 3.02 (2H, d, J=7Hz), 3.17 (5H, a), 3.37 (2H, a), 3.58 (6H, m) , 4.07 (IH x 1/3, d, J=16Hz), 4.17 (IH x 2/3, d, J=15Hz), 4.30 (IH κ 1/3, d, J=16Hz), 4.63 (IH κ 2/3, d, J=15Hz) , 5.14 (IH, q, J=7Hz), 5.22- 5.33 (IH, m) , 6.81 (2H, d, J=8Hz), 6.90 (IK, d, J=8Hz), 6.98 (2H, d, J=8Hz), 7.07 (6H, a) , 7.22- 7.27 (IH, a), 7.44 (IH, d, J=8Hz), 7.64 (IH, d, J=8Hz), 8.05 (IH, t, J=7Hz), 8.14-3.21 (IH, m) (34) MASS (m/z) : 597 (M + +l) NMR (CDC1 3 , δ) : 2.59-2.72 (IH, m) , 2.73 (3H κ 2/3, s), 2.88 (3H x 1/3, s), 2.91-3.06 (2H, m) , 3.16 (IH, dt, J=4, 16Hz), 3.35 (2H, m) , 3.58 (6H, a), 4.12 (IH x 2/3, d, J " =15Hz) , 4.37 (IH x 1/3, d, J=16Hz), 4.53 (IH x 1/3, d, J=16Hz) , 4.73 (IH x 2/3, d, J=15Hz), 5.14-5.27 (2H, a), 6.94-7.15 (8H, a), 7.27-7.29 (3H, a), 7.44 (IH, d, J=8Hz) , 7.65 (IH, d, J=8Hz), 8.05-8.14 (2H, a), 8.32 (IH, d, J=5Hz) (35) MASS (m/z) : 593 (M + +l) NMR (CDCI3, δ) : 2.54-2.69 (IH, m) , 2.77 (3H κ 2/3, s), 2.89 (3H κ 1/3, s), 2.91-3.12 (2K, m) , 3.27 (IH, dt, J=4, 16Hz), 3.47 (2H, m) , 3.67 (6H, m) , 4.24 (IH κ 2/3, d, J=15Hz) , 4.42 (IK κ 1/3, d, J=16Hz), 4.49 (IH x 1/3, d, J=16Hz), 4.71 (IH x 2/3, d, J=15Kz), 5.03 (IH x 1/3, a), 5.11 (IH x 2/3, m) , 5.15 (IH, m) , 7.00-7.13 (5H, m) , 7.27-7.32 (3H, m) , 7.45 (IH, t, J=8Hz) , 7.52 (IH, s) , 7.58 (IH, d, J=8Hz), 7.64-7.72 (2H, m) , 8.21 (IH, d, J=8Hz), 8.39 (2H, d, J=5Hz) (36) MASS (m/z) : 664 (M + +l) NMR (CDCI3, δ) : 2.61-2.70 (IH, a), 2.57 (3H x 3/4,s), 2.81 (3H x 1/4, s), 3.07 (2K, a), 3.27-3.37 (IH, a), 3.48 (2H, a), 3.68 (6H, a), 4.18 (IH x 1/4, d, J=16Hz), 4.38 (IK x 1/4, d, J=16Hz) , 4.39 (IH x 3/4, d, J=15Hz), 4.62 (IH κ 3/4, d, J=15Hz) , 5.13 (2H, a), 7.06-7.22 (7H, a), 7.31 (IK, t, J=8Hz) , 7.44 (IH, t, J=8Hz), 7.52 (IH, s), 7.55-7.59 (3H, a), 7.70 (2H, t, J=8Hz) , 8.11 (IH, s), 8.21 (IH, a), 8.53 (IH κ 3/4, s), 8.55 (IH x 1/4, s) (37) MASS (a/z) : 663 (M + +l) NMR (CDC1 3 , δ) : 2.67 (3H κ 3/4, s), 2.73 (IH, dd, J=7, 16Hz), 2.80 (3H κ 1/4, s), 3.04 (2H, a) , 3.22 (IH, dd, J=3, 16Hz), 3.37 (2H, a), 3.60 (6H, a), 4.18 (IH κ 1/4, d, J=16Hz) , 4.33 (IH κ 3/4, d, J=15Hz), 4.35 (IH κ 1/4, d, J=15Hz), 4.61 (IH x 3/4, d, J=16Hz) , 5.18 (IH, q, J=7H∑), 5.27 (IH, m) , 6.99- 7.15 (10H, m) , 7.23 (IH, d, J=8H∑) , 7.44 (IH, d, J=8Hz), 7.51 (2H, m) , 7.63 (IH, d, J=8Hz) , 8.10 (IH, s), 8.13 (2H, m) , 8.50 (IH κ 3/4, s) , 8.53 (IH κ 1/4, s) (38) MASS (m/z) : 648 (M+H) + NMR (CDCI3, δ) : 2.55-2.72 (IH, m) , 2.68 (3/4 κ 3H, s) , 2.85 (1/4 κ 3H, s), 2.98-3.21 (2H, m) , 3.21- 3.38 (IH, m) , 3.38-3.79 (8H, m) , 4.29 (1/4 κ IH, d, J=17Hz), 4.56 (1/4 κ IH, d, J=17Hz) , 4.65 (3/4 κ 2H, ABq, Δ=0.22, J=15Hz) , 5.02-5.25 (2K, m) , 7.00- 8.28 (17H, m) , 8.65 (1/4 κ IH, d, J=2Hz), 8.73 (3/4 κ IH, d, J=2Hz) (39) MASS (m/z) : 647 (M+H) + NMR (CDCI3, δ) : 2.55-2.76 (IH, m) , 2.71 (3/4 κ 3H, s), 2.85 (1/4 κ 3H, s), 2.95-3.30 (3H, m) , 3.35- 3.75 (8H, m) , 4.30 (1/4 κ IH, d, J=17Hz), 4.57 (1/4 κ IH, d, J=17Hz), 4.63 (3/4 κ 2H, ABq, Δ=0.12, =15Hz), 5.05-5.28 (2H, a), 6.95-8.15 (17H, a), 8.65 (1/4 κ IH, d, J=2Hz) , 8.73 (3/4 κ IK, d, J=2Hz) , 9.75 (1/4 κ IH, s), 9.95 (3/4 κ IH, s) (40) MASS (a/z) : 648 (M+H) + NMR (CDCI3, δ) : 2.54-2.73 (IH, a) , 2.70 (2/3 κ 3H, s), 2.87 (1/3 κ 3H, s), 2.95-3.18 (2H, a) , 3.20- 3.78 (9H, a), 4.43 (1/3 x 2H, ABq, Δ =0.16, J=17Hz( 4.51 (2/3 κ IH, d, J=15Hz) , 4.80 (2/3 κ IH, d, J=15Hz), 5.00-5.22 (2H, m) , 7.08-7.80 (14H, m) , 7.95-8.30 (3H, m) , 8.90 (IH, d, J=2Hz) (41) MASS (m/z) : 647 (M+H) ' NMR (CDC1 3 , δ) : 2.55-2.75 (IH, a), 2.70 (2/3 κ 3H, s), 2.87 (1/3 x 3H, s), 2.95-3.14 (2H, a), 3.14- 3.33 (IH, m) , 3.33-3.75 (8H, ) , 4.46 (1/3 x 2K, ABq, Δ=0.15, J=17Hz) , 4.48 (2/3 x IH, d, J=15Hz), 4.82 (2/3 κ IH, d, J=15Hz), 5.08-5.25 (2H, m) , 6.94-7.72 (13H, a), 7.82-8.14 (4H, m) , 8.39 (IH, d, J=2Hz), 9.70 (1/3 κ IH, s), 9.72 (2/3 κ IH, s) (42) MASS (m/z) : 655 (M+H) + NMR (CDC1 3 , δ) : 2.20 (3H, s), 2.58-2.70 (IH, a), 2.61 (3/4 κ 3H, s), 2.72 (1/4 κ 3H, s), 2.93-3.18 (2H, a), 3.22-3.37 (IH, a), 3.37-3.80 (8H, a), 3.95 (1/4 κ IH, d, J=17Hz), 4.24 (3/4 κ IK, d, J=15Hz), 4.29 (1/4 x IH, d, J=17Hz), 4.56 (3/4 x IK, d, J=15Hz), 5.00-5.20 (2H, a), 7.06-7.80 (14H, a), 7.92-8.28 (2H, a) (43) MASS (m/z) : 654 (M+H) + NMR (CDCI3, δ) : 2.20 (3H, s), 2.58-2.72 (IH, m) , 2.59 (3/4 x 3H, s), 2.71 (1/4 x 3H, s), 2.88-3.12 (2H, m) , 3.14-3.30 (IH, m) , 3.33-3.78 (8H, m) , 3.88 (1/4 κ IH, d, J=17Hz) , 4.29 (1/4 κ IH, d, J=17Hz), 4.39 (3/4 x 2H, ABq, Δ=0.10, J=15HZ) , 5.00-5.18 (2H, m) , 6.90-8.50 (16K, m) , 9.84 (1/4 x IH, s) , 9.95 (3/4 κ IH, s) (44) MASS : 624 (M+l) NMR (CDCI3, δ) : 2.05-2.20 (IH, m) , 2.23-2.43 (4H, m) , 2.25 (3H, s), 2.45-2.60 (2H, m) , 2.70 (3 x 2/3H, s), 2.71-2.80 (IH, m) , 2.87 ( 3 κ 1/3H, s), 2.97- 3.14 (2H, m) , 3.40-3.53 (2H, m) , 3.60-3.75 (2H, m) 4.30 (2 κ 1/4H, d, J=16Hz), 4.35 (2 x 1/4H, d, J=15Hz), 4.41 (2 x I/4H, d, J=16Hz) , 4.69 (2 x 1/4H, d, J=15Hz), 4.61-4.72 (IH, m) , 5.10-5.20 (IH m) , 7.03-7.20 (8H, a), 7.23-7.34 (3H, m) , 7.40-7.5 (3H, a), 7.67 (IH, d, J=8Hz), 7.87-7.93 (IH, a), 8.1 " (IK, t, J=8Hz) (45) MASS (a/z) : 580 (M + +l) NMR (CDC1 3 , δ) : 2.64-2.75 (IH, a), 2.86 (IH, t, J=15Hz), 3.23-3.43 (4H, a), 3.68 (6H, a) , 4.59-4.7 (IH, a), 4.80-4.87 (IH, a), 5.21-5.37 (2K, a) , 6.8 (IH, a), 6.94-7.27 (11H, a), 7.37-7.62 (2H, a), 8.05-8.31 (2H, a) (46) MASS (a/z) : 581 (M + +l) NMR (CDCI3, δ) : 2.64-2.73 (IH, a), 2.35-3.00 (IH, m) , 3.31-3.59 (4H, m) , 3.67 (6H, m) , 4.57-4.75 (IH, m) , 4.84-4.92 (IH, a), 5.21 (IH, a), 5.39 (IH, d, J=16Hz), 6.89 (IH, d, J=8Hz) , 7.01 (IH, t, J=8Hz) , 7.12-7.31 (8H, a), 7.38-7.45 (IH, a) , 7.52-7.56 (2H, a), 7.67 (IH, d, J=8Hz), 7.92-8.12 (IH, a), 8.24-8.41 (IH, a) (47) MASS (a/z) : 603 (M+l) + NMR (CDCI3, δ) : 2.61 (IH x 1/3, dd, J=16.0, 6.0Hz) , 2.67 (IK x 2/3, dd, J=lδ.O, 6.0Hz), 2.79 (3H x 1/3, s), 2.87 (3H κ 2/3, s), 3.16-3.57 (5H, a) , 3.61- 3.80 (6H, a) , 4.37 (IK, a, J=14.5Hz) , 4.49 (IH κ 1/3, d, J=14.5Hz), 4.66 (IH κ 2/3, a, J=14.5H∑), 5.03-5.21 (2H, a), 6.81-6.90 (2K, a), 7.01-7.13 (3H, a), 7.23-7.36 (4H, a), 7.44 (IH, t, J=7.5Hz) , 7.51 (IH, a, J=15Hz), 7.55-7.74 (3H, a), 8.22 (IH, d, J=7.5Hz) (48) MASS (m/z) : 602 (M+l) + NMR (CDC1 3 , δ) : 2.60 (IH x 1/3, dd, J=16.0, 7.0Hz), 2.67 (IH x 2/3, dd, J=16.0, 7.0Hz), 2.80 (3H x 2/3, s), 2.88 (3H x 1/3, s) , 3.12-3.38 (3H, ) , 3.40- 3.55 (2H, m), 3.59-3.74 (6H, m) , 4.35 (IH x 2/3, d, J=14.5Hz), 4.39 (IH x 1/3, d, J=14.5Hz), 4.49 (IH x 1/3, d, J=14.5Hz), 4.70 (IH x 2/3, d, J=14.5Hz), 5.04-5.21 (2H, m) , 6.76-6.84 (2H, ) , 6.98-7.19 (5H, m) , 7.23-7.34 (4H, m) , 7.43 (IH, d, J=7.5Hz), 7.67 (IH, d, J=7.5Hz), 7.81 (IH x 1/3, d, J=7.5Hz), 7.89 (IH x 2/3, d, J=7.5Hz), 8.07 (IH, d, J=7.5Hz), 9.49 (IH x 1/3, br s) , 9.55 (IH x 2/3, br s) (49) MASS (m/z) : 676 (M+H) + NMR (CDCI3, δ) : 2.57-2.78 (IH, m) , 2.62 (2/3 x 3H,s), 2.83 (1/3 x 3H, s) , 2.93-3.11 (2H, m) , 3.11-3.29 (IH, m) , 3.29-3.72 (8H, m) , 3.93 (3H, s), 4.27 (2/3 x IH, d, J=15Hz), 4.30 (1/3 x 2H, ABq, Δ=0.20, J=17Hz) , 4.72 (2/3 x IH, d, J=15Hz) , 5.09-5.32 (2H, m) , 6.50 (IH, a), 6.93-8.14 (17H, a), 10.00 (IH, br s) (50) MASS (m/z) : 677 (M+H) + NMR (CDCI3, δ) : 2.53-2.72 (IH, a), 2.62 (2/3 κ 3H, s), 2.82 (1/3 x 3H, s), 2.95-3.13 (2H, a), 3.21- 3.38 (IH, m) , 3.38-3.88 (8H, m) , 3.94 (3H, s), 4.28 (1/3 x 2H, ABq, J=17HZ) , 4.29 (2/3 x IH, d, J=15H∑), 4.69 (2/3 κ IH, d, J=15Hz), 5.02-5.22 (2H, m.«, 6.51 (IH, d, J=2Hz), 6.97-7.78 (17H, a , 8.15- 8.27 (IH, a) (51) MASS (a/z) : 640 (M+H) + NMR (CDCI3, δ) : 2.58 (2/3 κ 3H, s), 2.62-2.76 (IH, a), 2.73 (1/3 κ 3H, s), 2.92-3.04 (2H, a), 3.05 (1/3 κ 6H, s), 3.07 (2/3 κ 6H, s), 3.13-3.30 (IH, a), 3.32-3.72 (8H, a), 3.82 (1/3 κ IK, a, J=17H∑i , 4.28 (1/3 κ IH, d, J=17Hz) , 4.32 (2/3 κ 2H, ABq, Δ=0.24, J=15Hz), 5.02-5.33 (2H, a) , 6.41 (IH, d, J=9Hz), 6.95-8.15 (14H, a), 10.0C 'IH, br s) (52) MASS (a/z) : 641 (M+H) + NMR (CDC1 3 , δ) : 2.55-2.31 (IH, a), 2.56 (2/3 κ 3H, s), 2.72 (1/3 κ 3H, s), 2.97-3.07 (2H, aj , 3.03 (6H, s), 3.22-3.38 (IH, a), 3.38-3.78 (8H, a), 3.80 (1/3 κ IH, d, J=17Hz), 4.27 (1/3 κ IH, a, J=17Hz), 4.32 (2/3 κ 2H, ABq, Δ=0.24, J=15H∑) , 4.98-5.30 (2K, a) , 6.42 (1/3 κ IH, d, J=9Hz), 6.45 (2/3 κ IH, d, J=9Hz) , 7.04-8.25 (14H, a) (53) MASS (a/z) : 662 (M+H) + NMR (CDCI3, δ) : 2.55-2.71 (IH, a), 2.68 (3/4 κ 3H, s), 2.82 (1/4 κ 3H, s), 2.92-3.14 (2H, a), 3.20- 3.35 (IH, a), 3.35-3.76 (8H, a), 4.27 (1/4 κ 2H, ABq, Δ=0.20, J=17Hz), 4.49 (3/4 κ 2H, ABq, Δ=0.20, J=15Hz), 5.05-5.21 (2H, a), 6.95-8.13 (19H, a), 9.55 (IH, br s) (54) MASS (a/z) : 663 (M+HA NMR (CDCI3, δ) : 2.57-2.72 (IH, a), 2.68 (3/4 κ 3H, s), 2.81 (1/4 κ 3H, s) , 2.97-3.18 (2H, a) , 3.25- 3.40 (IH, a), 3.40-3.82 (8H, a) , 4.26 (1/4 κ 2H, ABq, Δ=0.20, J=17Hz) , 4.49 (3/4 κ 2H, ABq, J=15Hz), 5.03-5.20 (2H, a) , 7.00-7.86 (18H, a), 8.14-8.27 (IH, m) (55) MASS (m/z) : 664 (M+H) + NMR (CDCI3, δ) : 2.58 (2/5 κ 3H, s) , 2.60-2.73 (IH, m) , 2.62 (3/5 κ 3H, s) , 2.65 (3/5 κ 3H, s; , 2.80 (2/5 κ 3H, s), 2.92-3.12 (2H, m) , 3.17-3.30 (IH, m) , 3.36-3.74 (8H, m) , 3.70 (3K, s) , 4.12 (2/5 x IH, d, J=17Hz) , 4.43 (3/5 x IH, d, J=15Hz) , 4.57 (2/5 x 1H, d, J=17Hz), 4.75 (3/5 x IH, d, J=15Kz) , 5.02-5.32 (2H, m) , 6.38-8.13 (15H, ) , 9.73 (2/5 κ IH, s) , 10.52 (3/5 κ IH, s) (56) MASS (m/z) : 665 (M+H) + NMR (CDC1 3 , 5) : 2.58-2.72 (IH, m) , 2.58 (3H, s), 2.60 (2/3 κ 3H, s), 2.78 (1/3 κ 3H, s), 2.92-3.14 (2H, m) , 3.22-3.38 (IH, m) , 3.40-3.80 (8H, m) , 3.70 (3H, s), 4.13 (1/3 κ IH, d, J=17Hz), 4.48 (2/3 κ IK, d, J=15H∑), 4.53 (1/3 κ IH, d, J=17Hz) , 4.69 (2/3 κ IH, d, J=15H∑), 5.02-5.30 (2H, m) , 6.85-7.80 (14H, a) , 8.15-8.28 (IK, a) (57) MASS (a/z) : 586 (M+K) + NMR (CDCI3, δ) : 2.53-3.00 (3H, a), 2.87 (2/3 κ 3H, s), 2.89 (1/3 κ 3H, s), 3.16-3.33 (IH, a), 3.33- 3.76 (8H, a), 4.32 (2/3 κ IH, d, J=15Hz) 4.51 (1/3 κ 2H, ABq, Δ=0.05, J=17Hz) , 4.72 (2/3 κ IH, d, J=15Hz), 5.01-5.22 (2H, a), 6.18 (1/3 κ IH, s), 6.22 (2/3 x IH, s), 6.92-8.14 (14H, a), 9.66 (1/3 x IH, br s) , 9.70 (2/3 x IH, br s) (58) MASS (a/z) : 587 (M+H) + NMR (CDCI3, δ) : 2.53-3.05 (3H, a), 2.88 (3H, s), 3.22-3.80 (9H, a), 4.35 (2/3 κ IH, d, J=15Hz) , 4.51 (1/3 κ 2H, ABq, J=17Hz) , 4.70 (2/3 κ IH, d, J=15Hz), 4.98-5.18 (2H, a), 6.21 (1/3 x IH, ε), 6.27 (2/3 x IH, s), 7.03-7.74 (13H, a) , 8.22 (IK, d, J=8Hz) (59) MASS (a/z) : 600 (M+H) + NMR (CDCI3, δ) : 2.59-2.73 (IH, a), 2.63 (2/3 x 3H, s), 2.81 (1/3 x 3H, s), 2.92-3.14 (2H, a), 3.18- 3.32 (IH, a), 3.37-3.75 (8H, a), 3.81 (1/3 x 3H, s), 3.84 (2/3 κ 3K, s) , 4.08 (1/3 x 2H, A3q, Δ=0.18, J=17Hz), 4.12 (2/3 x IH, a, J=15Hz), 4.42 (2/3 κ IH, d, J=15Hz), 5.00-5.28 (2H, a) , 6.95-8.10 (14H, a) , 9.63 (IK, br s) 60) MASS (a/z) : 601 (M+H) + NMR (CDCI 3 , δ) : 2.56-2.72 (IH, a), 2.62 (2/3 κ 3H, s), 2.80 (1/3 κ 3H, s), 2.90-3.18 (2H, a) , 3.24- 3.33 (IH, a), 3.38-3.80 (8H, a) , 3.82 (1/3 κ 3H, s) , 3.85 (2/3 x 3H, S), 4.06 (1/3 x 2K, ABq, Δ=0.20, J=17Hz) , 4.13 (2/3 x IK, a, J=15Hz), 4.42 (2/3 x IH, d, J=15Hz) , 4.98-5.25 (2K, a) , 6.98-7.72 (13K, a) , 8.13-8.25 (IH, a) (61) MASS (a/z) : 630 (M+H) + NMR {CDCI3, δ) : 2.52-2.92 (IH, a), 2.72 (2/3 κ 3H, s), 2.85-3.08 (2H, a), 2.87 (1/3 κ 3H, s) , 3.13- 3.30 (IH, a), 3.33-3.75 (8H, a), 4.21 (2/3 κ IH, d, J=15Hz), 4.41 (1/3 κ 2H, ABq, J=17HZ) , 4.74 (2/3 κ IH, d, J=15Hz), 5.04-5.25 (I-, m) , 6.90-8.12 (16H, a), 9.77 (1/3 κ IH, s), 9.82 (2/3 κ IH, s) (62) MASS (a/z) : 631 (M+H) + NMR (CDCI3, δ) : 2.51-2.78 (IH, a) , 2.72 (2/3 κ 3K, s), 2.84 (1/3 κ 3H, s) , 2.85-3.11 (2H, a) , 3.20- 3.37 (IH, a) , 3.37-3.82 (8K, a), 4.25 (2/3 x IH, a, J=15Hz), 4.40 (1/3 x 2H, s), 4.71 (2/3 x IH, a, J=15Hz), 4.98-5.18 (2H, a) , 6.90-7.74 (15H, m) , 8.20 (IH, d, J=9Hz) (63) MASS (m/z) : 586 (M+H) " NMR (CDCI3, δ) : 2.53-2.75 (IH, a) , 2.60 (2/3 x 3H, s), 2.87 (1/3 κ 3H, s), 2.95-3.31 (3H, a) , 3.31- 3.78 (8H, a), 4.24 (2/3 κ IH, d, J=15Hz; , 4.45 (1/3 κ 2H, ABq, Δ=0.13, J=17HZ) , 4.81 (2/3 κ IH, d, J=15Hz) , 5.08-5.32 (2H, a), 5.97-6.21 (2H, a), 6.92-8.15 (13H, a), 9.82 (1/3 x IH, br s), 9.88 (2/3 x IH, br s) (64) MASS (m/z) : 587 (M+H) + NMR (CDC1 3 , δ) : 2.52-2.72 (IH, m) , 2.79 (2/3 x 3H, s), 2.85 (1/3 κ 3H, s), 2.96-3.19 (2H, m) , 3.21- 3.38 (IH, a), 3.38-3.82 (8H, a), 4.29 (2/3 κ IK, d, J=15Hz), 4.43 (1/3 κ 2H, ABq, J=17HZ) , 4 . 11 (2/3 κ IH, d, J=15Hz), 5.01-5.28 (2H, a), 6.03-6.27 (2H, a), 7.07-7.80 (12H, a), 3.15-8.30 (IK, a) (65) MASS (m/z) : 603 (M+H) ÷ NMR (CDCI3, δ) : 2.51-2.70 (IH, m) , 2.81 (2/3 κ 3H, s), 2.86 (1/3 κ 3H, s) , 2.96-3.18 (2H, m) , 3.18- 3.38 (IH, a), 3.33-3.82 (8H, a), 4.30 (2/3 κ IK, d, J=15Hz), 4.45 (1/3 κ 2H, ABq, Δ=0.18, J=17Hz) , 4.77 (2/3 x IH, d, J=15Hz), 4.96-5.25 (2K, a), 6.05-6.25 (2H, a) , 7.05-8.22 (13H, a) (66) MASS : 648 (M+l) NMR (CDCI3, δ) : 2.60-2.78 (IH, a), 2.70 (3 x 2/3H, s), 2.85 (3 x 1/3H, s), 2.95-3.12 (2H, a), 3.13- 3.30 (IH, a), 3.31-3.50 (2H, a), 3.51-3.90 (6H, a), 4.36 (2 x 1/6H, d, J=16Hz), 4.55 (2 x 1/6H, d, J=16Hz), 4.61 (2 x 1/3H, d, J=15Hz), 4.73 (2 x 1/3H, d, J=15Hz), 5.10-5.33 (2K, a), 6.95-7.35 (8H, a), 7.36-7.50 (2H, a), 7.62 (IH, d, J=8H∑) , 7.78 (1 κ 1/3H, s), 7.83 (1 κ 2/3H, s), 7.93-8.20 (3H, a), 8.81 (2H, s) (67) MASS : 649 (M+l) NMR (CDCI3, δ) : 2.61-2.70 (IH, a), 2.71 (3 κ 2/3H, s), 2.88 (3 κ 1/3K, s) , 3.00-3.18 (2H, a), 3.29 (IH, t, J=15Hz), 3.40-3.59 (2H, a), 3.60-3.80 (6H, a), 4.38 (2 κ 1/6H, d, J=16Hz) , 4.58 (2 x 1/6H, d. J=16H∑) , 4.62 (2 x 1/3H, d, J=15H∑) , 4.79 (2 x 1/3H, d, J=15Hz), 5.08-5.22 (2H, m) , 7.11-7.25 (5H, m) , 7.26-7.37 (IH, m) , 7.40-7.50 (2H, m) , 7.51 (IH, s), 7.56 (IH, d, J=8Hz), 7.68 (IH, d, J=8Hz), 7.75- 7.90 (2H, m) , 8.02 (IH, d, J=8H∑), 8.20 (1 κ 1/3H, d, J=8Hz) , 8.23 (1 κ 2/3H, d, J=8Hz), 8.80 (2H, s) (68) MASS : 646 (M+l) NMR (CDC1 3 , δ) : 2.02 (3 κ 2/3H, s), 2.68 (3 κ 1/3K, s), 2.71-2.90 (IH, m) , 3.17-3.50 (5H, m) , 3.51-3.70 (6H, m) , 3.67 (2 κ 1/6H, d, J=16Hz), 3.96 (2 κ - 1/6H, d, J=16Hz), 4.18 (2 x 1/3H, d, J=15Hz), 4.50 (2 x 1/3H, d, J=15Hz), 5.27-5.50 (2H, m) , 6.71-6.30 (2 κ 1/3H, m) , 6.90-7.00 (2 κ 2/3H, m) , 7.01-7.32 (8H, a), 7.33-7.57 (3H, a), 7.60-7.70 (2H, m) , 7.74 (IH, d, J=8Hz), 7.93-8.12 (IH, m) , 3.24 (2 κ 1/3H, d, J=8Hz), 8.31 (2 x 2/3H, d, J=8Hz) (69) MASS : 647 (M+l) NMR (CDCI3, δ) : 1.99 (3 x 2/3H, s), 2.61 (3 κ 1/3H, s), 2.58-2.74 (IH, m) , 3.28-3.60 (5H, a), 3.60-3.80 (6H, m) , 3.72 (2 x 1/6H, d, J=16Hz), 3.89 (2 x 1/6H, d, J=16Hz), 4.19 (2 x 1/3H, d, J=15Hz) , 4.40 (2 x 1/3H, d, J=15Hz), 5.08-5.22 (IK, m) , 5.27-5.40 (IH, m) , 6.68-6.78 (2 κ 1/3H, m) , 6.90-6.99 (2 κ 2/3H, m) , 7.10-7.37 (6H, m) , 7.38-7.62 (5H, m) , 7.62-7.90 (4H, m) , 8.10-8.40 (2H, ) (70) MASS : 598 (M+l) NMR (CDCI3, δ) : 2.53-2.70 (IH, m) , 2.71 (3 x 2/3H, s), 2.85 (3 x 1/3H, s), 2.90-3.15 (2H, m) , 3.22- 3.35 (IH, m) , 3.37-3.58 (2H, m) , 3.60-3.80 (6H, m) , 4.37 (2 x 1/3H, d, J=15Hz) , 4.38 (2 x 1/6H, d, J=16Hz), 4.43 (2 κ 1/6H, d, J=16Hz), 4.60 (2 κ 1/3H, d, J=15Hz), 5.00-5.20 (2H, m) , 7.98-8.18 (3H, m) , 7.22-7.38 (4H, m) , 7.40-7.73 (6H, a), 8.20 (IH, d, J=8Hz), 8.33 (1 κ 1/3H, s) , 8.44 (IH, d, J=2Hz) , 8.49 (1 x 2/3H, s) (71) MASS : 597 (M+l) NMR (CDC1 3 , δ) : 2.58-2.75 (IH, a), 2.78 (3 x 2/3H, s), 2.88 (3 x 1/3H, s), 2.91-3.30 (3H, a), 3.31- 3.50 (2H, a), 3.51-3.70 (6H, a), 4.31 (2 κ 1/3H, d, J=15Hz), 4.42 (2 κ 1/6H, d, J=16Hz), 4.51 (2 κ 1/6H, d, J=16Hz), 4.67 (2 κ 1/3H, d, J=15Hz), 5.10- 5.30 (2H, a), 6.90-7.18 (5H, a), 7.20-7.33 (4H, a), 7.34-7.50 (2H, a), 7.64 (IH, d, J=8Hz) , 7.95-8.10 (2H, m) , 8.32 (1 x 1/3H, s), 8.43 (1 x 2/3H, s), 8.45 (IH, s) (72) MASS : 658 (M+l) NMR (CDCI3, δ) : 2.27 (3H, s) , 2.31-2.48 (4H, m) , 2.52 (3 x 2/3H, s), 2.64-2.80 (IH, m) , 2.70 (3 x 1/3H, s), 2.93-3.15 (2H, m) , 3.29 (IH, d, J=15Hz) , 3.39- 3.57 (2H, m 3.58-3.73 (2H, m) , 3.88 (3H, s) , 4.18 (2 x 1/6H, d, J=16Hz), 4.19 (2 x 1/3H, d, J=15Hz) , 4.23 (2 x 1/6H, d, J=16Hz), 4.49 (2 x 1/3H, d, J=15Hz), 4.98-5.22 (2H, a), 6.61 (1 κ 1/3H, d, J=8Hz), 6.63 (1 x 2/3H, d, J=8Hz) , 7.00-7.37 (6H, m) , 7.40-7.60 (2H, m) , 7.68 (1 x 1/3H, d, J=8Hz) , 7.70 (1 x 2/3H, d, J=8Hz), 7.81 (1 x 1/3H, s) , 7.90 (1 x 2/3H, s), 7.93 (IH, d, J=8Hz), 8.11 (IH, d, J=8Hz), 8.80 (IH, d, J=8Hz) (73) MASS : 563 (M+l) NMR (CDCI3, δ) : 0.70-0.95 (3H, m) , 1.15-1.45 (4H, m) , 1.55-1.85 (2H, a), 2.60-2.72 (IH, a), 2.90 (3 x 1/3H, s), 3.00 (3 x 2/3H, s), 3.30 (IH, d, J=15Hz), 3.38-3.58 (2H, a), 3.58-3.77 (6H, a), 4.38 (2 x 1/3H, d, J=15Hz), 4.62 (2 x 1/3H, s), 4.76 (2 x 1/3H, d, J=15Hz), 4.83-4.99 (IH, a), 5.05-5.20 (IH, a), 7.10-7.37 (5H, a), 7.37-7.46 (2H, a), 7.49-7.60 (2H, a), 7.61-7.78 (2H, a), 8.27 (IH, d, J=8Hz) (74) MASS : 562 (M+l) NMR (CDCI 3 , δ) : 0.60-0.90 (3H, a), 1.03-1.38 (4H, a), 1.50-1.80 (2H, a), 2.60-2.75 (IH, a), 2.83 (3 κ 1/3H, s), 2.91 (3 κ 2/3H, s), 3.10-3.28 (IH, a), 3.29-3.43 (2H, a), 3.44-3.68 (6H, a), 4.22 (2 κ 1/3H, d, J=15H∑), 4.52 (2 κ I/6H, d, J=16H∑) , 4.61 (2 κ 1/6H, d, J=16Hz) , 4.80 (2 κ I/3H, d, J=15H∑), 4.86-5.00 (IH, a), 5.12-5.35 (IH, a), 7.01 (IH, s) , 7.03-7.38 (7H, a), 7.42 (IH, d, J=8Hz), 7.62 (IH, a, J=8Hz), 7.97 (1 κ 1/3H, d, J=8Hz) 8.07 (1 x 2/3H, d, J=8Hz), 8.11 (IH, d, J=8Hz) (75) MASS : 644 (M+l) NMR (CDCI3, δ) : 2.58-2.70 (IH, a), 2.61 (3 x 2/3H, s), 2.73 (3 x 1/3H, s), 2.97-3.12 (2H, a) , 3.22- 3.34 (IH, a), 3.40-3.58 (2H, m) , 3.60-3.78 (6H, m) , 3.87 (3H, s), 4.22 (2 x 1/3H, d, J=15Hz) , 4.23 (2 x 1/6H, d, J=16Hz), 4.31 (2 x 1/6H, d, J=16Hz), 4.51 (2 x 1/3H, d, J=15Hz), 5.02-5.21 (2K, m) , 6.61-6.70 (IH, a), 7.08-7.23 (5H, a), 7.30-7.50 (3H, a) , 7.72-7.98 (5H, a), 8.13 (IH, d, J=8Hz) Exaaple 38 The following coapound was obtained according to a siailar aanner to that of Exaaple 8. MASS (a/∑) : 610 (M+H) + NMR (CDCI3, δ) : 2.2-2.3 (2H, a) , 2.4-2.6 (2H, a), 2.73 (2/3 x 3H, s), 2.93 (1/3 x 3H, s), 3.0-3.1 (2H, a), 3.3-3.6 (8H, a), 4.2-4.8 (2H, m) , 5.0-5.1 (IK, m) , 5.2-5.3 (IH, a), 7.0-7.7 (15H, a), 7.72 (IH, br s), 8.05 (IH, br s), 8.50 (IH, br s) (IH, a) , 5.2-5.3 (IH, a) ' , 7.0- .- '15 H , . l , , ~ .72 (IH, br s) , 8.05 (IH, br si, 8.5f ' IK, br ≤ Example 39 To a mixture of Starting Compound (112 ag! and triethylamine (70 ul) in dichloromethane A .2 mi; was added (benzofuran-2-yl) sulfonyi chloride (68 mg) with ice-cooling. The mixture was stirred at rooa temperature fcr 12 hours then subjected to column chromatography (silica gel, chlcrofcrm/methanol = 50/1) to give Object Compound ,130 ag) as a white powder. MASS (a/z) : 633 (M+H)" NMR (CDC1 3 , δ; : 2.38-2.59 (IH, a), 2.52 (2/3 x 3H, s), 2.73 (1/3 x 3K, s), 2.81-3.04 (2H, a), 3.04- 3.72 (9H, m) , 3.98 (1/3 x IH, d, J=17Hz), 4.24 (1/3 κ IH, d, J=17Hz), 4.25 (2/3 κ IH, a, J=15Hz), 4.28- 4.44 (IK, m) , 4.57 (2/3 κ IH, a, J=15Hz), 4.36-5.05 (IH, m) , 6.78-6.90 (17H, m) Example 40 The following object compounds were obtained according to a similar manner to that of Example 39. (1) MASS (m/z) : 571 (M+HA NMR (CDC1 3 , δ) : 2.61 (3/4 x 3H, s), 2.74 ,1/4 x 3H, s), 2.78-3.05 (2H, m) , 3.50-3.78 (2H, a), 3.87-4.04 (IH, m) , 3.88 (1/4 x IH, d, J=17Hz), 4.12 (IH, br s), 4.30 (1/4 x IH, a, J=I7Hz), 4.42 (3/4 x 2H, ABq, J=15Hzi, 4.90-5.05 (IH, a( , 6.45 (IH, br s), 6.96-7.72 (13H, a).. 6.00-8.22 (IH, a, (2i MASS (a/z) : 598 (M+H) " NMR (CDC1 3 , δ) : 2.51 (3/4 x 3H, s), 2.58-2.95 ;2H, a), 2.72 (1/4 κ 3H, s), 2.95-3.34 (2H, a), 4.08 (1/4 x 2H, ABq, Δ=0.21, =17Hz) , 4.24 (3/4 x IH, d, J=15Hzi , 4.31-4.44 'IH, jr.) , 4.55 '2 A x IH, a, J=15Hz, , 4.90-5.06 'IH, a), 6.90-A53 iAH, n , 8.14-8.55 (3H, a) (3) MASS (a/z) : 646 (MτH) + NMR (CDC1 3 , δ) : 2.11-2.40 (4H, a,, 2.25 ,3H, s. , 2.40-2.55 (IH, a) , 2.50 (2/2 x 2H, s\ 2 A3 1/3 x 3H, s), 2.82-3.05 (2H, a), 3.13-5 A3 (5H, a), 4.11 (1/3 κ 2H, A3q, Δ=0.25, J=17Hz) , 4.22 (2/3 x IH, d, J=15Hzi, 4.25-4.41 (IH, a, , 4.53 X/3 x IK, d, J=15Hz), 4.89-5.05 (IH, a) , 6.78-7.9C (17H, a) Exaaple 41 The following object coapounas were obtained according to a siaiiar aanner to that of Exaaple 1. (1) MASS : 573 (M+l) NMR (CDCI3, δ) : 2.00 (3 κ 1/3H, s) , 2.01 (3 x 2/3K, 5) , 2.70 (3 x 2/3H, s) , 2.91 (3 κ 1/3K, s, , 2.93- 3.07 (2H, a) , 3.07-3.23 (2K, a) , 4.22 (2 x 1/3H, s) , 4.27 (2 κ I/3H, d, J=15Kz) , 4.97 (2 κ 1/3K, d, J=15Hz) , 5.10-5.40 (IK, a) , 5.60-5.60 (IH, a, , 6.78 (IH, d, J=8Hz) , 6.82 (IH, d, J=8Hz, , 6.39-7.15 (UK, a), 7.13-7.40 (5H, a), 7.48 ,1H, d, J=8Hz) , 7.67 (IH, a, J=8H∑) , 8.99 (IH, t, =3Hz) (2) MASS : 574 (M+l) NMR (CDCi 2 , δ) : 2.22 (3H, si , 2. cZ (3 x 2/3K, 5 , 2.83 (3 κ 1/3H, s), 2.90-3.C3 (2H, a, , 3.08-3.20 (2H, ) , 4.11 (2 κ 1/6H, d, AlόHzj , 4.27 (2 κ 1/6H, d, J=16Hz) , 4.32 (2 κ 1/3H, a, J=15H∑) , 4.62 (2 κ 1/3K, d, J=15Hz) , 4.95-5.08 (IH, __.) , 5.10-5.21 (IH, m) , 6.90-7.33 (AH, m) , 7.4C 7.43-7.56 (2H, a) , 7.63 (IK, d, J=6Hz; ( 3 ) MASS : 571 (M+ l ) NMR (CDC1 3 , δ) : 2.73 (3 x 1/4H, s ] , 3AC (3 x 3/4K, s), 2.90-3.30 (2H, a,' , 3.30-3.46 :1H, a), 4.40-4.53 (IH, m) , 4.54-4.77 (2K, m) , 4."8-4.96 (2K, a), 5.10-5.20 (IH, a), 5.50-5.68 (IH, a), 5.70-7.50 (19H, a), 7.58 (1 x 3/4H, d, J=3Hz), 7.72 (1 x 1/4H, a, J=8Hz), 9.73 (1 x 1/4H, s), 9.82 (1 x 3/4H, s) (4) MASS : 517 (M+l) NMR (CDCI3, δ) : 0.75 (3 κ 1/5H, t, J=8Hz) , 0.81 (3 κ 4/5H, t, J=8Hz), 1.06-1.48 (4H, a), 1.62-1.90 (2H, a), 2.99 (3 κ 1/5K, s), 3.11 (3 x 4/5H, si, 3.70- 3.90 (IH, a), 4.01-4.22 (IH, a), 4. 3 ' 2 x 1/2H, d, J=15Hz), 4.32 (2 x 1/2H, d, J=15Hz) , 4.83-5.10 (3H, m) , 7.27 (IH, t, J=7Hz), 7.38 (IH, t, J=6Hz), 7.42- 7.53 (3H, m) , 7.54-7.90 (5H, a), 7.98-8.18 (2H, m) , 8.80 (1 x 4/5H, d, J=2Hz) , 8.90 (1 κ 1/5H, d, J=2Hz) (5) MASS : 516 (M+l) NMR (CDCI3, δ) : 0.69 (3 x 1/5H, t, J=8Hz), 0.79 (3 x 4/5H, t, J=8Hz), 1.08-1.45 (4H, m) , 1.60-2.01 (2H, m) , 3.10 (3 x 1/5K, s), 3.22 > 3 x 4/5H, s), 3.90- 4.16 (2H, a), 4.60 (2 x 2/5H, a, J=15Hz) , 4.71 (2 x 1/5H, s), 5.01 (2 x 2/5H, d, J=15Kz) , 4.82-5.15 (IH, a), 5.50-5.70 (IH, a), 6.58 (1 κ 1/5H, s), 6.71 (1 x 4/5H, s), 6.92-7.20 (3H, a), 7.30-7.42 (3H, a), 7.5C (IK, a, J=6Kz) , 7.51-7.76 (2H, a) , 7.81 (IH, s), 7.93 (IH, a, J=8Hz), 6.71 (1 x 4/5H, s), 8.82 (1 κ 1/5H, s) , 3.90 (1 κ 1/5H, d, J=3Hz) , 9.00 (1 κ 4/5H, d, J=8Hz) (6) MASS : 578 (M+l) NMR (CDCI3, δ) : 0.72 (3 κ 1/4H, t, =8Hz) , 0.73 (3 κ 3/4H, t, J=8Hz) , 1.16-1.36 !4H, a) , 1.49-1.80 !2K, a), 2.92 (3 x 1/4H, s), 3.00 (3 x 3/4H, s), 3.28- 3.52 (2H, a), 4.53 (2 x. 3/8H, a, J=15Hz , 4.79 (2 x 1/8H, a, J=16Hz, , 4.55 (2 x 1/6H, a, J=16Hz , 4.90 (2 x 3/8H, a, J=15H∑), 4.83-5.01 (IH, a , 5.02-5.18 (IK, a), 7.18 (iH, , J=8Hz) , 7.21-7.35 (2H, a), 7.41 (IH, t, J=8Hz), 7.43-7.89 (7H, a), 7.95-8.23 (3H, a) , 8.59 (IH, a, J=4Hz), 6.73 ( IH, a, J=2Hz) , 3.79 (IH, a, J=8H∑) (7) MASS : 577 (M+l) NMR (CDC1 3 , δ) : 0.62 (3 x 1/4H, t, J=8H∑) , 0.68 (3 x 3/4H, t, J=8Kz), 0.95-1.30 (4H, a), 1.38-1.57 (IH, a), 1.53-1.72 (IH, a), 2.92 (3 κ 1/4H, s, , 2.98 (3 x 3/4H, s), 2.98-3.50 (2H, a;, 4.63 (2 x 3/3H, d, J=15H∑), 4.64 (2 x 1/8H, 0, J=16Kz) , 4.78 (2 x 3/8H, a, J=15H∑), 4.61 (2 κ 1/8H, d, J=16Hz,, 4.82- 5.05 (IK, a), 5.17-5.38 (IH, a), 6.97-7.12 (3H, a), 7.13-7.22 (2H, a), 7.32-7.59 (3H, a), 7.60-7.80 (3H, m) , 7.94 (IH, s), 8.06-8.18 (2H, m) , 8.41 (1 κ 1/4H, d, J=8Hz), 8.48 (1 x 1/4H, d, J=4Hz), 3.51 (1 κ 3/4H, d, J=4Hz) , 8.69 (1 κ 3/4H, a, J=3Hzi, 8.73 (1 κ 3/4H, d, J=2Hz) , 8.78 (1 κ 1/4H, a, J=2H∑) (8) MASS : 575 (M+l) NMR (CDCI3, δ) : 2.06-2.23 (2H, m) , 2.10 (3H, s) , 2.50-2.70 (2H, .i , 2.61 (3 κ 2/3H, s:, 2.81 (3 x 1/3H, s), 2.92-3.12 (2H, m) , 3.91 (3H, s) , 3.99 (2 x 1/6H, d, J=16Hz) , 4.31 (2 x 1/2H, d, =15Hz, , 4.32 (2 x 1/6H, d, J=16Hz) , 4.52 (2 x 1/3H, J=15Hz), 4.97 (IH, q, J=8Kz), 5.12 (1 x 2/3H, q, J=8Hz) , 5.27 (1 x 1/3H, q, =3Hz) , 6.6 " (1 x 1/3H, d, J=8Hz), 6.69 (1 x 2/3H, d, J=8Hz; , 7.05-7.21 (5H, m) , 7.22-7.48 (5H, a), 7.51 (IH, a, J=3Hz) , 7.54 (IH, S) , 7.69 (IH, d, J=8H∑! , 7.89 (1 x 1/3H, a, J=2Hz), ".99 (1 x 2/3H, a, J=2HZ) (9) MASS : 591 (MAL) NMR (CDCI 3 , δ) : 2.07-2.23 (2H, a, , 2.09 (3H, s , 2.50-2.72 (2H, m) , 2.65 (3 x 2/3H, s), 2.79 (3 x 1/3K, s), 2.92-3.12 (2H, a', 3.39 (3H, s), 3.94 (2 x 1/6H, d, J=16Hz) , 4.29 (2 x 1/3H, d, J=15H∑) , 4.33 (2 κ 1/6H, d, J=16Hz), 4.51 (2 κ 1/3H, a, J=15Hz), 4.91 (IH, q, J=8Hz) , 5.11 (1 κ 2/3H, q, J=8Hz) , 5.25 (1 κ 1/3H, q, J=8Hz), 6.63 (1 κ I/3K, d, J=8Kz), 6.67 (1 x 2/3H, d, J=6Hz), ".02-".21 (5H, a), 7.30-7.60 (5H, a), 7.73-7.90 (3K, a 1 , 7.87 (1 x 1/3H, d, J=2Hz), 7.98 (1 x 2/2H, d, J=2Hz) (10) MASS : 574 (M+l) NMR (CDCI3, δ) : 2.07 (3 x 2/3H, sj, 2.08 (3 x 1/3H, s), 2.10-2.41 (2H, a), 2.53-2.63 (2H, a), 2.70 (3 x 2/3H, s), 2.93-3.12 (2H, m) , 2.97 ■ (3 x 1/3K, s), 3.91 (3 x 1/3H, s), 3.92 (3 x 2/3H, s) , 4.02 (2 x 1/6H, d, J=16Hz), 4.32 (2 κ I/6H, d, J=16Hz , 4.42 (2 κ 1/3H, d, J=15Hz) , 4.70 (2 x 1/3H, d, =15Hz) , 5.30-5.50 (IH, m) , 5.51-5.52 (IH, m) , 6.62 '1 x I/3K, d, J=8Hz), 6.69 (1 x 2/3H, d, J=6Hz), 6.93- 7.18 (7K, a), 7.19-7.40 (3H, a;, 7.50 (IH, a, J=8Hz), 7.69 (IH, d, J=3Hz) , 7.89 (1 x 1/3H, a, J=2Hz), 8.02 (1 κ 2/3H, d, J=2Hz), 9.03 (1 κ 2/3H, d, J=8Hz), 9.11 (1 κ 1/3K, a, J=8Hz) (11) MASS : 561 (M+l) NMR (CDC1 5 , δ) : 0.72 (3 x 1/4H, t, J=8H∑), 0.63 (3 κ 3/4H, t, J=8Hz), 1.10-1.40 (4H, a), 1.60-1.90 (2H, a), 2.08 (3H, s), 2.12-2.23 (2K, a), 2.53-2.73 (2H, m) , 3.01 (3 x 1/4H, s), 3.11 (3 x 3/4H, s), 4.7C (2 κ 3/8H, d, J=15Hz), 4.69 (2 κ 1/4H, s) , 4.91 (2 κ 3/8H, d, J=15Hz), 4.93-5.11 (2K, a), 7.20-".33 (IH, a), 7.34-7.60 ( 6H, π) , A 60-7.89 , JH, a , 6.01 'IH, s) , 8.10 (1 κ 3/4H, a, J=3Hz), 8.12 (1 x 1/4H, d, J=8Hz) , 8.81 (1 κ 3/4H, si, 8.33 X x 1/4H, s) (12) MASS : 560 (Mι-1) NMR (CDC1 3 , Si : C.59 (3 x 1/4H, t, J=3Hz, , 0.65 (3 x 3/4H, t, J=8H∑>, 0.98-1.50 (4H, a, , 1.53-1.90 (2H, a) , 2.00 (3 x 3/4H, s) , 2.02 (2 x ι/4 , S ) , 2.10- 2.33 (2H, a) , 2.52-2.80 (2H, a}, 3.13 '3H, s», 4.79 (2 x 3/8H, d, J=15Hz) , 4.91 (2 κ 1/4H, s, , 5.1C (2 κ 3/8H, d, J=15Hz), 5.12-5.31 (IH, a), 5.43-5.60 (IH, a), 6.96-7.13 (3H, a) , 7.27-7.47 (2H, a) , 7.50-7.53 (2H, a), 7.69-7.9C (2H, π) , 3. CO (1 κ 1/4H, si , 8.06 (1 x 3/4H, si, 3.11 (IH, d, J=3Hz) , 8.72-9.00 (2H, a) (13) MASS : 566 (MA) NMR (CDC1 3 , δ) : 0.58 (3 x 1/4H, t, J=8Hz), 0.63 (3 κ 3/4H, t, J=8Kz) , 0.93-1.37 (4H, aι , 1.5C-1.80 (2H, a), 3.00 (3 x 1/4H, S), 3.07 (3 x 3/4K, si , 3.12- 3.28 (2H, a) , 4.61 (2 x 3/8H, a, J=15Hz) , 4.71 (2 κ 1/8H, d, J=16Hz) , 4.87 (2 κ 3/8H, a, J=15Hz) , 4.99 (2 κ 1/8H, d, J=16Hz), 4.90-5.10 (IH, a) , 5.30-5.50 (IK, a) , 6.69 (1 x 3/4H, Si, 6.73 (1 x 1/4H, s), 6.94-7.20 (3K, a) , 7.32 (1 x 3/4H, s) , 7.36 (1 κ 1/4H, s), 7.40 (IH, ε;, 7.48-7.61 (2H, mj , 7.62- 7.90 (3H, a) , 7.99 (IH, s), 3.C9 (IH, a, J=3Hz) , 3.53-8.70 (IH, a) , 8."5 (IH, s. (14) MASS : 567 (M+l) NMR (CDCI3, δ) : 0.70 (3 κ 1/4H, t, J=8Hz), C.78 (3 x 3/4H, t, J=8Hz), 1.00-1.40 (4H, a) , 1.57-1.85 (2H, a) , 3.01 (3 κ 1/4H, ε), 3.11 (3 κ 3/4K, s) , 3.03- 3.33 (2H, a), 4.65-4.97 (3H, a), 4.98-5.10 (IH, a) , 6.81 (IK, s), 7.18-7.30 (2H, ai , 7.4C (IK, t, J=8Hz) , 7.42-7.90 !όK, a), S.ϋi (IH, s), 9.13 (2H d, J=8Hz), 5.2-3.40 (IH, a), S.3C ■ * 1 κ 3/4H, ε), 8.67 :l x 1/4H, s; (15) MASS : 530 (M+l) NMR (CDC1 3 , δ) : 2.70 (3 κ 4/5H, s), 2.68 (3 κ 1/5H, s), 3.00-3.20 (2H.. a) , 3.86 (3H, si, 3.91-4.03 (2H, a), 4.16 (2 x 1/lOH, d, J=16Hz), 4.30 (2 x I/IOH, d, J=16Hz), 4.4" (2 x 4/5H, ε) , 4.61 (IH, br s), 5.30 (1 x 4/5H, q, J=3H∑), 5.39 (1 x 1/5H, q, J=8Hz), 5.59 (IH, q, J=8Hz), 6.49 (1 κ 4/5H, a, J=8Hz), 6.61 (1 x 1/5H, d, J=8Hz) , 6.97-7.41 (1CH, a), 7.48 (IH, d, J=8Hz) , 7.63 (1 x 1/5H, d, J=8Hz) , 7.86 (1 x 4/5H, a, J=2Kz) , 7.90 (iH, a, J=2Hz) , 9.01 (1 x 1/5H, d, J=3Hz) , 9.05 (1 κ 4/5H, d, J=8Hz) (16) MASS : 531 (M+l) NMR (CDCI3, δ) : 2.68 (3 κ 3/4H, s), 2.81 (3 κ 1/4H, s), 2.92-3.17 (2H, a), 3.69-3.50 (IH, a), 3.90 (3H, s), 4.00 (2 x 1/8H, a, J=16Hz), 4.03-4.18 (IH, m) , 4.30 (2 x 3/8H, d, J=15Hz), 4.41 (2 κ 1/SH, a, J=16Hz), 4.52 (2 x 3/8K, d, J=15Hz) , 4.73-4.88 (IH, a), 5.12 (1 x 3/4H, q, J=8Hz), 5.23 (1 x 1/4H, q, J=8Hz), 6.69 (1 x 3/4H, d, J=8Hz), 5.70 (1 x 1/4H, d, J=8Hz), 7.00-7.21 (6H, a), 7.28 'IH, t, J=SHz), 7.32-7.43 (2K, a), 7.48-7.72 ( 4n, a) , 7.92 (1 x 1/4H, d, (17) MASS : 531 (M+l) NMR (CDCI T , δ) : 2.49 (3H, s) , 2.62 ( 3 x 3/4H, s) , 2.74 (3 x 1/4H, s) , 2.92-3.15 (2H, a), 3.73-3.88 (IH, a), 3.97 (2 x 1/8H, d, J=16Hz) , 4.01-4.18 (IH, a), 4.36 (2 x 3/8H, d, J=15Hz) , 4.48 (2 x 1/8K, d, J=16Hz), 4.49 (2 κ 3/8H, a, J=I5Hz) , 4.70-4.97 (2H, 16981 - 674 - a), 5.11 (1 κ 3/4H, c, J=8H∑i , 3.21 1 x 1/4H, q, J=8Hz) , 6.95-7.20 (6H, m; , " .20- • .42 ( 3H, a ', , 7.49 (1 x 3/4H, s), 7.51 (1 x 1/4H, s,, " . " 0-7.87 (3K, a) , 7.91 (1 x 3/4H, a, J=8Hz.. , A95 (1 x 1/4H, a, J=8H∑), 8.27 (IH, s) (18) MASS : 671 (M+l) NMR (CDC1 3 , δ) : 1.33 (3H, t, J=8Hz) , 2.30 (3H, ≤), 2.32-2.51 (4H, a), 2.52-2.7C (IH, mi , 2.53 (3 κ 3/4H, s), 2.73 (3 κ 1/4H, s ; , 2.93-2.13 '2H, a), 3.32 (IH, dd, J=17, 2Hzi , 3.40-3.59 (2H, a> , 3.60- 3.75 (2H, a) , 3.93 (2 x 1/8H, d, J=16Hz; , 4.15 (2 3/8H, d, J=15Hz), 4.26 (2 κ 1/8H, a, J=lόHz( , 4.31 (2H, q, J=8Hz), 4.51 (2 x 3/8H, d, J=15Hzi , 4,93- 5.20 (2H, a), 6.60 (1 x 1/4H, a, J=SHz>, 6.62 (1 κ 3/4H, d, J=8Hz) , 7.CC-7.22 (5H, a,, 7.29 (IH, άd, J=12, 2Hz), 7.32-7.45 (2H, a), 7.63-7.96 (5H, a), 8.14 (IH, d, J=8Hz) (19) MASS : 610 (M+l) NMR (CDCI3, δ) : 2.10 (3H, s), 2.55-2.5C (IH, a) , 2.68 (3 x 3/4H, s) , 2.82 (3 x 1/4H, si, 2.88-3.08 (2K, a), 3.09-3.21 (IH, a), 3.22-3.41 (2H, a), 3.42-3.70 (6H, a), 4.23 (2 x 3/8H, a, J=15Hz) , 4.3C (2 x 1/8H, a, J=16Hz) , 4.39 (2 κ I/8K, a, J=16Hz), 4.73 (2 κ 3/8H, d, J=15Hz) , 5.10-5.22 (IH, a), 5.23-5.4C (IH, a), 6.73-7.13 (9H, a) , 7.14-7.3C (3K, a), 7.41 (IH, d, J=8Hz), 7.61 (IH, d, J=8Hz), 8.00 (1 x 1/3K, d, J=8Hz), 8.07 (1 x 2/3H, a, J=8Hz) , 8.2C " κ 1/3H, d, (20) MASS : 611 (M+l) NMR (CDCI3, δ) : 2.22 (3K, s) , 2.53-2 A3 (IK, a) , 2.62 (3 κ 3/4H, s), 2.80 (3 x 1/4H, s) , 2.90-3.10 (2H, ra), 3.20-3.37 (IH, a), 3.33-3.58 (2H, a), 3.58-3.8 (6H, a) , 4.22 (2 κ l/8K, " d, =I6Hz. , 4.30 '2 x 3/8K, a, =15Hz), 4.39 (2 x 1/8K, a, J=I6Hz;, 4.63 (2 κ 3/8H, d, J=I5Hz), 5.02-5.20 (2H, a), 6.37-7.13 (6H, m) , 7.18-7.35 (4H, a), 7.42 (IH, t, =8Hz), 7.51 (IH, s), 7.57 (IK, d, =8Hz), 7 . 60 -7.72 (2H, a) , 8.21 (IH, a, J=8Hz) (21) MASS : 549 (M+l) NMR (CDC1 3 , δ) : 0.83 (3 x 1/3H, t, J=8Hz) , 0.92 (3 κ 2/3K, t, J=8Hz), 1.2C-1.5I (2H, a), 1.57-1.81 (2K, a), 2.58-2.72 (IK, m; , 2.83 (3 x 1/3H, ε), 2.94 (3 x 2/3H, s), 3.30 (IH, a, =I6Hz), 3.38-3.57 (2K, a), 3.58-3.80 (6H, a), 4.39 (2 x 1/3H, d, J=15Hz) , 4.60 (2 κ 1/3H, ε), 4.73 (2 κ 1/3H, d, J=15Hz) , 4.82-5.01 (IH, a), 5.06-5.20 (IH, m) , 7.10-7.47 (7H, m) , 7.48-7.60 (2H, a), 7.68 (2 x 2/3H, d, J=8Hz), 7.71 (2 x 1/3H, d, J=8Hz) , 8.27 (IH, d, J=8Hz) (22) MASS : 548 (M+l) NMR (CDCI3, δ) : 0.73 (3 x 1/3H, t, J=8Hz) , 0.81 (3 κ 2/3H, t, J=8Hz), 1.20-1.50 (2K, m) , 1.50-1.78 (2H, a), 2.60-2.73 (IH, a), 2.85 (3 κ 1/3H, s), 2.89 (3 κ 2/3H, s), 3.19 (IH, d, J=15Hz) , 3.26-3.40 (2H, a), 3.41-3.68 (6H, a), 4.21 (2 κ 1/3H, d, J=15Hz), 4.52 (2 x 1/6H, d, J=16Hz) , 4.61 (2 x 1/6H, d, J=16Kz), 4.80 (2 κ 1/3H, d, J=15Hz), 4.90-5.02 (IH, m) , 5.20-5.33 (IH, m) .. 6.84 (1 x 1/3H, s), 7.C1 (1 x 2/3H, s), 7.03-7.39 (7H, a), 7.43 (IH, a, J=8Hz) , 7.62 (IH, a, J=8Hz), 7.98-8.20 (2H, a ,! ) (23) MASS : 673 (M+l) NMR (CDCI3, δ) : 2.27 (3H, s), 2.32-2.4 7 (4 > r _ f 2 . S2 (3H, s), 2.58 (3 x 3/4H, s), 2.58-2.70 (IH, a). 2.73 (3 x 1/4H, s) , 2.92-3.13 (2H, 3.23-3.40 (IH, ~.) , 3.40-2.60 -2H, a), 3.60-3.50 (2H, ai , 4.01 (2 x 1/3H, a, J=I6Hz) , 4.21 3, -, a, —_DHz) , 4.3C :2 x 1/SH, d, J=16Hz) , 4.51 i2 x 2/8K, a, J=15Hzi , 4.98-5.18 (2H, a; , 6.98-7.23 '7H, a; , 7.32-7.5C (2H, a) , X 6 (IH, a, =έHs) , 7.79-7.93 (3H, a) , 8.09-3.19 (IH, a; , 8.21 -IH, s) (24) MASS : 514 (M+l) NMR (CDCI 3 , δ) : 0.8C (3 x 1/5H, t, , 0.83 (3 κ 4/5H, t, J=8Hz), 1.15-1.43 (4H, a; , 1.60-1.88 (2H, a), 2.68 (IH, dd, J-=I7, 7Hz), 2.95 (3 κ 1/5H, s), 3.09 (3 x 4/5H, S), 3.29 UK, dd, =17, 2Kz) , 3.38- 3.56 (2H, m) , 3.57-3.30 (6H, a), 4.cl (2 x I/2H, d, J=15Hz), 4.89 (2 x I/2H, d, J=15Hz, , 4.78-5.C3 (IH, m) , 5.04-5.20 (IH, m) , 7.21-7.33 (IH, m) , 7.41 (IK, t, J=8H∑), 7.48-7.60 (3H, a), 7.61-7.73 (2H, a), 7.74-7.39 (2K, a) , 8.01 (IH, s), 3.02-3.16 (IH, a), 8.28 (IH, d, J=8Hz;, 8.78 '1 x 4/5K, ε), 6.84 (1 x 1/5K, s) (25) MASS : 613 (M+l) NMR (CDCI3, δ) : 0.71 (3 x 1/5H, t, J=8Hz), 0.78 (3 x 4/5H, t, J=8Hz), 1.03-1.40 (4K, a) , 1.53-1.82 (2H, a), 2.68 (IH, dd, J=17, 7Hz) , 2.90 (3 x 1/5H, s), 2.93 (3 κ 4/5H, s), 3.23 (IH, a, J=I5Hz) , 3.30-3.48 (2K, a) , 3.48-3.71 (6H, mi , 4.51 (2 x 1/2H, d, J=15Kz), 4.81 (2 x 1/2H, a, J=15Hz, , 4.70-5.C4 (IH, ai , 3.15-5.30 (IH, a) , 6.99 (IH, ≤ ' , .Q9 (IH, t, J=8Kzi, 7.16-7.30 (IH, a), 7.39-7.57 (2H, a) , 7.58- 7.85 (3H, a), 7.92 (IH, s) , 7.98 (IH, d, J=3Hz), 8.10 (2H, t, J=8Hz), 8.73 (I x 4/5H, s,, 8.81 (1 x 1/5H, s) (26) MASS : 685 (M+l) NMR (CDCI3, c) : 0.91 (3H, t, J=8Hz), 1.63-1.82 (2H, m) , 2.28 (3H, ε 2.32-2.53 (4H, a .. 2.56-2.70 (IH, a), 2.58 (3 x 2/3H, s), 2.73 (3 κ 1/3H, ε), 2.93- 3.13 (2H, ) , 3.33 (IH, dd, J=15, 2Hz;, 3.41-3.60 (2H, m) , 3.61-3.71 (2H, a), 3. 2-3. 1 '2H, a), 3.33 (2 κ 1/6H, d, J=16Hz), 3.99 (2 κ 1/3H, a, J=15Kz), 4.10 (2 κ I/6K, d, J=16Hz), 4.31 (2 x 1/3H, d, J=15Hz), 4.93-5.12 (2K, a), 6.66 (1 x 1/3H, da, 2Hz) , 7.06 (IH, da, J=1C, 2Hz), 7.10-7.30 ;6H, a, , 7.37-7.49 (2K, a), 7.70 (1 x 2/3H, a, J=5Hz) , 7. 78 :1 x / 3H/ d, J=8Kz), 7.8C-7.90 (3H, a), 6.11 (1 x 1/3H, d, J=8Hz), 8.13 (1 x 2/3H, d, J=6H∑) (27) MASS : 628 (M+l) NMR (CDCI3, δ ) : 2.59 (3 x 3/4H, si , 2.65 (IK, dd, J=16, 8Hz), 2.72 (3 x 1/4K, s.' , 2.96-3.13 (2H, a), 3.30 (IH, dd, J=15, 2Kz) , 3.40-3.53 (2H, a;, 3.60- 3.30 (6H, a), 3.88 (3H, s) , 4.20 (2 x 1/3H, d, J=16Hz), 4.21 (2 x 3/8K, a, J=15Hz, , 4.29 (2 x 1/8H, d, J=16Hz), 4.51 (2 x 3/8H, a, J=15Hz) , 5.01- 5.22 (2H, a), 6.64 (1 x 1/4H, d, J=6Hz) , 6.68 (1 x 3/4H, d, =8Hz), 7.07-7.37 (7H, a) , 7.42 (IH, t, J=8Hz), 7.50 (IH, s), 7.57 (IH, d, J=8Hz), 7.68 (IH, d, J=8Hz), 7.70 (IK, a, =8Hz), 7.34 (1 x 1/4H, d, J=2Hz), 7.93 (1 x 3/4H, d, J=2Hz) , 6.21 (IH, d, J=8Hz) (28) MASS : 627 (M+l) NMR (CDCI3, δ) : 2.53 ;3 x 3/4H, s; , 2.61-2.78 (IH, m) , 2.73 (3 x 1/4H, sj, 2.90-3.1C (2H, a-, 2.18 (IH, d, J=16Hz), 3.26-3.43 (2H, a), 3.44-3.68 (6H, a), 3.87 (3H, s), 3.94 (2 x 1/8K, a, J=16Hz,., 4.13 (2 x 3/8H, a, J=15Hz), 4.24 (2 x 1/8K, a, J=16Kz) , 4.52 (2 x 3/8H, d, J=I5Hz) , 5.02-5.18 (IH, a) , 5.19-5.30 (IH, a), 6.60 (IH, a, J=8Hzi , 6.93-7.48 (9H, mi , 7.43 (IH, a, J=8Hz), " .63 • IH, d, J=8Hz) , 7.81 (1 x 1/4H, s) , 7.91 ιl x 3/4H, s) , 3.01-8.22 (2H, a) (29) MASS (a/z'' : 597 (M-t-H) ~ NMR (CDCI 3 , δ) : 2.51-2.67 (IH, a), 2.63 (3H κ 2/3, si, 2.82 (3H x 1/3, s " , 2.97-2.07 ,2H, ai , 3.23- 3.33 (IH, a), 3.40-3.59 (2H, m, , 2.60-3.80 (6H, a), 4.15 (IH x 1/3, d, J=ic.5H∑), 4.31 (IH x 2/3, d, J=16.5Hz), 4.4C (IH x 1/2, d, =16.5Hzi , 4.63 (IH κ 2/3, d, J=16.5Hz), 5.01-5.16 '2H, a; , 6.64 (IH, a, J=2.5Hz), 6.93-7.21 (7K, a) , 7.23-".33 (3H, a) , 7.54 (IH, d, J=7.5Kz,, 7.63-7.33 (3K, a), 3.C5-8.15 (2H, m) (30) MASS (a/z) : 623 (M+H) ~ NMR (CDCI3, δ) : 2.54-2.70 (IH, a), 2.62 (3H x 2/3, s), 2.82 (3H x 1/3, s,, 2.99-3.12 (2H, a, , 3.25 (IH κ 1/3, dd, J=16.0, 3.0Hz), 3.29 (IH κ 2/3, dd, J=16.0, 3.0Hz), 3.41-3.57 (2H, a), 3.61-3.77 (6K, a) , 4.17 (IH κ 1/3, d, J=15.0K∑), 4.31 (IH x 2/3, d, J=15.0H∑), 4.39 (IH x. 1/3, a, J=13.0H∑i, 4.64 (IH x 2/3, d, J=15.0H∑), 4.99-5.18 (2H, a) , 6.77 (IH, d, J=2.5H∑), 6.97-7.30 (IIH, a) , 7.36 (IH, d, J=7.5Hz), 7.44 (2H, t, J=7.5Hz), 7.60-7.73 (IH, a) , 7A5 (2H, t, J=7.5Hzi , 3.01 (IH, d, J=7.5Hz) (31) MASS (a/z) : 59 7 ( TH) " NMR (CDCI3, δ) : 2.42-2.50 (IH, a) , 2.63 (3H x 2/3, s), 2.82 (3H x 1/3, si , 2.98-3.77 (13H, a) , 4.06- 4.69 (3H, a), 4.83-5.15 (2H, m, , 6.75-7.02 (2H, a) , 7.06-7.33 (IIH, a) , 7. 1-7. 4 (2H, a), 8.C7 (IH x 1/3, d, J=8.5Hz), 8.32 (IH x 2/3, a, J=3.5Hz) , 9.23 (IH, br s) Example 42 The following object compounds were obtained according to a similar manner to that of Example 1. (1) MASS : 641 (M+l) NMR (CDC1 3 , δ) : 0.83 (3 x 1/4H, t, J=8Hz) , 0.87 (3 x 3/4H, t, J=8Hz), 1.17-1.43 (4H, m) , 1.58-1.84 (2H, m) , 2.69 (IH, dd, J=16, 7Hz) , 2.91 (3 x 1/4H, s), 3.02 (3 x 3/4H, s) , 3.30 (IH, dd, J=16, 2Hz) , 3.38- 3.58 (2H, m) , 3.58-3.78 (6H, m) , 4.51 (2 x 3/8H, d, J=15Hz), 4.62 (2 x 1/8H, d, J=16Hz) , 4.70 (2 x 3/8H, d, J=15Hz), 4.78 (2 x 1/8H, d, J=16Hz) , 4.82- 5.00 (IH, m) , 5.08-5.20 (IH, m) , 7.21-7.33 (IH, m) , 7.34-7.48 (2H, m) , 7.49 (IH, s) , 7.55 (IH, d, J=8Hz), 7.60-7.83 (4H, m) , 8.18-8.38 (2H, m) , 8.58 (1 x 3/4H, s), 8.61 (1 x 1/4H, s) , 8.68 (IH, br s), 9.21 (IH, br s) (2) MASS : 640 (M+l) NMR (CDCI3, δ) : 0.78 (3 x 1/4H, t, J=8Hz) , 0.80 (3 x 3/4H, t, J=8Hz), 1.08-1.40 (4H, m) , 1.51-1.81 (2H, m) , 2.69 (IH, dd, J=16, 4Hz), 2.89 (3 x 1/4H, s) , 2.93 (3 x 3/4H, s) , 3.30 (IH, dd, J=16, 2Hz) , 3.31- 3.50 (2H, m) , 3.50-3.72 (6H, m) , 4.40 (2 x 3/8H, d, J=15Hz), 4.61 (2 x 1/8H, d, J=16Hz) , 4.66 (2 x 3/8H, d, J=15Hz), 4.69 (2 x 1/8H, d, J=16Hz) , 4.81- 5.01 (IH, ), 5.18-5.30 (IH, m) , 6.99 (IH, s), 7.10 (IH, t, J=8Hz) , 7.22 (IH, t, J=8Hz) , 7.30-7.49 (2H, m) , 7.56-7.80 (3H, m) , 7.96 (IH, d, J=8Hz) , 8.11 (IH, d, J=8Hz), 8.28 (1 x 3/4H, s), 8.30 (1 x 1/4H, s), 8.51 (1 x 3/4H, s) , 8.59 (1 x 1/4H, s) , 8.63 (IH, s), 9.19 (IH, s) (3) MASS : 605 (M+l) NMR (CDCI3, δ) : 0.79 (3 x 1/4H, t, J=8Hz) , 0.80 (3 x - 680 - Ξ/4H, I=3Hz ' 1. C3-1.40 -i ' -; rc.i 4 " - • .7 £ !2H, a) , 2.90 (3 x 1/4K, s' , 3. CO ,3 x 3/4H, si , 3.31 (1 x 1/4H, d, J=6Hz) , 3.39 (1 x 3/4H, a, J=6Hz' , 3.43 (1 κ 1/4H, d, J=4Hzi , 3.5C (I κ 3/4.-I, d, J=4Hz) , 4.51 (2 κ 3/8H, d, J=15Hz), 4.63 (2 x 1/8H, a, =16Hz), 4.63 (2 κ 1/8H, d, =16HA , 4. 7 2 (2 κ 2/8K, a, J=15Hz), 4.81-5. CO (IH, ai , 5.03-5.17 (IH, a), 7.19 (IH, t, J=8Hz), 7.22-7.33 (2H, mi , 7.33- 7.43 (2H, a) , 7.48 (IK, Si , 7.51 (1 x 3/4H, s) , ϋ 7.55 .1 κ 1/4H, s) , 7.58-7.81 (4H, a) , 3.11 (IH, d, J=8Hz) , 8.28 (1 κ 3/4H, d, J=8Hz), 8.31 (1 x 1/4H, d, J=8Hz) , 3.50-8.70 (3H, mi , 3.73 (1 x 1/4K, a, J=8Hz) , 8.80 (1 x 3/4H, d, J=SHzi , 9.13 (1 x 3/4H, s) , 9.21 (1 κ 1/4K, s) 5 (4) MASS : 604 (M+l) NMR (CDC1 3 , δ) : 0.70 (2 x 1/5H, t, J=8H∑), 0.72 (3 x 4/5H, t, J=8H∑), C.97-1.30 I4 ' ή, a; , 1.38-1.53 (IH, m) , 1.54-1.70 (IH, m) , 2.90 (3 κ A5K, si, 2.97 (3 0 x 4/5H, s), 3.30-3.50 (2H, mi , 4.53 (2 x 4/5H, s) , 4.61 (2 κ 1/5H, s) , 4.39 (1 κ 4/5H, q, J=8H∑), 4.95 (1 κ 1/5H, q, J=8H∑) , 5.22 (1 κ 4/5H, q, J=3H∑), 5.31 (1 x 1/5H, q, J=3Hz), 7.00-7.74 (IIH, a) , 8.09 (1 x 4/5H, a, J=8Hz), 8.3C (1 x 1/5H, d, =8Hz) , 5 8.25 (1 κ 4/5H, d, J=8Hz), 3.36 (1 x 1/5H, d, J=8Hz), 8.47-8.60 (2H, a), 3.62 (IH, ,d, J=2Hz) , 8.71 (IH, a, J=2Hz) , 9.13 (1 κ 4/5H, s< , 9.19 (I κ 1/5H, s) 0 (5) MASS : 588 (M+l) NMR (CDCI- 5 , δ) : 0.78 (3 κ 1/5H, t, J=8Hz) , 0.81 (3 κ 4/5H, t, J=8Hz) , 1.2C-1.43 (4H, a), 1.37-1.90 (2H, a), 2.08 (3K, s), 2.13-2.2" (2h\ a) , 2.64 (2H, t, J=8Hz) , 3.00 (3 κ 1/5H, s), 3.04 (3 κ 4/5H, s) , 5 4.60-4.82 (2H, a), 4.92-5.07 (2H, a) , 7.2C-7.84 ( 10H, mi , 3 . 32 ( IH, d, =3Hz ) , 3 . 62 ( IK, ≤ . 5 . 63- (6) MASS : 567 (M+li NMR (CDCI 3 , δ) : 0.61 (3 κ 1/5H, t, , 0.65 (3 κ 4/5H, t, J=9Hz), 1.03-1.40 (4H, a), 1.56-1.90 (2H, a) , 2.02 (3H, s), 2.14-2.40 (2H, a 1 , 2.63 (2H, t, J=8H∑), 3.14 (3 x 1/5H, s), 3.17 (3 x 4/5H, ≤), 4.64-4.96 (2H, a), 5.18 (IH, q, J=8Hz), 5.52 (IH, q, J=8Hz), 7.00-7.50 (7K, a), 7.64 V 1H, d, J=8Kz), 7.68-7.85 (2H, a), 8.34 (IH, a, J=6Hz), 8.64 (IH, S), 5.32 (1 x 4/5K, d, =3Hz), 8.9" (1 x 1/5H, a, J=8Hz), 9.22 (IK, ≤, (7) MASS (m/z) : 578 (M + AL; NMR (CDCI3, δ) : 0.81 (3H, t, J=7Kz), 1.26 (4H, m) , 1.63 (2H, m) , 2.50 (3H, s), 2.57-2.65 (IH, a), 2.81 (3H x 1/4, s), 2.93 (3H x 3/4, s) , 3.22-3.27 (IH, a) , 3.42 (2H, a), 3.60 (6H, a), 4.32 (IH κ 3/4, a, J=15Hz), 4.50 (IH κ 1/4, a, J=16Kz), 4.61 (IH κ 1/4, d, J=16Hz), 4.63 (IH κ 3/4, d, J=I5Hz), 4.83 (IK, a), 5.06 (IH, a), 7.05-7.26 (2H, a), 7.35-7.51 (4H, a), 7.61-7.69 (2K, a) , 3.20 (IH, a) , 8.29-8.34 (IH, a) (8) MASS (a/z) : 577 (M + +D NMR (CDC1 3 , δ) : 0.77 (3H, t, J=7Hz), 1.27 (4K, a), 1.64 (2H, a), 2.51 (3H, si, 2.6 * - (IH, a) , 2.52 (3H x 1/4, s), 2.90 (3H κ 3/4, s) , 3.22-3.28 (IH, a) , 3.37 (2H, a), 3.58 ( 6r., a), 4.27 (IH x 3/4, a, J=15Hz), 4.53 (2H κ 1/4, s), 4.62 (IH κ 3/4, d, J=15Hz), 4.86 (IH, a 1 , 5.18 (IH, a), 6.98 (IH, a), 7.04-7.13 (2H, a), 7.25 (IH, a), 7.40-7.45 (2H, a), 7.62 (IH, m) , 7.90 (IH, m) , 8.10 (IH, m) , 8.30-8.37 (IH, m) (9) MASS (m/z; : 542 (M τ -1) NMR (CDCi 3 , δ) : 0.75 (3H, z, J= " H:; , 1.11 !4H, a) , 1.43 (IH, m) , 1.60 (IH, m) , 2.45 (3H, si , 2.8C (3K x 1/3, s), 2.92 (3K x 2/3, si, 3.25-3.46 (2H, m) , 4.31 (IH x 2/3, d, J=15Hz) , 4.54 (IH x 1/3, s) , 4.62 (IH x 2/3, d, J=15Hz), 4.83 (IH, mi , 5.07 (IH, a) , 7.03-7.27 (4H, mi, 7.37-7.62 (6H, a, , 3.06 (IH, m) , 8.29 (IH, a), 3.53 (IH, a, , 5. " 2 (IH, a) (10) MASS (a/z) : 541 (M + A; NMR (CDC1 3 , δ) : 0.74 (3K, t, J=7Hz, , 1.09 (4H, a), 1.42 (IH, a) , 1.60 (IH, a) , 2.53 (3K, s , 2.92 (3K, s), 3.38 (2H, a) , 4.49 (2K, si, 4.37 , ; 1 / - ι . 5> 19 (IH, a), 7.08-7.37 ( H, a), 7.39-". 3 '3H, a), 7.65 (IH, a) , 7.97 (IH, a) , 3.32 (IH, a) , 8.52 (IH, m) , 8.65 (IH, a) (11) MASS (a/z) : 525 (M + A) NMR (CDCI3, δ) : 0.80 (3H, t, J=7Hz) , 1.29 (4H, a) , 1.62 (IH, a) , 1.72 (IH, a), 2.10 (3H, s), 2.14-2.20 (2H, a), 2.52 (3H, s, , 2.60 (2H, a) .. 2.91 (3K x 1/4, s), 3.01 (3H κ 3/4, s) , 4.4 7 (IH κ 3/4, d, J=15Hz), 4.56 (IH κ 1/4, d, J=16Hz), 4.65 (IH κ 3/4, d, J=15Hz), 4.66 (IH x 1/4, a, J=16Hz) , 4.93 (2H, m) , 7.11 (IH, a) , 7.21-7.47 (7H, a), 7.63-7.65 (IH, a) , 8.35-8.40 (IK, a) (12) MASS (a/z) : 524 (M + Ai NMR (CDCi 3 , δ! : 0.66 (3H, t, J= 7 Hz) , 1.22 (4H, a), 1.63 (IH, a), 1.74 (IH, a) , 2.05 (3H, si , 2.17 ( 2H, a) , 2.55 (3K, s), 2.62 (2K, a), 3.1C (3H, ~ , 4.64 (IK, d, J=15Hz), 4.83 (IH, d, J=15Hz) , 5.13 (IK, a) , 5.50 (IH, a), 7.02-7.33 (6H, a) , 7.45-7.64 (2H, a) , 8.43 (IH, a) , 3.79 (IH, a) (13) MASS (m/z): 481 (M + +l) NMR (CDC1 3 , δ) : 0.83 (3H, t, J=7Hz), 1.33 (4H, m) , 1.72 (2H, m) , 2.49 (3H x 5/6, s), 2.55 (3H x 1/6, s), 2.89 (3H x 1/4, s) , 3.03 (3H x 3/4, s), 3.77 (IH, m), 4.09 (IH, m) , 4.54 (2H, a) , 4.95 (3H, a), 7.04-7.49 (5H, a), 7.61-7.77 (3H, a), 8.30-8.42 (IH, a) (14) MASS (m/z): 480 (M + +l) NMR (CDCI3, δ) : 0.81 (3H, t, J=7Hz) , 1.31 (4H, m) , 1.73 (IH, m) , 1.93 (IH, m) , 2.38 (3H, s), 3.03 (3H x 1/6, s), 3.15 (3H x 5/6, s), 3.97 (2H, m) , 4.38 (IH, d, J=15Hz), 4.87 (IH, d, J=15Hz) , 5.08 (IH, m) , 5.62 (IH, m) , 6.72 (IH, ) , 6.95 (IH, m) , 7.07- 7.36 (6H, m), 7.61 (IH, m) , 8.27 (IH x 5/6, m) , 8.38 (IH x 1/6, ) , 9.09 (IH, m) (15) MASS (m/z) : 641 (M + +l) NMR (CDCI3, δ) : 2.30 (3H, s), 2.33-2.58 (4H, m) , 2.60 (3 x 3/4H, s) , 2.68 (IH, dd, J=17 and 8Hz) , 2.79 (3 x 1/4H, s) , 2.98-3.12 (2H, a) , 3.23-3.40 (IH, a), 3.40-3.60 (2H, a), 3.62-3.75 (2H, m) , 3.82 (3H, s), 3.90 (2 x 1/8H, d, J=16Hz) , 4.38 (2 x 1/8H, d, J=16Hz), 4.41 (2 x 3/8H, d, J=15Hz) , 4.49 (2 x 3/8H, d, J=15Hz) , 5.01-5.20 (2H, m) , 7.07 (IH, s), 7.11-7.38 (6H, m) , 7.43 (IH, t, j=8Hz) , 7.50 (IH, s), 7.58 (IH, d, J=8Hz), 7.69 (IH, d, J=8Hz) , 7.80 (1 x 3/4H, d, J=8Hz) , 7.84 (1 x 1/4H, d, J=8Hz), 7.90 (1 x 1/4H, s) , 8.00 (1 x 3/4H, s), 8.13-8.30 (2H, m) (16) MASS (m/z) : 640 (M + +l) NMR (CDCI3, δ) : 2.21 (3H, s) , 2.27-2.40 (4H, m) , 2.56 (3 x 3/4H, s), 2.69 (IH, dd, J=17 and 6Hz) , 2.73 (3 x 1/4H, s), 2.92-3.10 (2H, m) , 3.11-3.27 (IH, a), 3.30-3.48 (2H, m) , 3.50-3.70 (2H, m) , 3.72 (3 x 3/4H, s), 3.78 (3 x 1/4H, s) , 3.93 (2 x 1/8H, d, J=16Hz), 4.30 (2 x 1/8H, d, J=16Hz) , 4.31 (2 x 3/8H, d, J=15Hz), 4.47 (2 x 3/8H, d, J=15Hz) , 5.08 (IH, q, J=8Hz) , 5.17-5.26 (IH, m) , 6.90-7.20 (8H, m) , 7.21 (IH, d, J=8Hz), 7.42 (IH, d, J=8Hz) , 7.62 (IH, d, J=8Hz), 7.87 (1 x 1/4H, s) , 7.97 (1 x 3/4H, s), 8.02-8.17 (2H, a), 8.20 (IH, s) (17) NMR (CDC1 3 , δ) : 2.29 (3H, s) , 2.32-2.55 (4H, a), 2.62-2.74 (IH, a), 2.68 (3 x 2/3H, s), 2.70 (3 x 1/3H, s), 2.98-3.18 (2H, a), 3.27-3.42 (IH, a), 3.43-3.60 (2H, a), 3.61-3.72 (2H, a), 3.82 (3H, s), 3.56 (2 x 1/6H, d, J=16Hz) , 4.33 (2 x 1/3H, d, J=15Hz), 4.38 (2 x 1/6H, d, J=16Hz) , 4.60 (2 x 1/3H, d, J=15Hz) , 5.04-5.14 (IH, m) , 5.10 (1 x 2/3H, q, J=8Hz), 5.39 (1 x 1/3H, q, J=8Hz) , 6.72 (IH, d, J=7Hz), 7.10-7.32 (6H, a), 7.41 (IH, t, J=8Hz) , 7.49 (IH, s) , 7.53-7.82 (3H, m) , 8.03 (1 x 1/3H, s), 8.20 (1 x 2/3H, s) , 8.18-8.30 (IH, a), 8.41 (IH, dd, J=7, 2Hz) (18) NMR (CDCI3, δ) : 2.22 (3H, s) , 2.29-2.48 (4H, m) , 2.61-2.80 (IH, m) , 2.69 (3 x 2/3H, s), 2.71 (3 x 1/3H, s), 2.90-3.12 (2H, m) , 3.13-3.33 (IH, m) , 3.35-3.50 (2H, m) , 3.51-3.71 (2H, a), 3.73 (3 x 1/3H, s), 3.76 (3 x 2/3H, s) , 3.70 (2 x 1/6H, d, J=16Hz), 4.37 (2 x 1/6H, d, J=16Hz) , 4.42 (2 x 1/3H, d, J=15Hz), 4.52 (2 x 1/3H, d, J=15Hz) , 5.08- 5.25 (IH, m) , 5.18 (1 x 2/3H, q, J=8Hz) , 5.41 (1 x 1/3H, q, J=8Hz), 6.65-6.78 (IH, m) , 6.99 (IH, s) , 7.00-7.20 (5H, m) , 7.21 (IH, d, J=8Hz) , 7.27 (IH, s), 7.42 (IH, d, J=8Hz), 7.62 (IH, d, J=8Hz) , 7.91- 8.09 (2H, m) , 8.10 (1 x 1/3H, s) , 8.20 (1 x 2/3H, s ) , 8 . 37-8 . 50 ( IH, m) ( 19) MASS : 705 (M+l ) NMR (CDC1 3 , δ) : 2.28 (3H, s) , 2.32-2.52 (4H, m) , 2.58-2.72 (IH, m) , 2.60 (3 x 3/4H, s) , 2.77 (3 x 1/4H, s), 2.96-3.12 (2H, a), 3.31 (IH, dd, J=16, 2Hz), 3.40-3.60 (2H, m) , 3.61-3.80 (2H, m) , 4.02 (2 x 1/8H, d, J=16Hz), 4.30 (2 x 3/8H, d, J=15Hz) , 4.33 (2 x 3/8H, d, J=15Hz) , 4.54 (2 x 1/8H, d, J=16Hz), 4.97-5.11 (2H, m) , 7.10-7.23 (5H, m) , 7.35-7.49 (2H, m) , 7.51 (1 x 1/4H, s) , 7.68 (1 x 3/4H, s), 7.78-7.90 (4H, m) , 8.11 (1 x 3/4H, d, J=8Hz), 8.18 (1 x 1/4H, d, J=8Hz) , 8.30 (IH, s) , 8.59 (IH, s) Example 43 A aixture of Starting Coapound (209 ag) and O-aethyl benzo[b] furan-2-carbothioate (104 ag) in methanol (2.5 ml) was stirred at room temperature for 3 hours. The solvent was evaporated, and the residue was purified by column chromatography (silica gel, chloroform/methanol = 70/1) to give Object Compound (121 mg) as yellow powder. MASS (m/z) : 578 (M+H) + NMR (CDCI3, δ) : 2.63 (4/5 x 3H, s) , 2.77 (1/5 x 3H, s), 2.85-3.08 (2H, m) , 3.25-3.42 (IH, m) , 3.50-3.66 (IH, m) , 4.23 (1/5 x 2H, ABq, Δ=0.20, J=17Hz) , 4.45 (4/5 x 2H, ABq, J=15Hz) , 5.05-5.21 (IH, m) , 5.41-5.58 (IH, m) , 7.05-7.80 (16H, m) , 8.23-8.82 (4H, m) Example 44 The following compounds were obtained according to a similar manner to that of Example 1. (1) MASS (m/z): 559 (M+H) + NMR (CDCI3, δ) : 1.60-2.05 (2H, a), 1.88 (1/4 κ 3H, s), 1.94 (3/4 x 3H, s), 2.12-2.40 (2H, a) , 2.54 (1/4 x 3H, s), 2.58 (3/4 x 3H, s) , 2.87 (1/4 x 3H, s), 2.99 (3/4 x 3H, s) , 3.25-3.52 (2H, a) , 4.52 (3/4 x 2H, ABq, Δ=0.26, J=15Hz) , 4.60 (1/4 x 2H, ABq, Δ=0.08, J=17Hz), 4.96-5.24 (2H, a) , 7.00-7.80 (IIH, a), 8.27-8.80 (3H, m) , 10.50 (IH, br s) (2) MASS (m/z) : 560 (M+H) + NMR {CDCI3, δ) : 1.70-2.05 (2H, m) , 1.93 (1/4 κ 3H, s), 1.98 (3/4 x 3H, s) , 2.20-2.40 (2H, m) , 2.51 (3/4 x 3H, s), 2.55 (1/4 x 3H, s) , 2.83 (1/4 κ 3H, s), 2.98 (3/4 x 3H, s), 3.23-3.56 (2H, a), 4.51 (3/4 x 2H, ABq, Δ=0.27, J=15Hz) , 4.60 (1/4 x 2H, ABq, Δ=0.13, J=17Hz) , 4.95-5.18 (2H, a) , 7.02-7.72 (10H, m) 8.02-8.83 (4H, m) (3) MASS (m/z) : 498 (M+H) + NMR (CDCI3, δ) : 1.92-2.32 (2H, a), 1.97 (1/5 κ 3H, s), 2.06 (4/5 x 3H, s), 2.39 (3H, s), 2.42-2.70 (2H, m) , 3.08 (1/5 x 3H, s), 3.25 (4/5 x 3H, s) , 3.85-4.08 (2H, m) , 4.30 (4/5 x IH, d, J=15Hz) , 4.52 (1/5 x IH, d, J=17Hz), 4.91 (1/5 x IH, d, J=17Hz) , 4.97 (4/5 x IH, d, J=15Hz) , 5.23-5.67 (2H, m) , 6.62-7.68 (8H, m) , 8.25 (4/5 x IH, s), 8.43 (1/5 x IH, s) , 9.02 (1/5 x IH, d, J=9Hz) , 9.16 (4/5 x IH, d, J=9Hz) , 10.50 (IH, br s) (4) MASS (m/z) : 499 (M+H) + NMR (CDCI3, δ) : 1.80-2.15 (2H, a), 1.98 (1/4 κ 3H, s), 2.06 (3/4 x 3H, s), 2.45-2.67 (2H, a) , 2.50 (3H, s), 2.92 (1/4 x 3H, s), 3.08 (3/4 x 3H, s) , 3.68-3.88 (IH, m) , 4.02-4.22 (IH, m) , 4.48 (1/4 κ IH, d, J=17Hz), 4.56 (3/4 κ 2H, ABq, Δ=0.06, J=15Hz) , 4.68 (IH, br s), 4.80-5.28 (2H, m) , 4.83 (1/4 x IH, d, J=17Hz), 7.00-7.78 (9H, m) , 8.32 (3/4 x IH, s) , 8.43 (1/4 x IH, s) (5) MASS (m/z) : 595 (M+H) + NMR (CDC1 3 , δ) : 1.80-2.07 (2H, m) , 1.99 (3H x 1/5, 5), 2.04 (3H x 4/5, s) , 2.47-2.59 (2H, m) , 2.56 (3H, s), 2.63 (IH, dd, J=16.0, 6.0Hz), 2.85 (3H x 1/5, s), 2.99 (3H x 4/5, s) , 3.35 (IH, dd, J=16.0, 3.0Hz), 3.41-3.52 (2H, m) , 3.58-3.77 (6H, m) , 4.41 (IH x 4/5, d, J=15Hz) , 4.51 (IH x 1/5, d, J=16.0Hz), 4.56 (IH x 4/5, d, J=15.0Hz), 4.70 (IH x 1/5, d, J=16.0Hz), 5.04-5.22 (2H, m) , 7.00 (IH, d, J-l.OHz), 7.09-7.21 (2H, m) , 7.30 (IH, t, J=7.5Hz), 7.40-7.52 (2H, m) , 7.69 (2H, t, J=7.5Hz), 8.04 (IH, d, J=7.5Hz), 8.31 (IH x 4/5, d, J=1.0Hz), 8.39 (IH x 1/5, d, J=1.0Hz), 9.34 (IH x 1/5, br s) , 9.70 (IH x 4/5, br s) (6) MASS (m/z) : 596 (M+H) + NMR (CDCI3, δ) : 1.82-2.07 (2H, m) , 2.02 (3H x 1/4, S), 2.10 (3H x 3/4, s), 2.50-2.70 (3H, m) , 2.53 (3H, s), 2.87 (3H x 1/4, s) , 3.04 (3H x 3/4, s), 3.29-3.57 (3H, a) , 3.60-3.78 (6H, m) , 4.40 (IH x 3/4, d, J=15.0Hz), 4.53 (IH x 1/4, d, J=16.0Hz) , 4.67 (IH x 3/4, d, J=15.0Hz), 4.75 (IH x 1/4, d, J=16.0Hz), 5.06-5.26 (2H, m) , 7.12 (IH x 3/4, d, J=7.5HZ), 7.21 (IH x 1/4, d, J=7.5Hz), 7.31 (IH, t, J=7.5Hz), 7.44 (2H, t, J=7.5Hz), 7.51 (IH, s) , 7.58 (IH, d, J=7.5Hz), 7.66-7.74 (2H, m) , 8.21 (IH, d, J=7.5Hz), 8.35 (IH x 3/4, d, J=1.0Hz) , 8.40 (IH x 1/4, d, J=1.0Hz) (7) MASS (m/z) : 542 (M+H) + NMR (CDCI3, δ) : 1.72-2.31 (4H, m) , 1.88 (3H x 1/4, s), 1.91 (3H x 3/4, s) , 2.09 (3H, s), 2.39-2.54 (2H, m) , 2.57-2.69 (2H, a), 2.58 (3H, s), 3.08 (3H x 1/4, s), 3.15 (3H x 3/4, s), 4.62 (IH x 1/4, d, J=16.0Hz), 4.69 (IH x 3/4, d, J=15.0Hz), 4.73 (IH x 3/4, d, J=15.0Hz), 4.88 (IH x 1/4, d, J=16.0Hz), 5.23-5.42 (2H, a), 6.99 (IH, s), 7.09-7.25 (4H, m) , 7.40 (IH, d, J=7.5Hz), 7.52 (IH, m) , 7.67 (IH, d, J=7.5Hz), 8.44 (IH, s), 8.47 (IH x 3/4, d, J=7.5Hz), 8.61 (IH x 1/4, d, J=7.5Hz), 10.10 (IH, br s) (8) MASS (m/z) : 543 (M+H) + NMR (CDC1 3 , δ) : 1.83-2.27 (4H, m) , 1.99 (3H x 1/4, s), 2.04 (3H x 3/4, s), 2.17 (3H, s) , 2.43-2.76 (4H, m) , 2.55 (3H, s) , 2.91 (3H x 1/4, s) , 3.07 (3H x 3/4, s), 4.49 (IH x 3/4, d, J=15.0Hz), 4.60 (IH x 1/4, d, J=16.0Hz), 4.65 (IH x 3/4, d, J=15.0Hz), 4.79 (IH x 1/4, d, J=16.0Hz), 4.83-4.96 (IH, m) , 5.06-5.27 (IH, m) , 7.05-7.23 (2H, m) , 7.24-7.36 (IH, a), 7.37-7.57 (5H, a), 7.68 (IH, d, J=7.5Hz), 8.37 (IH x 3/4, s), 8.40 (IH x 1/4, s)

Claims: C 1 A M 5 A compound of the formula where n s lower aikyl, aryl which may have suitable substituent (s) , fluorenyl which may have suitable substituent (s) , heteromonocyclic group wr.ich may have suitable substituent (s) , or a group of tr.e formula : [in which R l is hydrogen, halogen, lower alkyl, nitre, di (lower) alkylamino, ammo, protected amino, hydroxyamino or lower alkoxy, Q is CK or N, L is a bivalent radical selected from ■ Y (m which Y is Cή' or N, Z is NH, 0 cr 5, ana is a single bond cr a double bond) and 'in wmch M s CH cr X, a a J is CH or N) ; , V w icn V is C or S) , o -SO T nyarogen, aryl wmch aay nave suitable s-ibstituent (s, , neterocyciic group, nyoroxy, acyloκ , ar \ lower, alxoxy, sulfooxy, aercapto, lower alkylthio, mcr.c (or d or tri) ar (lower/ alkylthio, acyltnio, am o, protected am o, guanidmo, acylguaniamo cr a group cf tne formula : ,ιr. which R~ s hyαroκy, ar (lower, alkoxy, aorpr.clmyl, piperazmyi wnicn may have suitable suostituent (s) , pipeπayl whicn aay nave εuitable suostituent (s ) , pyrrolidmyl, thiomorpholmyi, homopiperaz yl which aay have suitable suostituent r , s , iperaz c whicn may have suitable substituen (si . pipenaymxy wnicn aav have suitaole suostituent (s, , cr aamo having one or two suitable substituent is) , A^ s lower alxylene, R is nydrogen or lower aikyl, or R 8 and a group of the foraula : - ^-T are linked together t rorm R J is hydrogen, aryl which may have suitable substituent (s) , hydroxy, protected hyarcκ , cyclo (lower) lkyl, lower alkylthio, or heterocyclic group which aay have suitable substituent (s. , A 3 is bond or lower alkylene, Q R J is hydrogen cr lower aikyl, or R 9 and a group of the formula : -A 3 -R 3 are iir.jced tcgethe. to form ana 4 is carboκy, protected carboκy, heterocycliccarbonyl which may have suitable substituent (s) , or a group of the , * -CO-N (in which R° is hydrogen cr lower alkyl, and R c is hydrogen, aryl, ar(lower) lkyl which may have suitable substituent (≤; , [di (lower) al ylaminoj (lower) aikyl, or heterocyclic (lower) aikyl which may have suitable substituent (s) ) , or - 692 - R- and a group of the formula -A- J _ r. et -^the: tc form (in which R 10 is ar (lower) alkyl) , with proviso that when M is CH, ana J is CH, then Q is N, and a pharmaceutically acceptable salt thereof. 2. A compound of claim I, whereir. is lower alkyl, 1,2-methyienedioκyphenyi, pnenyi, naphthyl, fluorenyl which may have oκo, pyrrolyl, pyridyl, furyl whicn may have phenyl, thienyl or a group of the formula : in which R 1 is hydrogen, halogen, lower alkyl, nitro, di (lower) alkylamino, aair.c, hydroκyaaino or lower alkoκy, Q is CH cr N, L is a bivalent radical selected froa .V iin which Y lε Cή' or N, Z is NH, 0 or S, ana I ~ l ~ - is a single bend cr a dcub bond) and <(m which M is CH or N, and J is CH or N) ] , V A 1 is lower alkylene, -NHCO-, -C- (in which V is 0 or S), or -S0 2 -, T is hydrogen, phenyl or naphthyl, each cf which may have 1 to 3 substituent (s) selected from the group consisting of hydroxy, protected hydroxy, halogen, lower alkoxy and lower alkyl; imidazolyl; pyridyl; indolyl; thienyl; furyi; hydroxy; lower alkanoyloxy; heterocyciiccarbonyioxy; heterocyclic (lower) alkanoyloxy; [di (lower) alkylamino] (lower) alkanoyloxy; ar (lower) alkoxy; sulfooxy; mercaptc; lower alkylthio; mono (or di or tri)phenyl (lower) alkylthio; [di (lower) - alkylamino] (lower) alkanoyl hic; amine; acylamino; guanidino; guanidino having phenylsuifonyl substituted with 3 lower alkyl ana lower alkoxy; cr a group cf the formula : (in which R- is hydroxy, phenyl (lower) alkoxy; morpholinyl; pipera∑inyl which aay have 1 to 3 substituent (s) selected from the group consisting A lower alky ,]1 carboκy, protected carooκy, carboxy lower, alkyl, protected carboxy (lower; alkyl, heterocyclic group, cyclo (lower) alkyl, aryl, hydroxy • ( lowe ) alkyl, protected hydroxy (lower) alkyl, di (lower) alkylamino (lower) aikyl and acyi; piperidyl which may have 1 to 3 heterocyclic croup; pyrrciidinyl; thiomorphciinyl; hcmcciperazinyl which may have 1 to 2 lower alkyl; ciperazinio which aay have two or three lower alkyl; piperidyioxy whicn may have 1 to 3 lower alkyl; or amino having one cr two substituent ;s ) selected from the group consisting cf lower alkyl, ar (lower) alkyl, cyclo (lower) alkyl, heterocyclic group, monofcr di or tri) hydroxy (lower) alkyl, mono (or di or tri) (protected hydroxy) (lower) aikyl ana [di (lower) alkylamino] ( lower) alkyl; A- is lower alkylene, R° is hydrogen cr lower alkyl, or R° and a group of the foraula : -A--T are ked together to fora a group of the foraula : R J is hydrogen; phenyl which aay nave 1 to 3 substituen (s) selected from the group consisting of hydroxy, protected hydroxy, lower alkoxy ana halogen; hydroxy; protected hydroxy; cyclo (lower) lkyl; lower alkylthio; pyridyl; imidazolyl which may have acyl; thienyl; cr furyi; A 3 is bond or lower alkviene, ^ is hydrogen or lower alkyl, or * A and a group of the formula : -A J -A are ' . ir.kea together to form a group of the formula : R *1 is carboxy, esterified carboκy, piperazinylcarbonyl which may have lower alkyl, tetrahyaroquinoiylcarbonyl, or a group of the formula : R° -CO-N ; in which R is hydrogen or lower alkyl, and R D is hydrogen; phenyl; phenyl (lower) alkyl which aay have 1 to 3 substituent (s) selected from the group consisting of lower alkyl, lower alkoxy, carboxy, protected carboxy, mono (or di or tri)halo(lower) alkyl, ai (lower) alkylamino, [di (lower) alkylamino] (lower) aikyl, [di (lower) alkylamino] (lower) alkoxy, halogen and heterocyclic group which may have lower alkyl; [di (lower) alkylamino] (lower) alkyl; pyridyl (lower) lkyl which aay have 1 tc 3 substituent (s) selected from the group consisting of lower aikyl, lower alkoxy, halogen, ai (lower) alkylamino, protected amino, heterocyclic group and lower alkylthio; quinolyl (lower) aikyl; quinoxalinyl (lower) aikyl; pyrimidinyl (lower) aikyl; pyrazinyl (lower) alkyl; pyrazolyl (lower) aikyl or benzimidazolyl (lower) aikyl) ; or " 1 and a group c: ne rorau. -A 3 -P : .n.<ea tocetner :orm (in which R i0 is phenyi (lower) alkyli , with proviso that when M is CH, and J is CH, then Q is N. 3. A compound of claim 2, wherein T is hydrogen; phenyl cr naphthyi, each of which may have on or two substituent (s) selected from the group consistin of hydroκy, halogen, lower alkoxy and lower alkyl; imidazolyl; pyridyl; thienyl; furyl; hydroxy; lower alkanoyloxy; pyridylcarbonyloxy; pyridyl (lower) alkanoyloxy; piperidyl (lower) alkanoyloxy; [di (lower) alkylamino] (lower) alkanoyloxy; phenyl (lower) alkoxy; sulfooxy; mercapto; lower alkylthio; mono (or di cr tri)phenyi !lower) alkylthio; [di (lower) alkylamino] (lower) alkanoylthic; amino; aroylamino; lower alkanoylaaino; ar (lower) alkoxycarbonyla ino; guanidino; guanidino having phenylsulfonyl substitutea with 3 lower alkyl an lower alkoxy; or a group cf the formula : wmch R- s hycroxy, phenyi vlower) lkoxy; morpholinyl; piperazmyl whicn may have one cr two substituent (s) selected from the group consisting of lower alkyl, carboxy, esteπf eα carocxy, carboκy(lower)alkyl, esterified carooxy(lower)alkyl, pyriayl, pyrimidinyl, cyclo ,lower ) aikyl, pneny , nyoroκy lower alκvl, acyloxy(lower) aikyl, di (lower) alkylaamc (lower) aixyi, lower a_.-:ar.oyl ana lower alkoκycarbonyl; piperidyl wnicn aay have one or two piperidyl; pyrroliamyl; t omorphclmyl; hoaopiperazmyl wnicn aay have one or two lower al v ; piperazmio wnicn aay nave two _cwer aixyl; piperidyloxy wmch aay nave one cr two lower alkyl; cr ammo having one or two substituent ( s i selected from the group consisting of lower alkyl, phenyl (lower)alkyl, cyclo(lower ιalkyl, morpnolmyl, pyrazolyl, dι(or tnmyaroxy(lower alkyl, di (or tri)acyloxy(lower)alkyl ana [di (lower)alkylamino] (lower)alkyl • ; A 2 is lower alkylene, R° is hydrogen or lower alkyl, or R 8 and a group of the formula : -A 2 -T are linked together to form a group of the formula R" is hydrogen; phenyl which may have one cr two substituent(s) selected from the group consisting cf hydroxy, phenyl (lower)alkoxy, lower alkoxy ana nalogen; nydroxy; acyloxy; cyclo (lower)alkyl; lower alxylthio; pyridyl; imidazolyl whicn may have tolyisulfonyl; t ienyi; or furyl; A J is bond cr lower alkylene, 9 is hydrogen or lower alkyl, or ana a group or the rormuia : -A J 3-R3 are _mkea together to form a group cf the formula : R" 1 is carboxy, ..ower alkoxycarbonyi, piperazinylcarbonyl which may have lower aikyl, tetrahydrcqumolyicarbcnyi, or a group of the formula : .R- -CO-N Ε' vin which R 5 is hydrogen or lower alkyl, ana ° is hydrogen; phenyl; phenyl (lower) alkyl which aay have one or two substituent (s) selected fro- the group consisting of lower alkyl, lower alkoxy, carboxy, esterified carboκy, trihalo (lower) alkyl, di (lower) alkylaaino, [ai (lower) alkylaainoj (lower) aikyl, [ai (lower) alkylamino] (lower: lkoxy, halogen, triazolyl, piperazinyi which may have lower alkyl, pyrazolyl which may have lower alkyl, ana imidazolyl; [di (lower) alkylamino] >,lower) alxyl; pyriayl (lower) alkyl which may have one cr twc substituent (s) selected from the group consisting of lower alkyl, lower alkoxy, halogen, di (lower) alkylamino, acylamino, pyridyl and lower alkylthio; quinolyi (lower) aikyi; quinoxalinyl (lower) alkyl; pyrimidinyl 'lower) lkyl; pyrazinyl (lower) alkyl; pyrazolyl (lower.- lkyl or benzimidazolyl (lower;alkyl) ; or R - ana a group of the formula : -A~-R-' are linked together to fo m (in which R i0 is phenyl (lower)alkyl; 4. A compound of claim 3, wherein T is hydrogen; phenyl or naphthyl, each c z which may have one substituent selected from the group consisting of hydroxy, halogen, lower alkoxy and lower aikyl; imidazolyl; pyridyl; thienyl; furyl; hydroxy; lower al anoyloxy; pyridylcarbonyloxy; pyridyl 'lower) alkanoyloxy; piperidyl (lower) lkanoyloxy; [di (lower)alkylamino] (lower)al anoyloxy; phenyl (lower) alkoxy; sulfooxy; mercapto; lower alkylthio; mono (or di cr tri)phenyl (lower) aikylthio; [di (lower)alkylamino] (lower) ikanoylthic; amino; benzoylamino; lower alkanoylamino; phenyl (lower)alkoκycarbcnylamino; guanidino; guanidino having phenvlsulfonyl substituted with 2 lower aikyl ana lower alkoκy; or a group of the formula : R' r° ,m whicn R- is hyaroxy, phenyl \lower) alkoxy; morpholinyl; piperazmyl wnicn may nave cr.e suostitue t selected from the group consisting of lower ai.yl, carooxy, lower altoxycaroonyi; carooxy lower) alkyl, lower alkoxycarbonyi (lower) aikyl, pyridyl, pyπmiamyl, cyclo (lower) alkyl, phenyl, hyaroxy lower) a_. :yl, di (lower) alkylamino (lower) alkyl, lower alkanoyl and lower alkoxycarbonyi; pipencyl v/nicn may nave piperidyl; pyrrol αmyl; t oaorpnclmyl; homopiperazmy- wnicn may have j.ower alkyl; piperazimo whicn may have two lower alxyl; piperiαyioxy which may nave lower alxyi; mono (or di) (lower) alkylamino; cyclo (lower: alkylamino; phenyl (lower) alkylamino; morpholmyiaamo; pyrazolylammo; [di (lower) alkylamino] (lower) alkylamino; ammo having lower alkyl and [ai (lower) ai.Kylammo] (lower) alkyl; or [dι(or tri) hydroκy(lower) alkylamino; ; A~ is lower alkylene, P. is hydrogen or lower alkyl, or R 8 and a group of the formula : -A 2 -T are linked together to form a group of the formula : R J is nyarogen; phenyl whicn may nave one suostituent selected from tne group consisting of nydroκy, phenyl (lower! alkoxy, lower alkoxy and halogen; hydroxy; cyclo (lower) alkyl; lower alxyithio; pyriαyi; imidazolyl whicn may have tolylsulfonyl; t enyl; cr furyl; J is bond or lower alkylene, R is hydrogen cr lower aikyl, or y ana a group of the formula : -A 3 -R J are iι:;κed together to form a croup of the formula : R^ is carboκy, lower alkoxycarbonyi, piperazinylcarbonyl which may have lower alkyi, tetrahydroquinolylcarbonyi, or a group cf the formula : ,R- -CO- (in which R 5 is hydrogen cr lower aikyl, and R° is hydrogen; phenyi; phenyi (lower) alkyl which may have one substituent selected from the group consisting of lower aikyl, lower alkoxy, carboxy, lower alkoxycarbonyi, trihalo(lower) aikyl, di (lower) alkylamino, [di (lower) alkylamino] (lower) alkyl, [di (lower) alkylamino] (lower) alkoxy, halogen, triazolyl, lower alkyipiperazinyl, lower alkylpyrazolyl and imidazolyl; [di (lower) alkylamino] (lower) aikyl; pyridyl (lower)alkyi which may have one substituent selected from the group consisting cf lower alkyl, lower alkoxy, halogen, di (lower)alkylamino, lower alkanoylamino, pyridyl and lower alkylthio; quinciyl (lower) alkyl; σumoκalinyi (lower) alkyl; pyrimidinyl (lower) alkyl; pyrazinyl (lower) aikyl; pyrazolyl (lower) alkyl cr benzimidazolyl (lowe ) aikyl, ; or R- and a group of the formula : -. a . -P- 5 are .nked together to form in which P. is phenyl (lower) aikyl; A comoound cf the formula wherein W is lower alkyi, 1, 2-methyIenedioxyphenyi, phenyl, naphthyl, fluorenyi which may have oκo, pyrrolyl, pyridyl, furyl which aay have phenyl, thienyl or a group of the foraula : [in which R- is hydrogen, halogen, lower alkyl, nitro, di (lower) lkylamino, amino, hydroκyamino cr lower alkoxy, is CH or N, L is a bivalent radical selected froa —Y (in wnich Y is CH or N, Z is NH, 0 or S, and ZZ is a single bond or a double bond) and (in which M is C ' ή or M, and J is CH or N) ], T L 1 is lower alkylene, -NHCO-, I in which V is 0 or S) or -SC 2 -, R- is morpholinyl, A 2 is lower alkylene, p R is hydrogen or lower alkyi, 3 is hydrogen; phenyl which may have I to 3 substituent (s) selected from the group consisting of hydroxy, protected hydroxy, lower alkoxy and halogen; hydroxy; protected hydroxy; cyclo (lower) aikyl; lower alkylthio; pyridyl; imidazolyl which may have acyl; thienyl; cr furyl; A J is bond or lower alkylene, R 9 is hydrogen cr lower alkyl, or q 3 3 R and a group of the formula : -A J -R J are linked together to form a group of the formula : carboxy, esterified carbcxy, piperazinylcarbonyl which may have lower aikyl, tetrahydroquinciyicarbonyi, or a group of the formula : R- -CO-N R b (in which R 5 is hydrogen or lower alkyi, and P. is hydrogen; phenyl; pyridyl (lowe ) alkyl subεtituted with 1 to 3 substituen (s) selected froa the group consisting of lower alkyi, lower alkoxy, halogen, di (lower) alkylamino.. protected amino, heterocyclic group and lower alkylthio; quinolyl (lower) alkyl; quinoxalinyl (lower) alkyi; pyrimidinyl (lower) alkyl; pyrazinyl (lower) aikyl; pyrazolyl (lower) alkyl or benzi iaazolyl (lower) alkyl) ; or d a group of the formula -A J -R J are linked togethe to form in which R 10 is phenyl (lower) alkyi; with proviso that when M is CH, and J is CH, then Q is N, and a pharmaceutically acceptable salt thereof. 6. A compound of claim 5, wherein D R 3 is hydrogen; phenyl which aay have one cr two substituent is) selected froa the group consisting of hydroxy, phenyl (lower: alkoxy, lower aA.oκy ana halogen; hydroxy; acyloxy; cycle iicwer alkyi; lower alkylthio; pyridyl; iaidazolyi which may have tolylsulfonyi; 0 thienyl; or furyi; A ~ is ocnd or lower alkylene, Q R^ is hydrogen or lower alkyl, cr R 9 and a group of the formula : -A 3 -R J are _inked together to form a group of the formula : R is carboxy, lower alkoxycarbonyi, piperazinylcarbonyl which may have lower alkyl, tetrahydroσuinciylcarbonyl, or a group of the formula : ,R- -CO-N R < (in which R° is hydrogen or lower alkyl, and R 6 is hydrogen; phenyl; pyridyl (lower) aikyl substituted with one or two substituent (s) selected from the group consisting cf lower aikyl, lower alkoxy, halogen, di (lower) alkylamino, acylamino, pyridyl ana lower alkylthio; σumciyi (lower. -.-:yi; quinoxalinyl (lower; alkyi; pyrimidiny.. 'lower, alkyl; pyrazinyl (lower) alkyi; pyrazolyl (lower' lkyl cr cenzimidazolyi (lower) lkyl; ; cr R 4 and a group of the formula : -A J -R^ are lm.-:ea together (in which R-° is phenyl (lower) alkyl) . 7. A compound cf claim 6, wherein R J is hydrogen; phenyl which may have one substituent selected from the group consisting of hydroxy, phenyl (lower) alkoκy, lower aikoκy and halogen; hydroκy; cyclo (lower) alkyl; lower alkylthio; pyridyl; imidazolyl which may have tolylsulfonyi; thienyl; or furyi; A" is bond or lower alkylene, R y is hydrogen cr lower alkyi, or R 9 and a group of the formula : -A J -R J are linked together tc form a group of the foraula : R 4 is carboκy, lower alkoxycarbonyi, piperazinylcarbonyl which aay have lower aikyl, tetrahy roquinclylcarbonyl. a group of the formul; (in which p-' is hydrogen cr lower aikyl, and R° is hydrogen; phenyi; pyridyl (lower) aikyl substituted with one substituent selected from the group consisting cf lower alkyl, lower alkoxy, halogen, ai (lower: alkylamino, lower alkanoylamino, pyridyl and lower alkylthio; quinolyl (lowe : lkyl; quinoκalinyl (lower) alkyi; pyrimidinyl (lower) aikyl; pyrazinyl (lower)alkyi; pyrazolyl (lower)alkyi or benzimidazolyl (lower)alkyi) ; or R 4 and a group of the formula : -A 3 -R J are linked together tc form 0 (in which R 10 is phenyl (lower) alkyi; 8. A compound of claim 7, wherein is a σrouϋ of the formula : ( whicn R- is hydrogen, ana 2 is NH or C , V (in which V is 0) , p is hydrogen, " R J is hydrogen or phenyl, A A i • s l-ower a--. ■ yι-ene, P. is hydrogen, R is a group cf the formula : - R - 1 -CO-N A* (in which R D is lower alkyi, and P° is lower aikyipyridyi (lower; alkyi c: pyridyipyridyi (Icwer) lkyi, . 9. A comocund of the formula : whereir. W is lower alkyl, 1, 2-methyIenedioxyphenyi, pr.enyi, naphthyl, fluorenyl which may have cxc, pyrrciyl, pyridyl, furyl which may have phenyi, thienyl or a group of the formula : v»hιc. τ> - is hyaroge , halogen, lower alkyi, nitre, di (lower) ai <ylammo, armc, hyarcxyammo cr lower al .oxv, a s CH or N, 1 is a bivalent radical selected from Z is NH, 0 or S, ana H. IS a single bone or a aouble bond) and (in whicn M is CH or N, ana 1- is lower alkylene, -NKCO-, - IC- (m wnicn is C cr S, , or -SO ? -, R 2 s lower aikylpiperazmyi, A- is lower alkylene, R 8 is hydrogen or lower alkyl, RΛ is hydrogen; phenyi wnicn may have 1 to 3 suostituent (s! selected from the group consisting of hydroxy, protecte hydroxy, lower alkoxy and halogen; hydroxy; protected hydroxy; cyclo (lower) alkyl; lower alkylthio; pyridyl; imidazolyl which may have acyl; thienyl; or furyl; A 3 is bond or lower alkylene, R 9 is hydrogen or lower alkyl, or R^ and a group of the formula : -A 3 -R 3 are linked together to form a group of the formula : R 4 is carboxy, esterified carboxy, piperazinylcarbonyl which may have lower alkyl, tetrahydroquinolylcarbonyl, or a group of the formula : (in which R 5 is hydrogen or lower alkyl, and R is hydrogen; phenyl; phenyl (lower)alkyl which may have 1 to 3 substituent(s) selected from the group consisting of lower alkyl, lower alkoxy, carboκy, protected carboxy, mono (or di or tri)halo(lower) alkyl, di (lower) alkylamino, [di (lower) alkylamino] (lower) alkyl, [di (lower) alkylamino] (lower)alkoxy, halogen and heterocyclic group which may have lower alkyl; [di (lower) alkylamino] (lower) alkyl; pyridyl (lower) alkyl which may have 1 to 3 substituent (s) selected from the group consisting of lower alkyl, lower alkoxy, halogen, di (lower)alkylamino, protected amino, heterocyclic group, lower alkylthio; quinolyl (lower) alkyl; quinoxalinyl (lower) alkyl; pyrimidinyl (lower) alkyl; pyrazinyl (lower) alkyl; pyrazolyl (lower) alkyl or benzimidazolyl (lower)alkyl) ; or R 4 and a group of the formula : -A 3 -R 3 are linked together to form (in which R^ 0 is phenyl (lower)alkyl) , with proviso that when M is CH, and J is CH, then Q is N, and a pharmaceutically acceptable salt thereof. 10. A compound of claim 9, wherein R J is hydrogen; phenyl which may have one or two substituent(s) selected from the group consisting of hydroxy, phenyl (lower)alkoxy, lower alkoxy and halogen; hydroxy; acyloxy; cyclo (lower)alkyl; lower alkylthio; pyridyl; imidazolyl which may have tolylsulfonyi; thienyl; or furyl; "3 A J is bond or lower alkylene, R 9 is hydrogen or lower alkyl, or R 9 and a group of the formula : -A 3 -R 3 are linked together to form a group of the formula : R 4 is carooxy, lower alkoxycarbonyi, piperazmylcaroony. wnicn may have lower alkyl, tetranyaroq inclylcarocny1, cr a group of the formula : -CO-N A 5 \ R 6 (m wnicn R D is hydrogen or lower alkyl, ana ?° is nydrogen; phenyl; phenyl (lower) aAyl ft r.ιch may have one or two substituent (s) selectea from tne group consisting of lower alkyl, lower alkoxy, carboxy, esterified carboxy, trihalo 'lower, aikyl, di 'lower: alkylamino, [di (lower) alkylamino] (lower) alkyl, [di dower) alkylamino] (lower: aIκoxy, nalogen, triazolyl, piperazmyl which may have lower alkyi, pyrazolyl which may have lower alkyi, and imidazolyl; [di (lower: alkylamino] (lower) alkyl; pyridyl (lower) alkyl which may have one or two substituent (s) selected froa the group consisting of lower alkyi, lower alkoxy, halogen, ai (lowerj aixylaamo, acylamino, pyriαyl ana lower alkylthio; quino-yl ιlower) alkyi; quinoxalinyl (lower) alkyl; pyrimidm l 'lower) al yl; pyrazinyl (lower) aikyl; pyrazciyAlower; aA.yl or oenzimidazolyl (lower) alkyl) ; or R 4 and a group of the formula : -A J -R J are linked togetner tc form 1 n (in wnich R- 10 is phenyi (lower) aikyl.. 11. A compound of claim 10, wherein ?. is hydrogen; phenyl which may have one substituent selected from the group consisting of hydroxy, phenyl (lower)alkoxy, lower alkoκy and halogen; hydroκy; cyclo(lower)alkyl; lower alkylthio; pyridyl; imidazolyl which may have tolylsulfonyi; thienyl; cr furyi; A J is bond or lower alkylene, R 9 is hydrogen or lower alkyl, or R^ and a group of the formula : -A J -R" are linked together to form a group of the formula : R 4 is carboκy, lower alkoxycarbonyi, piperazinylcarbonyl which may have lower alkyl, tetrahydroquinolylcarbonyl, or a grouo cf the formula : R- -CO-N ,m wnicn R>5° is hydrogen or lower alkyl, and R° is hydrogen; phenyl; phenyl (lower) alkyi which may nave one substituent selectea from tne arcup ccnε_stmg cf lower alky., lower aA.exy, caroox lower alxoxycaroonyl, trmalo ,.o er; alkyl, di flower ' alkylamino, [d (lower) alkylamino] (lower, aikyl, [di (lower) alkylamino. 'lower > lkoxy, nalogen, triazolyl, lower alkylpiperazmyl. lower alkyipyrazciyl and imiαazolyl; [di (lower) alkylamino] (lower) al.-yi; pyridyl (lower) alkyl which may nave one suostitue selected from the group consisting of lower aiky lower alkoxy, halogen, di dower' alkylamino, lowe alxanoylammc, pyridyl and lower al.-:yithιc; qumolvl (lower) alkyl; quinoxal nyl (lower) alkyi; pyrimidinyl (lower)alkyl; pyrazinyl (lower) aikyl; pyrazolyl (lower) alkyl or oenzimiaazolyl (lower) lkyl ■ , cr and a group of the foraula : -A J -R J are linked togetne to form (in w ch R- is pnenyi (lower) alkyl 12. A compound cf claim II, whereir. W is a group of the formula : .m wm. .c.n __-i i.s .nyd,rogen, and ' Z is NH or 0) , V - , i .s -C II- (in which V is 0), Q R is hydrogen, R 3 is phenyi, -3 is lower alkylene, 5 is hydrogen R 4 is a group of the formula : R- 5 -CO-N ^ \ R 6 (in which R 5 is lower alkyl, and R° is phenyl (lower) alkyi, lower alkcκypyridy. (lower)aikyl or haiopyridyl (lower) alkyl) 13. A compound of the formula : wnerem W is lower alkyl, 1,2-methylenedioxyphenyi, phenyl, naphthyl, fluorenyl which may have oxo, pyrrolyl, pyridyl, furyl which may have phenyl, thienyl cr a group of the formula : in which P.- is hydrogen, halogen, lower alkyl, nitr di (lower) alkylamino, amino, hydroxyam or lower alkoκy, Q is CH or N, L is a bivalent radical selected from (in which Y is CH or N, Z is NH, 0 or S, and ZZZ- is a single bond cr a double bond) ana ι ' m which M or N, and .s _H or .\ A- is lower alkylene -NHCO-, -C- (in which V is C or Ξ) , -so 2 -, A- is lower alkylene, R 8 is hydrogen or lower alkyi, R 3 is hydrogen; phenyl which may have 1 tc 3 substituent ! selected from the group consisting of hydroxy, prote 1 - 717 - hydroκy, lower alkoκy and halogen; hyaroxy; protected hydroxy; cyclo (lower) alkyl; lower alkylthio; pyridyl; imidazolyl which may have acyi; thienyl; cr furyl; A is oond or lower alkylene, R 5 is hydrogen cr lower aikyl, or ?X and a group of the formula : -A 3 -?.- are linked together to form a group of the formula : R 4 is carboxy, esterified carboxy, piperazinylcarbonyl which may have lower alkyi, tetrahydroquinolylcarbonyl, or a group of the formula : (in which R 5 is hydrogen or lower alkyi, and P. is hydrogen; phenyl; phenyl (lower)aikyl which may have 1 to 3 substituent 'si selected froa the group ccnsiεting of lower aikyl, lower alkoxy, carboxy, protected carboxy, mono >or ai cr tri)halo (lower) aikyl, di (lower! alkylamino, [di (lower) alkylamino] (lower: alkyi, [di (lower) alkylamino] (lower) lkoxy, halogen and heterocyclic group which may have lower alkyi; [di (lower) alkylamino] (lower) lkyi; pyridyl (lower) alkyi which may have 1 to 3 substituent (s) selected from the group consisting of lower alkyl, lower alkoxy, halogen, di(lower) alkylamino, protected amino, heterocyclic group and lower alkylthio; quinolyl (lower) alkyl; quinoxalinyl (lower) alkyl; pyrimidinyl (lower) alkyl; pyrazinyl(lower)alkyl; pyrazolyl (lower)alkyl or benzi idazolyl (lower) alkyl) , or R 4 and a group of the formula : -A 3 -R 3 are linked together to form (in which R 10 is phenyl (lower) alkyl) , with proviso that when M is CH, and J is CH, then Q is N, and a pharmaceutically acceptable salt thereof. 14. A compound of claim 13, wherein R 3 is hydrogen; phenyl which may have one or two substituent (s) selected from the group consisting of hydroxy, phenyl (lower)alkoxy, lower alkoxy and halogen; hydroxy; acyloxy; cyclo (lower) alkyl; lower alkylthio; pyridyl; imidazolyl which may have tolylsulfonyi; thienyl; or furyl; A 3 is bond or lower alkylene, R 9 is hydrogen or lower alkyl, or R 9 and a group of the formula : -A 3 -R 3 are linked together to form a group of the formula : is carboxy, lower alkoxycarbonyi, piperazinylcarbonyl v.'hich may have lower alkyl, tεtrahyαroquinoiyicarbonyl, or a group of the formula : R- -CO-.NT (in which R- is hydrogen cr lower aikyl, and R~ is hydrogen; phenyi; phenyl (lower) aikyl which may have one cr two substituent (s) selected from the group consisting of lower alkyl, lower alkoxy, carboκy, esterified carboκy, trihalc (lower) lkyl, di (lower) alkylamino, [di (lower) alkylamino] (lower) alkyl, [di (lower) alkylamino] (lower) alkoκy, halogen, triazolyl, piperazinyi which may have lower alkyl, pyrazolyl which may have lower alkyl, and imidazolyl; [di (lower) alkylaminoj (lower) ikyl; pyridyl (lower) aikyl which may have one cr two substituent (ε) εeiected from the group consisting cf lower alkyi, lower alkoxy, halogen, di (lower) alkylamino, acylamino, pyridyl ana lower alkylthio; quinoiyl (lower) lkyi; quinoxalinyl (lower) alkyl; pyrimidinyl (lower) aikyl; pyrazinyl (lower) alkyl; pyrazolyl (lower: lkyl or benzimidazciyl (lower) alkyl) , or and a group of the formula : -A J -R J are linked together to form (in which R 10 iε phenyl (lower) alkyl • . 15. A compound of claim 14, wherein R 3 is hydrogen; phenyl which may have one suostituent selectea from the group consisting cf hyaroxy, phenyl (lower) lkoxy, lower alkoxy ana halogen; hydro cyclo (lower) alkyi; lower aikylthic; pyridyl; imidazo which may have tolylsulfonyi; thienyl; or furyi; A 3 is bond cr lower alkylene, R is hydrogen or lower aikyl, cr R Q andi aa ggrroouupp ooff tthnee ffoorrmmuullaa :: -A^ ~- 3 are linked togeth to form a group of the formul R * is carboxy, lower alkoxycarbonyi, piperazinylcarbonyl which may have lower aikyl, tetrahydroquinolylcarbon or a σrouo of the formula : .R- -CO-N R' 1 - 721 - ( in which R^ is nydrogen cr lower aikyj., ana R Ό is hydrogen; phenyl; phenyl dower alkyi which may- nave one substituent selectea froa tne group consisting of lower alkyl, lower alkoxy, carboxy, lower alkoxycarbonyi, trihaic dower) aikyl, di (lower: alkylamino, [di (lower;alkylamino] dower. l yl, [di (lower) alkylamino] (lower alkoxy, halogen triazolyl, iower alkyipiperazinyl, lower aikylpyrazclyl and imidazciyi; [di (iower) aikylammo] (lower; al l; pyridyl (iower)alkyl which may have one substituent selected from the group consisting cf iower alkyl, lower alkoxy, halogen, di (lower) alkylamino, lower alkanoylamino, pyridyl and lower alkylthio; quinolyl (lower) alkyl; quinoxalinyl (ioweraaaOalkyl; pyrimidinyl (iower)alkyi; pyrazinyl dower)alkyl; pyrazolyl (iower)alkyi or benzimidazoiyl(lower) alkyi) ; or R *5 and a group of the formula : -A 3 -R^ are linked together to form (in which R-° is phenyi dower) alkyl, 16. A compound of claim 15, wherein W is a group cf the formula : (in which R- is hydrogen, and Z is NH or 0) , V is -CI- (in which V is 0 or S) , R 8 is hydrogen, R 3 is hydrogen or phenyl, A 3 is lower alkylene, R 9 is hydrogen, and R 4 is a group of the formula R- -CO-N (in which R~* is lower alkyl, and R^ is pyridyl (lower) alkyl which may have lower alkyl or pyridyl, or quinolyl (lower) alkyl) . 17. A compound of the formula wherein is lower alkyl, 1,2-methylenedioxyphenyl, phenyl, naphthyl, fluorenyi which may have oxo, pyrrolyl, pyridyl, furyl which may have phenyl, thienyl or a group of the formula : [in which R~ is hydrogen, halogen, lower alkyl, nitro, di (lower) alkylamino, amino, hydroxyamino cr lower alkoxy, Q is CH or N, L is a bivalent radical selected from (in which Y is C ' ή or N, Z is NH, 0 or S, and is a single bond or a double bond) and (in which M is CH or N, and J is C . or N) j , XT A is lower alkylene, -NHC0-, -C- .in which V is 0 or S) • sc '2 9 - ' . T is hydroxy or iower alkylthio, A- is lower alkylene, R° is hydrogen cr lower alkyi, R 3 is hydrogen; phenyi which may nave 1 tc ? substituent (s) selected frca the group consisting of hyaroxy, protecte hydroxy, iower alkoxy ana halogen; hyaroxy; protected hydroxy; cyclo (lower) aikyl; lower alkylthio; pyridyl; imidazolyl which may have acyi; thienyl; or furyl; J is bond or lower alkylene, R 9 is hydrogen or iower alkyl, or ?.q ana a group or tne formula : -A3- 3 are _m.<eα tcgetner to form a σrouo cf the foraula : R^ is carboxy, esterified carboxy, piperazinylcarbonyl which aay have lower alkyi, tetrahydroquinolylcarbonyl, or a group of the foraula : y -CO-N -R' (in which R 3 is hydrogen or lower aikyl, ana R° is hydrogen; phenyi; [di (iower) alkyiam.mo] (lower) aikyl; pyridyl (lower) alkyi substituted with 1 to 3 substituent (s) selected froa the group consisting of iower alkyl, iower alkoκy, halogen, di (lower)alkylamino, protected amino, heterocyclic group and lower alkylthio; quinolyl (lower) alkyl; quinoxalinyl (lower)alkyl; pyrimidinyl (lower) alkyl; pyrazinyl (lower) alkyl; pyrazolyl (lower) alkyl or benzimidazolyl (lower)alkyl) ; or R 4 and a group of the formula : -A 3 -R 3 are linked together to form (in which R^° is phenyl (lower) alkyl) , with proviso that when M is CH, and J is CH, then Q is N, and a pharmaceutically acceptable salt thereof. 18. A compound of claim 17, wherein R 3 is hydrogen; phenyl which may have one or two substituent (s) selected from the group consisting of hydroxy, phenyl (lower) alkoxy, lower alkoxy and halogen; hydroxy; acyloxy; cyclo (lower) alkyl; lower alkylthio; pyridyl; imidazolyl which may have tolylsulfonyi; thienyl; or furyl; A 3 is bond or lower alkylene, R^ is hydrogen or lower alkyl, or R 9 and a group of the formula : -A 3 -R 3 are linked together to form a group of the formula : R 4 is carboxy, lower alkoxycaroonyl.. pioeraz yicarocnyi which may have lower aikyl, tetrahydrcqu olyicarbony or a group of the formula : ,R * -CO- .-6 wnicn R^ is hydrogen or lower aikyl, and R 6 is hydrogen; phenyl; [di (lower) alkylamino] (lower) aikyl; pyridyl (iower) alkyl substituted with one or two substituent (s) selected froa the grcuo consistin of iower aikyl, iower alkoxy, halogen, di (lower)alkylamino, acylamino, pyridyl and iowe alkylthio; σuinolyl (iower) lkyi; quinoxalinyl (lower/ aikyl; pyrimidinyl (lower) lky pyrazinyl (lower) aikyl; pyrazolyl (iower; alkyi or benzimidazclyl (lower) alkyl) ; or R 4 and a group of the formula : -A^-R -3 are linked togethe to form (in which R i is phenyi (iower) aikyl) . 19. A compound of claim 18, wherein R is hydrogen; phenyi which aay have one suostituen" selectee froa the group consisting cf hyaroxy, phenyl (iower) alkoxy, iower alkoxy and halogen; hyaroxy; cyclo (lower) alkyl; iower alkylthio; pyridyl; imidazolyl which may have tolylsulfonyi; thienyl; cr furyl; A 3 is bond cr iower alkylene, R is hydrogen or iower aikyl, cr R 9 and a group cf the formula : - ^-R J are linked together to form a αrouo cf the formula : R 4 is carboxy, lower alkoκycarbonyi, piperazinylcarbonyl which may have lower aikyl, tetrahydroquinolylcarbonyl, or a group of the formula : X -CO-N \ R 6 (in which R 5 is hydrogen or lower alkyl, and R is hydrogen; phenyl; [di (lower) alkylamino] (lower)aikyl; pyridyl dower) aikyl substituted with one substituent selected from the group consisting cf iower alkyl, lower aikoκy, halogen, di (lower) alkylamino, iower alkanoylamino, pyridyl and lower alkylthio; quinolyi (lower, alkyi; quinoxalinyl (lower) alkyl; pyrimidinyl dower) alkyl; pyrazinyl (lower) alkyl; pyrazolyl (iower) alkyl or benzimidazolyl (lower) alkyi) ; cr 1 - 728 - ana a group or tne rormula —n -*— * ■ are -inked tcgethe to fora 1U ;in which R 10 .s Dhenvl ( (1lowerj aiκv. 20. A compound of claim 19, wherein W is a group of the formula : (in which R- is hydrogen, ana Z is NH or C) , V A 1 is -C- (in which V is 0 cr S), R° is hydrogen, R 3 is hydrogen cr phenyl, A 3 is iower alkylene, y is hydrogen, and R^ is a group of the formula : A -CO-N R β (in which R- 1 is iower aikyl. ana R° is iower alkylpyridyl (lower, alkyi o: pyridyipy idyl (lower) al.-:yi) . 21. A process for preparing a compound of the formula wherein W is iower aikyi, aryl which may have suitable substituent (s) , fluorenyi which may have suitable substituent (ε) , heteromonocyclic group which may have suitable substituent (s) , or a group of the formula : [in which R 1 is hydrogen, halogen, iower alkyl, nitro, di (lower! lkylamino, amine, protected amino, hydroxyamino or iower alkoκy, Q is CH or N, L is a bivalent radical selectee 981 - 730 - ( which Y is Cή ' or N, Z is NH, C or S, and 211-1 is a single bona cr a aoubie bond) and (in which M is C'ή or N, and J is CH or N) ] , V A ^ is lower alkylene, -NHC0-, -C- (in which 7 is C cr S) , or _so 2 ~ ' T is hydrogen, aryl which may have suitable substituent (s) , heterocyclic group, hydroκy, acyloxy, a (iower; alkoxy, sulfooxy, mercaptc, lower alkylthio, mono (or a or tri) ar (Iower)alkylthio, acylthio, amino, protected amino, guanidino, acylguanidino or a group cf the formula : (in which P~ is hydroxy, ar(lower) alkoxy, mcrphcimyl, piperazinyi which may have suitable substituent (εi , piperidyl which may have suitable substituent < s ) , pyrroliainyl, thiomorphoiinyl, homopiperazinyl which may have suitable substituent (s ' , piperazinio which may nave suitable substituent (s) , piperiayioxy which may have suitable substituen ,s, , cr amine having one or two suitable substituent (s) , A. 2 is lower alkylene, R 8 is hydrogen or lower aikyi, or R 8 and a group of the formula : -A 2 -? are linked togethe: to form R 3 is hydrogen; aryl which may have suitable substituent (ε) , hydroxy, protected hydroxy, cyclo (lower) lkyl, iower alkylthio, or heterocyciic group which may have suitable substituent(s) , A 3 is bond or lower alkylene, R 9 is hydrogen or iower alkyi, or R 9 and a group of the formula : -A 3 -R" are linked together to form and R .4- is carboxy, protected carboxy, heterocycliccarbonyl which may have suitable substituent (si , or a group of the formula : ;m wnicn R D is hydrogen or iower aikyl, and R is hydrogen, aryl, a (lower) alkyi which may have suitable substituen (s) , [di (lower)alkylamino] (lower) lkyi; or heterocyclic (iower)aikyl which aay nave suitable substituent (s) / , or and a group of the foraula : -A"-R" are -inked togethe: to form (in which R 10 is ar(lower)alkyl) , with proviso that when M is CH, and J is CH, then Q is N, or a salt thereof, which comprises. (1) reacting a compound of the formula wherein R 3 , R 4 , R 8 , R 9 , T, A 2 and A 3 are each as definec above. or its reactive derivative or a salt thereof with a comcound cf the formula wherein W and V are each as defined above, or its reactive derivative, or a salt thereof to give a compound of the formula wherein R 3 , R 4 , R 8 , R 9 , , T, V, A 2 and A 3 are each as defined above, or (2) reacting a compound of the formula : wherein R 3 , R 4 , R 8 , R 9 , , A-, A 2 and J are each as defined above, or its reactive derivative at the carboxy group, or a salt thereof with a comoour.d of tne fory—m,u,- 1 - H-N; wnerem .s morpholino, piperazino which aay have εuitabie substituent (s) , piperidmo which may have suitable substituent (s) , pyrrolidino, thiomorphoimo, - -. homopiperazino which may have suitable substituent (s) , piperazinio which may have suitable substituent (s) or amino having one or two suitable substituent (s) , or itε reactive derivative, or a εalt thereof to give ? . a compound of the formula : 30 wherein R 3 , R 4 , R 8 , R 9 , , A", A 2 , A 3 and -X ' i are each as defined above, or a salt thereof, 35 3) reacting a compound of the formula wherein R J , R 4 , R 6 , R 9 , A 2 , A 3 and T are each as defined above, or a salt thereof with a compound of the formula : W-N=C=0 wherein W is as defined above, or a salt thereof to give a compound of the formula wherein R 3 , R 4 , R 8 , R 9 , A 2 , A 3 , W and 7 are each as defined above, or a salt thereof, or (4) reacting a compound of the formula : wherein R J , R 4 , R 8 , R 9 , A ~ , A J ana T are each as defined above, or a salt thereof with a compound of the formula : W-A -CH0 wherein W is as defined above, ana A 4 is bond or C-, -C alkylene or a salt thereof, and then subjecting the resultant compound to reduction reaction to give a coapound of the foraula : wherein R 3 , R 4 , R 8 , R 9 , A 2 , A 3 , A 4 , W ana T are each as defined above, or a salt thereof, or (5) reacting a coapound of the foraula : wherein R 3 , R 4 , R 8 , R 9 , A 2 , A 3 and T are each as defined above, cr a salt thereof with a compound of the formula : w-sc 2 -x wherein W is as defined above, and X is a leaving group, or a salt thereof to give a compound of the formula R (8 A 2 9 13 w—SO- > N I C 1H CO N I CH- -R 4 wherein R 3 , R 4 , R 8 , R 9 , A 2 , A 3 , W and T are each as defined above, or a salt thereof. 22. A pharmaceutical composition which comprises, as an active ingredient, a compound of claim 1 or a pharmaceutically acceptable salt thereof in admixture with pharmaceutically acceptable carriers. 23. A use of a compound of claim 1 or a pharmaceutically 6981 - 738 - acceptable salt thereof as an inhibitor on the production cf nitric oxide (NO) . 24. A method for the prophylactic or therapeutic treatment of nitric oxide (NO) -mediated diseases which comprises administering a compound of claim I cr a pharmaceutically acceptable salts thereof to human or animals. 25. A process fcr preparing a pharmaceutical composition which comprises admixing a compound of claim 1 or a pharmaceutically acceptable salt thereof with a pharmaceutically acceptable carrier.

Inventors: HAMASHIMA HITOSHI, HASHIMOTO SEIJI, INOUE TAKAYUKI, ITOH YOSHIKUNI, IWAMOTO TOSHIRO, OKU TERUO, YATABE TAKUMI, HAMASHIMA, HITOSHI, HASHIMOTO, SEIJI, INOUE, TAKAYUKI, ITOH, YOSHIKUNI, IWAMOTO, TOSHIRO, OKU, TERUO, YATABE, TAKUMI
Applicants: FUJISAWA PHARMACEUTICAL CO, HAMASHIMA HITOSHI, HASHIMOTO SEIJI, INOUE TAKAYUKI, ITOH YOSHIKUNI, IWAMOTO TOSHIRO, OKU TERUO, YATABE TAKUMI, FUJISAWA PHARMACEUTICAL CO., LTD., HAMASHIMA, HITOSHI, HASHIMOTO, SEIJI, INOUE, TAKAYUKI, ITOH, YOSHIKUNI, IWAMOTO, TOSHIRO, OKU, TERUO, YATABE, TAKUMI
Application year: 1995
Main classification: C07K5
IPC codes: A61K38, A61P3, A61P9, A61P11, A61P13, A61P15, A61P25, A61P27, A61P29, A61P43, C07K5