NOVEL PHENYL-SUBSTITUTED SULFONAMIDES

Abstract: Sulfonamide derivatives of the formula wherein J is phenyl fused to a specified carbocyclic or heterocyclic ring, said phenyl and said ring both being optionally substituted; R is H or CH₃; W is O or S; A is substituted monocyclic or bicyclic heterocyclic group; and their agriculturally suitable salts, exhibit herbicidal and plant growth regulant activities. They may be formulated for agricultural use in conventional manner. The novel compounds may be made in various ways, e.g. by reacting a novel sulfonylisocyanate or sulfony­ lisothiocyanate of formula JSO₂NCW with an appropriate heterocyclic amine of formula RHNA.

Description: Title NOVEL PHENYL-SUBSTITUTED SULFONAMIDES Background of the Invention This invention relates to 1,2-benzothiazinesulfonamides, 2,1-benzothiazinesulfonamides, 1,2-benzisothiazolesulfonamides, 2,1-benzisothiazolesulfonamides, 1,2-benzoxathiinsulfonamides, 2,1-benzoxathiinsulfon- amides, l,2-benzoxathiolesulfonamides, 2,1-benzoxathiolesulfonamides, 2-quinolonesulfonamides, l-isoquinolonesulfonamides, 2-oxindolesulfonamides, l-oxisoindolesulfonamides, benzo[b]pyran-2-onesulfonamides, benzo[c]pyran-l-onesulfonamides, benzo (cpyran-3-one- sulfonamides, benzoicjthiopyran-l-onesulfonamides, benzo[b]furan-2-onesulfonamides, benzo[c]furan-1-onesulfonamides, benzo[c)thiophen-l-onesulfonamides, 1tetralonesulfonamides, 2-tetralonesulfonamides, l-in- danonesulfonamides, 2-indanonesulfonamides, benzo[b- furan-3-onesulfonamides, benzo[bjpyran-4-onesulfonamides, 1,2-benzothiazepinesulfonamides, 2,1-benzo- thiazepinesulfonamides, 2-benzoxepin-llSH]-onesulfonamides, 1-benzoxepin-2[3H]-onesulfonamides, 3-benzoxe pin-2[1Hl-onesulfonamides, 2-benzothiepin-115H]-onesul- fonamides, 2-benzazepine-l-onesulfonamides, l-benzazepine-2-onesulfonamides, 2,1-benzoxathiepinsulfonamides, l,2-benzoxathiepinsulfonamides, benzocyclohepten-5-onesulfonamides, benzocyclohepten-6-onesulfonamides and 1benzoxepin-5[4H]-onesulfonamides, which are useful as agricultural chemicals and in particular as growth regulants or herbicides. U.S. Patent 4,127,405 teaches compounds which are useful for controlling weeds in wheat having the formula: EMI1.1 wherein R1 is EMI2.1 R3 and R6 are independently hydrogen, fluorine, chlorine, bromine, iodine, alkyl of 1-4 carbon atoms, alkoxy of 1-4 carbon atoms, nitro, trifluoromethyl, cyano, CH3S(O)n- or CH3CH2S(O)n- ; R4 is hydrogen, fluorine, chlorine, bromine or methyl; R5 is hydrogen, fluorine, chlorine, bromine, methyl or methoxy; R7 is hydrogen, fluorine, chlorine, bromine, alkyl of 1-2 carbon atoms or alkoxy of 1-2 carbon atom; -R8- s hydrogen, methyl, chlorine or bromine; Rg and R10 are independently hydrogen, methyl, chlorine or bromine; Q are independently oxygen or sulfur; n is 0, 1 or 2; ; X is hydrogen, chlorine, bromine, methyl, g ttl, alkoxy of 1-3 carbon atoms, tri fluoromethyl, CH3S- or CH3OCH2-; and Y is methyl orwmethoxy; or their agricul turally suitable salts; provided that: (a) when R5 is other than hydrogen, at least one of R3, R4, R6 and R7 is other than hydrogen and at least two of R3, R4, R6 and R7 must be hydrogen; (b) when R5 is hydrogen and all of R3, R4, R6 and R7 are other than hydrogen, then all of R3, R4, R6 and R7 must be - either chlorine or methyl; and (c) when R3 and R7 are both hydrogen, at least one of R4, R5 or R6 must be hydrogen. French Patent No. 1,468,747 discloses the following para-substituted phenylsulfonamides, useful as antidiabetic agents: EMI3.1 wherein R = H, halogen, CF3 or alkyl. Logemann et al., Chem. Ab., 53, 18052g (1959), disclose a number of sulfonamides, including uracil derivatives and those having the formula: EMI3.2 wherein R is butyl, phenyl or EMI3.3 and R1 is hydrogen or methyl. When tested for hypoglycemic effect in rats (oral doses of 25 mg/lOO g), the compounds in which R is butyl and phenyl weramost potent. The others were of low potency or inactive. Wojciechowski, J. Acta. Polon. Pharm. 19, p. 121-5 (1962) [Chem. Ab., 59 1633 el describes the synthesis of N-[ (2,6-dimethoxypyrimidin-4-yl)aminocar- bonyl]-4-methylbenzenesulfonamide: EMI4.1 Based upon similarity to a known compound, the author predicted hypoglycemic activity for the foregoing compound. Netherlands Patent 121,788, published September 15, 1966, teaches the preparation of compounds of Formula (i), and their use as general or selective herbicides, EMI4.2 wherein R1 and R2 may independently be alkyl of 1-4 carbon atoms; and R3 and R4 may independently be hydrogen, chlorine or alkyl of 1-4 carbon atoms. Compounds of Formula (ii), and their use as antidiabetic agents, are reported in J. Drug. Res. 6, 123 (1974) EMI4.3 wherein R is pyridyl. The presenc.eiof undesired vegetation causes substantial damage to useful crops, especially agricultural products that satisfy man's basic food needs, such as soybeans, barley, wheat, and the like. The current population explosion and concomitant world food shortage demand improvements in the efficiency of producing these crops. Prevention or minimizing the loss of a portion of valuable crops by killing, or inhibiting the growth of undesired vegetation is one way of improving this efficiency. A wide variety of materials useful for killing, or inhibiting (controlling) the growth of undesired vegetation is available; such materials are commonly referred to as herbicides. The need exists, however, for still more effective herbicides that destroy or retard weeds without causing significant damage to useful crops. Summary of the Invention This invention relates to novel compounds of Formula I, agriculturally suitable compositions containing them, and their method-of-use as pre-emergent or post-emergent herbicides or plant growth regulants. EMI5.1 wherein J is EMI5.2 EMI6.1 EMI7.1 EMI8.1 n is 0, 1 or 2; W is O or S; W1 is O or S; R is H or CH3; R1 is H, F, Cl, Br, CH3, OCH3, CF3, SCH3 or OCF2H; R2 is H or C1-C4 alkyl; R3 and R4 are independently H, C1-C4 alkyl, Cl or Br; R5 is H or CH3 R6 is H or CH3 R7 is H or CH3 A is EMI8.2 EMI8.3 X is CH3, OCH3 OCH2CH3, Cl, F, Br, OCF2H, CH2F or CF3; Y is H, CH3, OCH3, OC2H5, CH2OCH3, NH2, NHCH3, N(CH3)2, C2H5, CF3, SCH3, OCH2CH=CH2, OCH2C=CH, OCH2CF3, CN, N3, OCH2CH2OCH3, CH2SCH3, CR6(QCH3)2, EMI9.1 EMI9.2 CR6(QCH2CH3)2 or QCF2T where Q is O or S and T is H, CHC1F, CHBrF or CHFCF3; Z is CH, N, CCH3, CC2H5, CC1 or CBr ; Y1 is O or CH2; X1 is CH3, OCH3, OC2H5 or OCF2H; X2 is CH3, C2H5 or CH2CF3s Y2 is OCH3, OC2H5 ; SCH3, SC2H5, CH3 or CH2CH3; X3 is CH3 or OCH3; provided that a) when W is S, then R is H, A is EMI9.3 Z is CH or N, and Y is CH3, OCH3, OC2H5, CH2OCH3, C2H5, CF3, SCH3, OCH2CH=CH2, OCH2C=CH, OCH2CF3, OCH2CH2OCH3, CH(OCH3)2 or EMI9.4 b) the total number of carbon' atoms in R3 and R4 is less than or en al to 4; c) when X is Cl, F or Br, then Z is CH and Y is OCH3, OC2H5 NH2, NHCH3, N(CH3)2 or OCF2H ; d) when R5 is CH3, then n is O; e) when J is J24' then R4 and R5 are not both H and R4 is not Cl or Br ; and their agriculturally suitable salts. Preferred for reasons of their higher herbicidal activity, greater plant growth regulant activity or more favorable ease of synthesis are: 1) Compounds of Formula I where W is O, R2 is H or C1-C3 alkyl, R3 and R4 are independently H or C1-C3 alkyl and R1 is bonded to the ortho or meta position of the ring relative to the sulfonylurea moiety. 2) compounds of Preferred 1 where R1 is H, F, C1, Br,-CH3, OCH3, CF3 or SCH3; Y is CH3, OCH3, OC2H5, CH2OCH3, NH2, NHCH3, N(CH3)2, C2H5, CF3, SCH3, OCH2CH=CH2, oCH2CECH, OCH2CF3, OCH2CH2OCH3, CR6(OCH3)2, EMI10.1 CR6(OCH2CH3)2 or OCF2H; and Z is CH or N. 3) Compounds of Preferred 2 where R1 is H, R5 is H, A is EMI10.2 X is CH3, OCH3, C1, Br, CH2F or OCF2H; and Y is CH3, OCH3, OC2H5, CH2OCH3, CF3, OCH2CF3, CH(OCH3)2, EMI10.3 CH(OCH2CH3)2 or OCF2H. 4) Compounds of Preferred 3 where R is H, Y is CH3 or OCH3 and X is CH3, OCH3, Cl or Br. 5) Compounds of Preferred 4 where J is J1. 6) Compounds of Preferred 4 where J is 7) Compounds of Preferred 4 where J is J3. 8) Compounds of Preferred 4 where J is J4. 9) Compounds of Preferred 4 where J is J5. 10) Compounds of Preferred 4 where J is 11) Compounds of Preferred 4 where J is J7. 12) Compounds of Preferred 4 where J is 13) Compounds of Preferred 4 where J is J9. 14) Compounds of Preferred 4 where J is J10. 15) Compounds of Preferred 4 where J is J11. 16) Compounds of Preferred 4 where J is J12 17) Compounds of Preferred 4 where J is J13 18) Compounds of Preferred 4 where J is J14 19) Compounds of Preferred 4 where J is J15 20) Compounds of Preferred 4 where J is J16. 21) Compounds of Preferred 4 where J is J17 22) Compounds of Preferred 4 where J is J18. 23) Compounds of Preferred 4 where J is Jl9 24) Compounds of Preferred 4 where J is J20. 25) Compounds of Preferred 4 where J is J21. 26) Compounds of Preferred 4 where J is J22. 27) Compounds of Preferred 4 where J is J23. 28) Compounds of Preferred 4 where J is J24. 29) Compounds of Preferred 4 where J is J25 30) Compounds of Preferred 4 where J is J26 Specifically preferred for reasons of their highest herbicidal activity, greatest plant growth regulant activity and/or most favorable ease of synthesis are: N-1(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-2,3- dihydro-2-methyl-1,2-benzisothiazole-7-sulfonamide, 1,1-dioxide, m.p. 218-221 C ; N-[(4-methoxy-6-methyl-1,3,5-triazin-2-yl)aminocar- bonyl]-2,3-dihydro-2-methyl-1,2-benzisothiazole-7 sulfonamide, 1,1-dioxide, m.p. 210-212 C ; . N-[(4-methoxymethyl-6-methylpyrimidin-2-yl)aminocar bonyl3-2,3-dihydro-2-methyl-1,2-benzisothiRzole-7- sulfonamide, l,l-dioxide, m.p. 169-1710C; N-1(4-chloro-6-methoxypyrimidin-2-yl)aminocarbonyl]- 2,3-dihydro-2-methyl-1,2-benzisothiazole-7-sulfon- amide, 1,1-dioxide, m.p. 206-2080C; N-t(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]- 2,3-dihydro-2-(1-methylethyl)-1,2-benzisothiazole-7 sulfonamide, 1,1-dioxide, m.p. 234-236 C ; N-1(4-methoxy-6-methyl-1,3,5-triazin-2-yl)aminocar- bonyl]-2,3-dihydro-2-(1-methylethyl)-1,2-benziso thiazole-7-sulfonamide, 1,1-dioxide, m.p. 186-1880C; ; N-1(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl] 2,3-dihydro-2-propyl-1,2-benzisothiazole-7-sulfon amide, 1,1-dioxide, m.p. 197-1990C; N-[(4-methoxy-6-methyl-1,3,5-triazin-2-yl)aminocar- bonyl]-2,3-dihydro-2-ethyl-1,2-benzisothiazole-7- sulfonamide, 1,1-dioxide, m.p. 169-171 C; . N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl] 2,3-dihydro-2-methyl-2H-1,2-benzisothiazole-8-sul- fonamide, 1,1-dioxide, m.p. 258-266 C ; . N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-1,3 dihydro-3-oxoisobenzofuran-4-sulfonamide, m.p. 218-2200C; . N-[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl] 1,3-dihydro-2-methyl-1-oxo-1H-isoindole-7-sulfon amide, m.p. 215-217 C ; and . N-[(4-bromo-6-methoxypyrimidin-2-yl)aminocarbonyl] 2,3-dihydro-2-methyl-1,2-benzisothiazole-7-sulfon amide, 1,1-dioxide, m.p. 219-2210C. DETAILED DESCRIPTION OF THE INVENTION Synthesis The compounds of Formula I can be prepared by one or more of the methods described below in Equations 1, 2, 3 and 4. As shown in Equation 1, compounds of Formula I where J is other than J J12' 522 and J23, can be prepared by reacting a sulfonylisocyanate (W r 0) or a sulfonylisothiocyanate (W - S) of Formula II with an appropriate heterocyclic amine of Formula III. R, A and W are as previously defined. Equation 1 EMI13.1 The reaction is carried out at 250 to 100 C in an inert, aprotic solvent such as methylene chloride or xylene for O.5 to 24 hours as taught in U.S. Patent 4,127,405. Compounds of Formula I, where W is S and R is H, (Ia) can be prepared by reacting the appropriate sulfonamide of Formula IV with a heterocyclic isothiocyanate of Formula V, as shown in Equation 2. Equation 2 EMI13.2 The reaction is carried out at 250 to 800C in an inert, aprotic solvent such as acetone or acetonitrile in the presence of a base such as potassium carbonate for 0.5 to 24 hours. The required heterocyclic iso- thiocyanates V are prepared from the corresponding amines III as taught in our EP-A-35,893. Compounds 4f Formula I. where W is O (Ib) and J is other than J4. J5. J10. J11. J16. J17. J21. J24 and J@ can be prepared by reacting the sulfonamides of Formula IV with an appropriate methylcarbamate of Formula VI in the presence of an equimolar amount of tri sethylaluminun, as shown in Equation 3. Equation 3 EMI14.1 The reaction is carried out at 25- to 40 C in a solvent such as methylene chloride for 10 to 96 hours under an inert atmosphere as taught in our EP-A-82681 The required carbamates VT are prepared by reacting the corresponding amines III with dimethylcarbonate or methyl chloroformate in the presence of a strong base. Alternatively, compounds of Formula Ib. can be prepared by reacting a sulfonylcarbamate of Formula VII with an appropriate amine of Formula III, as shown in Equation 4. Equation 4 EMI14.2 The reaction is carried out at 50 to 100 C in a solvent such as dioxane for 0.5 to 24 hours as taught in our EP-A-44,807. The required carbamates vir are prepared by reacting the corresponding sulfonamides IV wfth diphenylcarbonate in the presence of a strong base. The intermediate sulfonylisocyanates (W a 0) and sulfonylisothiocyanates (W r S) of Formula II from Equation 1 can be prepared as shown in Equations 5, 6 and 7. As shown in Equation 5, sulfonylisocyanates of Formula IIa where J is other than J6' J12' J22 and J23 can be prepared by the reaction of sulfonamides of Formula IV with phosgene, in the presence of n-butylisocyanate and a tertiary amine catalyst, at reflux in a solvent such as xylene by the method of U.S. Patent 4,238,621. Equation 5 EMI15.1 The sulfonylisocyanates can also be prepared from the sulfonamides by a two step procedure involving (a) reacting the sulfonamides with n-butyl isocyanate in the presence of a base such as K2CO3 at reflux in an inert solvent such as 2-butanone forming a n-butylsulfonylurea; and (b) reacting this compound with phosgene and a tertiary amine catalyst at reflux in xylene solvent. The method is similar to a procedure taught by Ulrich and Sayigh, Newer Methods of Preparative Organic Chemistry, Vol. VI, p. 223-241, Academic Press, New York and London, W. Foerst Ed. Alternatively, as shown in Equation 6, the sulfonylisocyanates of Formula IIa can be prepared by reacting the corresponding sulfonyl chlorides VIII with cyanic acid salts. Equation 6 EMI16.1 The reaction is carried out at 25O to 100 C in an inert aprotic solvent such as acetonitrile for 0.5-24 hours in the presence of phosphorus pentoxide and an alkali metal salt such as lithium iodide according to the teachings of Japanese Patent No. 76/26,816 (Chem. Abst., 85:77892e (1976)). The sulfonylisothiocyanates of Formula IIb where 3 is other than J6, J12' 522 and J23 can be prepared, as shown in Equation 7, by contacting the sulfonamides of Formula IV with carbon disulfide in the presence of twoequiva1ents of-a strong base. The resulting salt is then reacted with phosgene according to the teachings of K. Hartke, Arch. Pharm., 299, 174 (1966). Equation 7 EMI16.2 The sulfonamides of Formula IV of Equations 2, 3, 4, 5 and 7 are important intermediates for the preparation of the compounds of this invention. The syntheses of the required sulfonamide -intermediates are described in Equations 8 and 9. As shown in Equation 8, sulfonamides of Formula IV can be prepared from the corresponding sulfonyl chlorides of Formula VIII by contacting with either anhydrous or aqueous ammonia. Equation 8 EMI17.1 The preparation of sulfonamides from sulfonyl chlorides is widely reported in the literature, fbr reviews see: F. Hawking and J. S. Lawrence, "The Sulfonamides," H. K. Lewis and Co., London, 1950 and E. H. Northey, "The Sulfonamides and Allied Compounds," Reinhold Publishing Corp., New York, 1948. The unsaturated sulfonamides of Formula IVa can also be prepared from the corresponding saturated sulfonamides of Formula IVb by the two step procedure shown in Equation 9. G1-G2 is SO2-NR2, SO2-O, CO-NR2, CO-O, CO-S, NR2-SO2, O-SO2, NR2-CO and O-CO, R1 and R2 are as previously defined. Equation 9 EMI17.2 The first step involves benzylic bromination by N-bromosuccinimide to give a monobromide which is subsequently dehydrobrominated in a second step by reaction with a suitable base such as triethyl amine or potassium-t-butoxide in an inert solvent such as THF. This method has been used to prepare isocoumarins from 3,4-dihydroisocoumarins, see R. Barry, Chem. Rev., 64, 229 (1964). In cases where R1 is a methyl function, competitive bromination at this site may occur resulting in a mixture. The desired bromide may be separated at this stage, or after treatment with the base, by standard methods. A similar method may e- used to prepare sulfonamides where J is J23 from sulfonamides where J is J22 (n t 1). The sulfonyl chlorides of Formula VIII of Equation 6 and 8 can be prepared from the corresponding amines IX by the method shown in Equation 10. Equation 10 EMI18.1 The reaction involves diazotization of the amine IX with sodium nitrite in HC1, followed by reaction of the diazonium salt with sulfur dioxide and cupric chloride in acetic acid analogous to the teachings of Yale and Sowinski, J. Org. Chem., 25, 1824 (1960). Alternatively, sulfonyl chlorides of Formula VIII can be prepared by a modification of the above procedure whereby the diazotization reaction is carried out in dilute sulfuric acid and the resulting diazonium salt is reacted with sulfur dioxide, HC1 and cupric chloride in a cosolvent mixture consisting of acetic acid-water (1:1) and an immiscible, inert solvent such as l-chlorobutane or methylene chloride at 00-400C for 1 to 24 hours Some of the sulfonyl chlorides of Formula VIII may best be prepared by direct chlorosulfonation de pending on the substitution pattern on the ring and the nature of the substituent as will be known to one skilled in the art. The sulfonyl chlorides of Formula Villa can also be prepared from the chloro compounds X by the two step sequence shown in Equation 11. R1, R2 and n are as previously defined, except that R1 is not halogen when it is para to the sulfonyl group or SCH3. R' is C1-C4 alkyl or benzyl. Equation 11 EMI19.1 The first step involves nucleophilic displacement of the chlorine atom with an alkyl or benzyl mercaptide to give an intermediate sulfide. The reaction'can be carried out at 250 to 800C in a polar solvent such as DMF for 0.5-24 hours. The sulfide is then oxidatively chlorinated to the desired sulfonyl chloride VIIIa by the addition of molecular chlorine or a chlorine equivalent to the sulfide in the presence of water at 150 to 8O0C in an aliphatic carboxylic acid solvent such as acetic acid or an inert organic solvent such as dichloroethane for 1 to 24 hours. Many of the chloro compounds of Formula X in Equation 11, where n = 0, can be prepared by the reaction sequence shown in Equation 12. When R1 is para to the sulfonyl group, then it is H, OCH3 or CF3. When R1 is meta to the sulfonyl group, then it is F, Cl, CH3, OCH3 or CF3. R2 and R5 are as previously defined. Equation 12 EMI20.1 The sequence begins by contacting an appro pr iately substituted 6-t-butylbenzenesulfonamide XIa with two equivalents of butyl lithium at 0 to 250C in an inert solvent such as THF for 2 to 10 hours to give a dianion according to the teachings of J. Lombardino, J. Org. Chem., 36, 1843 (1971). The dianion can then be trapped with an ester or, when R5 is H, with dimethylformamide at -780 to 250C to produce, upon aqueous .id workup, the hemiaminal xrz. The hemiaminal XII can be de-t-butylated and dehydrated by a catalytic amount of acid such as i-toluenesulfonic acid in a solvent such as benzene or toluene at reflux. The resulting benzisothiazole XIII can be reduced with a reagent such as sodium borohydride in a suitable solvent such as ethanol to produce a 2,3-dihydrobenzisothiazole which is N-alkylated to give Xa by standard methods known to one skilled in the art. Many of the chloro compounds of Formula X in Equation 11, where n = 1, can be prepared by the reaction sequence shown in Equation 13. R1 and R2 are as defined for Equation 12. Equation 13 EMI21.1 As in Equation 12, the N-substituted-benzenesulfonamides XI is contacted with 2 equivalents of butyl lithium to form a dianion, which is now trapped with ethylene oxide to produce alcohol XIV. The alcohol can be mesylated by treatment of XIV with mesyl chloride in the presence of an equivalent of a tertiary amine at 0 to 250C for 1 to 24 hours in a solvent such as methylene chloride. The resulting mesylate is cyclized by heating with a base such as potassium carbonate in a solvent such as DMF to produce the desired compounds Xb. Many of the sulfonyl chlorides of Formula VIIIb can also be prepared from the thioether compounds A as shown in Equation 13a. R1 is not Br, SCH3 or oCF2H. R4 and R5 are as previously defined. Equation 13a EMI22.1 As in Equation 13a, the N-methyl carboxamide A is contacted with 2 equivalents of butyl lithium to form a dianion, which is trapped with 2 equivalents of the appropriate epoxide to produce B. Hydrolysis of the amide to its corresponding carboxylic acid followed by acid catalyzed cyclization gives the lactone C. Oxidative chlorination of C as described previously in Equation 11 produces the desired sulfonyl chloride VIIIb. The amines of Formula IX in Equation 10, can be prepared by reduction of the corresponding nitro compounds of Formula XV, as shown in Equation 14. Equation 14 EMI23.1 The reduction of nitro compounds to amines can be carried out by any of several known methods as described in Preparative Organic Chemistry, 4 Ed., p. 557-563, John Wiley and Sons, New York and London, G. Hilgetag and A. Martini Ed. The nitro compounds of Formula XV in Equation 14 can be prepared by the procedures outlined in Equations 15 to 41. As shown in Equation 15, nitro compounds of Formula XV, where J is J1 (XVa) can be prepared starting from the appropriately substituted nitrobenzenes of Formula XVI. R' is H or CH2C1, R1, R2, R5 and n are as previously defined. Equation 15 EMI24.1 The nitrobenzenes XVI are first reduced to their corresponding amines and nitrated by standard methods to produce, in part, compounds of Formula XVI I. In some instances, it may be desirable to first protect the amino group as its acetate prior to nitration as is known to one skilled in the art. The desired nitro compound XVII can be isolated by either fractional crystalization or chromatographic procedures and converted to sulfonyl chlorides XVI II by the method pre viously discussed in Equation 10. The intermediate sulfonyl chlorides XVIII can be converted into their corresponding sulfonamides by reaction with an appropriate amine (see Equation 8 for references) and subsequently cyclized a) when R' is CH2C1, to the nitro1,2-benzothiazines XVa, where n is 1, by heating in the presence of a base such as potassium carbonate or b) when R' is H, by contacting the sulfonamide with NBS in a solvent such as carbon tetrachloride to give sulfonamides where R' is Br, followed by contacting this product with a base to give the nitro benzisothiazoles XVa where n is 0. (Note discussion of Equation 9 for NBS brominations when R1 is methyl.) The procedure of Equation 15 is similar to the method taught by E. Sianesi et al., Chem. Ber., 104, 1880 (1971) for the preparation of substituted 1,2 benzothiazine-l,l-dioxides. The starting nitrobenzenes XVI can be prepared by standard methods known to one skilled in the art. Alternatively, as shown in Equation 16, the nitro compounds of Formula XVa where n is 1 can be prepared, in part, by contacting the nitro acetamides XIX with fuming sulfuric acid according to the method taught by H. Zenno and T. Mizutani, Japanese Patent No. 44/32,404 (1969) (Chem. Abst.: 72:79122 (1970)) for the preparation of 7-nitro-1,2-benzothiazine-l,ldioxide. The resulting benzothiazines can be isolated and subsequently alkylated by standard methods known to one skilled in the art. Equation 16 EMI26.1 The nitro compounds of Formula XVa where n is C can also be prepared from the corresponding 1,2-benzisothiazoles XX as shown in Equation 17. R1, R2 and R5 are as previously defined. Equation 17 EMI26.2 Nitration of XX gives, in part, the 7-nitro derivative which is isolated by standard methods. The derivative is converted to its l,l-dioxide by treatment with hydrogen peroxide. Reduction of the carbon-nitrogen double bond with NaBH4 followed by alkylation of the resulting sulfonamide gives compounds XVa where n is 0. The above reactions are characteristic of 1,2 benzisothiazoles XX. - For reviews of their synthesis and reactions, see L. L. Bambas, "The Chemistry of Heterocyclic Compounds," Vol. 4, part III, 1952, p. 223-378, and M. Davis, Adv. Heterocyclic Chem., Vol. 14 (1972) p. 43-98. 1,2-Benzothiazines are also well known in the literature, for a review of their chemistry and alternate methods of their preparation see J. G. Lombardino, D. E. Kuhla, Adv. Heterocyclic Chem., Vol. 28 (1981) p. 73-126. As shown in Equation 18, nitro compounds of Formula XVb where J=J2 can be prepared from the appropriately substituted nitro sulfonyl chlorides XVIII. R' is H or CH2Cl, R1, R5 and n are as previously defined. Equation 18 EMI27.1 The nitro sulfonyl chlorides XVII I, previously described in Equation 15, can be a) cyclized to the nitro benzoxathiins XVb (n=l) by heating in water at 500 to 1000C for 0.1 to 1 hour when R' is CH2C1 or b) cyclized to the nitro benzoxathioles XVb (n=0) by brominating with NBS or bromine (see discussion of Equation 9 for brominations when R1 is methyl followed by heating in water as described above. This is similar to the method taught by Clemo and Turnbull, 3. Chem. Soc., 124 (1947) for the preparation of substituted 2,1-benzoxathiins. 2,1-Benzoxathiins and 2,1-benzoxathioles are well known in the literature, for a review of their synthesis and reactions see Chemistry of Heterocyclic Compounds, Vol. 21, John Wiley and Sons, New York, 1966, part 2 and part 1, respectively. As shown in Equation 19, nitro compounds of Formula XV where J = J4 (XVd) can be prepared from the appropriately substituted amines XVI I. R' is H or CH2C1, R1, R and n are as previously defined. Equation 19 EMI28.1 The nitro amines XVII, previously described in Equation 15, can be converted into the corresponding cyano compounds XXI by the "Sandmeyer Reaction" (T. Sandmeyer, Chem. Ber., 17, 1633, 2650 (1884)). The cyano function is hydrolyzed to a carboxylic acid by methods known to one skilled in the art, and the carboxylic acids or their corresponding esters can be a) cyclized to the nitro isocoumarins XVd (n=l) by heating in the presence of base when R' is CH2C1, or b) cyclized to the nitro phthalides XVd (n=0) when R' is H by first brominating with NBS or bromine (note discussion of Equation 9 for brominations when R1 is methyl) followed by heating in a solvent such as aqueous dioxane. The latter method is that taught by J. A. Houbion et al., Org. Prep. and Procedures Int., 11, 27 (1979) for the preparation of 7-nitrophthalide (XVd, n=O, R1aH). The procedure of Equation 19 is similar to the method of P. Banejce and D. Chaudhury, 3. Org. Chem., 26, 4344 (1961) for the preparation of substituted isocoumarins; similar methods can be utilized for the preparation of isocoumarins of the J2q type. Isocoumarins are well known in the literature, for a review of their synthesis and reactions see R. Barry, Chem. Rev., 64, 229-260 (1964). The nitro compounds of Formula XVd, where n = 0 can also be prepared by reduction of the corresponding 3-nitrophthalic anhydrides with either sodium borohydride or lithium aluminum hydride in tetrahydrofuran as taught by M. Kayser and P. Morand, Can. J. Chem., 58, 2484 (1980) for the preparation of 7-nitrophthalide (XVd; n = 0, R1 = H). Phthalides and phthalic anhydrides are well known in the art, for a review of their synthesis and reactions see, S. Wawzonek, Heterocyclic Compounds, Vol. 2, John Wiley and Sons, Inc., New York, 1951. As shown in Equation 20, nitro compounds of Formula XV where J is J5 (XVe) can be prepared from the appropriately substituted cyano compounds XXI. R' is H or CH2C1, R1, R5 and n are as previously defined. Equation 20 EMI29.1 EMI30.1 The nitrobenzonitriles XXI, previously described in Equation 15, can be converted into mercaptans XXII by reacting compounds XXI where R' is Br or CH2C1 with an alkali metal salt of hydrogen sulfide in a polar solvent such as ethanol or DMF according to the teachings of S. Gabriel and E. Leupold, Chem. Ber., 31, 2646 (1898). The cyano mercaptans are cyclized to the thiol ethers by heating in aqueous acid as taught by M. Renson and R. Collienne, Bull. Soc. Chem. Belges, 73, 491 (1964) for the preparation of 2-thiophthalide. Alternatively, as shown in Equation 21, the nitro compounds of Formula XVe can be prepared from the lactones of Formula XVd by reaction with potassium t-butyl mercaptide in a solvent such as DMF at 0 to 100C for 0.5 to 24 hours to give the carboxylic acids XXII I, which are then heated in the presence of a catalytic amount of an acid such as p-toluenesulfonic acid in a solvent such as xylene at 1000 to 1400C for 2 to 24 hours. Equation 21 EMI30.2 EMI31.1 2-Thiophthalides are widely reported in the literature, for a review of their synthesis and reactions see, B. Iddon, Adv. Heterocyclic. Chem., Vol. 14 (1972) pp. 368-381. As shown in Equation 22, nitro compounds of Formula XV, where 3 is J3 (XVc) can be prepared from the appropriately substituted benzonitriles XXI. R' is H or CH2Cl, R1, R2' R5 and n are as previously defined. Equation 22 EMI31.2 The benzonitriles XXI, previously described in Equation 19, are hydrolyzed to carboxylic acids, converted to their corresponding acid chlorides by contacting with a reagent such as thionyl chloride and subsequently reacted with the appropriate amine, by standard methods, to give the amides XXIV. The intermediate amides XXIV can be cyclized to the nitro compounds XVc by the procedures previously described in Equation 15 for converting sulfonamides of XVI II into nitro compounds XVa. Alternatively, the nitro compounds of Formula XVc can be prepared from the nitro compounds of Formula XVd as shown in Equation 23. R1 R2, R5 and n are as previously defined. Equation 23 EMI32.1 The reactions of phthalides with amines to produce phthalimidines is well known, see C. Hollins, The Synthesis of Nitrogen Ring Compounds, Ernest Benn Limited, London, 1924. In these reactions, heating the phthalides (XVd, n = 0) with an amine produces the phthalimidines (XVc, n = 0) directly, the intermediate alcohols XXV (n = 0) are not isolated. With the 3,4dihydrocoumarins (XVd, n = 1) the intermediate amide alcohols XXV (n = 1) are formed (see P. Maitte, Collog. Intern. Centre Natl. Rech. Sci. (Paris), 64, 197 (1955), Chem. Abst., 55:10426 (1961)) and can be converted to the dihydroisoquinolines XVc (n = 1) by first conwers-ion to the corresponding mesylate followed by heating with a base as described above in Equation 13 for the preparation of compounds Xb from the sulfonamide alcohols XIV. For a comprehensive review of the synthesis and reactions of dihydroisoquinolones see N. J. McCorkindale, The Chemistry of Heterocyclic Compounds, Vol. 38, part III, John Wiley and Sons, New York, in press. As shown in Equation 24, nitro compounds of Formula XV, where J is J6 (XVf) can be prepared, in part, by cyclization of the appropriate arylproprionic (n = O) or arylbutyric (n = 1) acids XXVI. R1, R3, R4, R5 and n are as previously defined. Equation 24 EMI33.1 The reaction is carried out by heating the acid with a suitable condensing agent such as polyphosphoric acid, hydrofluoric acid, sulfuric acid or stannic chloride or the acid may be converted to its chloride and heated with a typical Friedel-Crafts reagent such as aluminum chloride or stannic chloride. For a comprehensive review of this and related reactions, see "Friedel-Crafts and Related Reactions", Vols. 1-4, Interscience, New York and London, G. A. Olah, Ed. This procedure has been used to prepare a number of substituted-7-nitro-l-indanones (XVf, n = 0), see: H. Jones and T. Y. Shen, German Patent 2,337,120 (1974) and Y. Takahi and Y. Yura, Japanese Patent 78/12,421 (1978) Chem. Abst., 89:101857c. Alternatively, the nitro compounds of Formula XVf can be prepared by benzylic oxidation of the corresponding nitroindanes or nitrotetralines as taught by D. Biggs, et al., J. Med. Chem., 19, 472 (1976) for the preparation of 8-nitrotetralone (XVf, n = 1, R1, R3, R4 and Rg = H). Nitroindanes and nitrotetralines are well known in the literature and can be prepared by methods known to one skilled in the art. Additionally, ketones of Formula XVf where R3 and/or R4 are other than hydrogen can be prepared from ketones XVf where R3 and/or R4 are hydrogen by standard ketone alkylation and halogenation methods. For a review, see: H. House, Modern Synthetic Reactions, 2nd Edition, W. A. Benjamin, Inc., Menlo Park, California, 1972, p. 542-570 and 459-478, respectively. As shown in Equation 25, nitro compounds of Formula XV where J is J7 (XVg) can be prepared from the appropriately substituted nitrobenzenes XVI. R' is Br or CH2Br, R1, R2, R5 and n are as previously defined. Equation 25 EMI35.1 The nitrobenzenes XVI, previously described in Equation 15, are heated with thiourea in a suitable solvent such as ethanol to give thiouronium salts which are oxidatively chlorinated in aqueous acetic acid to give the sulfonyl chlorides XXVI I (see also discussion of Equation 11). The sulfonyl chlorides XXVI I are dissolved in 108 aqueous sodium hydroxide solution and the nitro groups are catalytically hydrogenated to give intermediate amino sulfonate salts. The salts are cyclized with phosphorous pentachloride and acetyl chloride to give the sultams XXVIII according to the teachings of B. Loev and M. F. Kormendy, J. Org. Chem., 30, 3163 (1965) for the pre- paration of 3,4-dihydro-2,1-benzothiazine-2,2-dioxide (XXVIII, n - 1, R1, R5 = H). Alternatively, the sulfonyl chlorides XXVII can be converted to their corresponding sulfonamides by the methods discussed in Equation 8. Reduction of the nitro group according to procedures of Equation 14 gives the corresponding amino sulfonamides which are cyclized to sultams XXVIII by heating, in the presence of SC1, according to the teachings of E. Sianesi, et al., Chem. Ber., 104, 1880 (1971) for the preparation of 3,4-dihydro-2,1-benzothiazine-2,2-dioxide (XXVIII, n = 1, R1, R5 = H). The sultams XXVIII can be nitrated, in part, ortho to the ring nitrogen by standard methods known to one skilled in the art. Isolation by either fractional crystallization or chromatographic methods followed by alkylation of the ring nitrogen under standard conditions gives the nitrosultams XVg as taught by E. Sianesi loc. cit. for the preparation of l-methyl-8-nitro-3,4-dihydro-2,1-benzothiazine-2,2dioxide (XVg, n = 1, R1, R5 - H, R2 = CH3). The sultams of Formula XXVIII of Equation 25 where n = 1, can also be prepared from anilines XXIX as shown in Equation 26. R1 is as previously defined. Equation 26 EMI36.1 EMI37.1 The substituted anilines XXIX are reacted with methyl chlorosulfonylacetate in the presence of an acid scavenger to give methyl sulfamoyl acetate intermediates which are hydrolized with dilute sodium hydroxide solution to the corresponding carboxylic acids XXX. The carboxylic acids XXX can be cyclized (note discussion of Equation 24) by heating with polyphosphoric acid to give the 4-benzothiazinones XXXI as taught by B. Loev et al., J. Org. Chem., 31, 3531 (1966) for the preparation of 4-keto-3,4-dihydro-2,1benzothiazine-2,2-dioxide (XXXI, Ri = H). When R1 is meta to nitrogen, cyclization may produce an isomeric mixture. The desired compounds XXXI can be isolated by either fractional crystallization or chromatographic methods known to one skilled in the art. The benzothiazines XXVIII (n a 1) are prepared by reducing the tosylhydrazone derivative of ketones XXXI with catecholborane in a solvent such as chloroform for 2 to 24 hours at ambient temperatures according to the teachings of G. Kabalka and J. Chandler, Synthetic Commun., 9, 275 (1979). The synthesis and chemistry of 2,l-benzothia- zines has been reviewed, see J. G. Lombardino and D. E. Kuhla, Adv. Heterocyclic Chem., Vol. 28 (1981) p. 73-126. Additionally, for a review of the synthesis and chemistry of benzothiazinone dioxides, see P. Catsoulacos and Ch. Camoutsis, a. Heterocyclic Chem., 16, 1503 (1979). As shown in Equation 27, nitro compounds of Formula XV where J is J8 (XVh) can be prepared from the appropriately substituted nitrophenols XXXII. R' is Br or CH2Cl, Rl, R5 and n are as previously defined. Equation 27 EMI38.1 The nitrophenols XXXII, prepared by methods known to one skilled in the art, are heated with aqueous sodium sulfite to give the sulfonic acids XXXII I which are then cyclized by heating with phosphorous oxychloride. The method is similar to those taught by Marckwald and Frahne, Chem. Ber. 31, 1854 (1898) for the preparation of 1,2-benzoxathiole, and Truce and Hoerger, J. Amer. Chem. Soc., 76, 5357 (1954) and 77 2496 (1955) for the preparation of 1,2-benzoxathiin. Alternatively, compounds of Formula XVh where n " 0 can be prepared from nitrophenols XXXIV by the three step sequence shown in Equation 28. This is the method taught by Shearing and Smiles, J. Chem. Soc., 1348 (1937) for the preparation of 5-methyl-1,2-benzoxathiole. For a review of this and alternate methods of synthesis of 1,2-benzoxathioles, see Chemistry of Heterocyclic Compounds, Vol. 21, part 1 (1966). Equation 28 EMI39.1 Compounds of Formula XVh where n = 1 can be prepared from nitrophenols XXXII where R'=R5=H by the three step sequence shown in Equation 29. Equation 29 EMI39.2 The phenol is brominated with NBS in a solvent such as carbontetrachloride and the hydroxy group is then converted to its methanesulfonate ester by treatment with mesyl chloride in the presence of an acid scavenger such as triethylamine in a solvent such as methylene chloride. The methanesulfonate ester is then cyclized by reacting with a strong base such as sodium hydride or potassium t-butoxide in a polar solvent such as DMF at 0 to 800C for 0.5 to 24 hours. For alternative methods of synthesis and the reactions of 1,2-benzoxathiins, see Chemistry of Heterocyclic Compounds, Vol. 21, part 2, (1966). As shown in Equation 30, nitro compounds of Formula XV where J is Jg (XVi) can be prepared from the appropriately substituted nitrobenzenes XVI. R' is Br or CH2Br, R1, R2, R5 and n are as previously defined. Equation 24 EMI40.1 The nitrobenzenes XVI, previously discussed 1n - Equation 15, are reacted with potassium cyanide in a solvent such as acetone to give nitrile intermediates which are hydrolized to the corresponding carboxylic acids XXXV by standard methods known to one skilled in the art. The nitro carboxylic acids XXXV, when reduced by standard methods (see discussion of Equation 14), spontaneously cyclize to give the lactams XXXVI. For a discussion of this reaction when n is 0, see W. Sumpter and F. Miller, The Chemistry of Hetero- cyclic Compounds, Vol. 8, Inter science Publishers, Inc., New York, 1954, p. 134-135, and references cited therein. For a discussion of this reaction when n is 1, see G. Jones1 The Chemistry of Heterocyclic Compounds, Vol. 32, John Wiley and Sons, New York, 1977, p. 216-217, and references cited therein. The nitro lactams XVi are prepared from lactams XXXVI by the nitration, alkylation sequence described earlier for the preparation of nitro sultams XVg in Equation 25. Alternatively, lactams XXXVI of Equation 30 can be prepared from the substituted anilines XXIX of Equation 26, as shown in Equation 31. R1 and n are as previously defined. Equation 31 EMI41.1 The substituted anilines XXVII are reacted with either a chloroacetyl chloride (n = 0) or ss-chloropro- pionyl chloride (n ^ 1, R5 r H) in the presence of an acid scavenger to give the chloro amides XXXVI I. The amides XXXVI I are cyclized by heating in the presence of a suitable Friedel-Crafts reagent such as AlCl3 (see discussion of Equation 24) to give the lactams XXXVI. The method of Equation 31 has been widely used for the preparation of oxindoles (XXXVI, n = 0; see W. Sumpter and F. Miller, loc. cit., p. 135-136 for discussion and references) and for the preparation of 3,4-dihydro-2-quinolones (XXXVI, n = 1; see G. Jones, loc. cit., p. 164-168 for discussion and references). For a general review of oxindole chemistry see W. Sumpter and F. Miller, loc. cit., p. 134-153. As shown in Equation 32, nitro compounds of Formula XV where J is Jlo (XVj) can be prepared from the appropriately substituted phenols XXXI I. R' is Br or CH2Cl, R1, R5 and n are as previously defined. Equation 32 EMI42.1 The nitrophenols XXXI I, prepared by methods known to one skilled in the art, are reacted with potassium cyanide in a solvent such as DMF at 0 to 80C for 0.5 to 24 hours to give the cyanophenols XXXVIII. The cyano function is hydrolyzed to its corresponding carboxylic acid by methods known in the art. For n = 0, the carboxylic acids cyclize spontaneously. For n a 1, the carboxylic acid is cyclized by heating with a reagent such as thionyl chloride as taught by Wakselman et al. Tetrahedron, 30 4069 (1974) for the preparation of substituted dihydrocoumarins and 2-benzofuranones. Alternatively, as shown in Equation 33, nitro compounds of Formula XVj where n = 1 can be prepared by reducing the corresponding coumarins XVp, which are readily prepared from nitrosalicaldehydes XXXIX by heating with,for example where R3 is H, potassium acetate in acetic anhydride according to the teachings of Gqola, et al., Fort. Hare Pap., 6, 197 (1975) (Chem. Abst. 84:150452X (1975)) for the preparation of 8-nitrocoumarin (XVp, R1=H). Coumarins are well known in the literature, for a review see Comprehensive Organic Chemistry, Vol. 4, Pergamon Press 1979. Equation 33 EMI43.1 As shown in Equation 34, nitro Compounds @@ mula XV where J is J11 and n is 0 (XVk) can be prepared from the appropriately substituted nitro phenols XXXX. R6 and R7 are H, R1 is as previously defined. Equation 34 EMI44.1 This method is parrallel to that previously discussed for the preparation of Formula XVj in Equation 32. The 2-benzofuranones XVk, where R6 and/or R7 are other than hydrogen, can be prepared from the 2-benzo futanones XVk where R6 and/or R7 are hydrogen by standard alkylation methods known in the art. For a review see: H. House, Modern Synthetic Reactions, 2nd Edition, W. A. Benjamin, Inc., Menlo Park, California 1972, p. 542-570. As shown in Equation 35, nitro compounds of Formula XV where J is Jll and n is 1 (XV1) can be prepared from the appropriately substituted nitrophenylacetic acids XXXXI. R1, R6 and R7 are as previously defined. Equation 35 EMI44.2 The nitrophenylacetic acids, prepared by methods known to one skilled in the art, are treated with formaldehyde in the presence of a strong acid such as HC1 in a solvent such as acetic acid at 25 to 1000C for 2 to 48 hours. This method has been used to prepare substituted benzo[c]pyran-3-ones, see U.S. Patent 3,480,634 (Chem. Abst. 72:43486s (1970)). Alternatively, as shown in Equation 36, benzo [c]pyran-3-ones XV1 can be prepared from the appropriately substituted nitrotoluic acids XXXXII. R6 and R7 are H, R1 is as previously defined. Equation 36 EMI45.1 The nitrotoluic acids, prepared by methods known to one skilled in the art, are heated with dimethyl formamide dimethylacetal in DMF to produce, in part, the nitroisocoumarins XXXXIII. The isocoumarins are reduced by lithium aluminum hydride to give a hemiacetal which is then separated and oxidized with pyridinium chlorochromate (PCC) to give the desired benzo [c]pyran-3-ones. This is the method taught by Somei and Shoda, Heterocycles, 17, 417 (1982) for the pre: paration of 1,4-dihydro-5-nitrobenzo[c]pyran-3-one tXVl, R1, R6 and R7 " H). The benzo[cipyran-3-ones XV1 where R6 and/or R7 are other than hydrogen can be prepared by the standard alkylation methods discussed for Equation 34. Additionally, benzo[clpyran-3-ones XV1, where R1 is other than SCH3, can be prepared by the Baeyer-Villiger oxidation of 2-indanones XVm (n = 0) (vide infra). The Baeyer-Villiger oxidation of ketones to esters is well known in the literature, for a review see: Organic Reactions, Vol. 9, John Wiley and Sons, New York, 1957, p. 73 to 107. For application of this reaction to 2-indanones see G. Swan J. Chem. Soc., 1720 (1949). As shown in Equation 37, nitro compounds of Formula XV, where J is-J12 (XVm) , can be prepared from the appropriately substituted indenes and dihydronaphthalenes of Formula XXXXIV. R7 is H, R1, R6 and n are as previously defined. Equation 37 EMI46.1 The nitroolefins XXXXIV can be converted to their corresponding epoxides XXXXV by either direct oxidation with a per acid such as m-chloroperbenzoic acid or via hydrobromination followed by treatment with a base as known to one skilled in the art. The epoxides XXXXV are rearranged to the desired 2-indanones (XVm, n = O) or tetralones (XVm, n = 1) by reaction with either a protonic acid such as sulfuric acid as taught by Rosen et al., 3. Org. Chem., 29, 1723 (1964) or a Lewis Acid such as BF3-etherate as taught by Bondinell and Pendleton, U.S. Patent 4,192,888 (1980). The starting nitroindenes (XXXXIV, n = 0) and nitrodihydronaphthalenes (XXXXIV, n = 1) are well known in the literature and can be prepared by methods known to one skilled in the art. Alternatively, as shown in Equation 38, 2-tetralones of Formula XVm (n = 1) can be prepared from the appropriately substituted nitrophenylacetic acids XXXXI discussed previously in Equation 35 by reaction with ethylene under Friedel-Crafts conditions. For a review of this and alternate syntheses of 2-tetralones see Shner and Przhiyaglovskaya, Russian Chemical Reviews, 35, 523 (1966). Equation 38 EMI47.1 Additionallis, the 2-indanones (XVm, n = 0) and 2-tetralones (XVm, n = 1) can be prepared from the corresponding l-indanones (XVf, n - 0) and l-tetralones (XVf, n - 1), respectively, via a 1,2-carbonyl transposition, as shown in Equation 39. R1, R6 and n are as previously defined. Equation 39 EMI48.1 1,2-Carbonyl transpositions are well known in the literature and can be performed by a wide variety of methods, for a recent review, see: D. G. Morris, Chem. Soc. Reviews, II, 397-434 (1983). For application of this method to indanones, see U.S. Patent 4,192,888. For application of the method to tetralones, see Shner and Przhiyaglovskaya loc. cit. As shown in Equation 40, nitro compounds of Formula XV, where J is J22 (XVn), can be prepared from the appropriately substituted nitrophenols XXXXVI. R1, R3, R4 and n are as previously defined. Equation 40 EMI48.2 The reaction of the nitrophenol XXXXVI with the halo-acid salts produces the nitro ethers XXXXVII which are subsequently cyclized, in part, to give XVn (R3, RaH) by heating the acid with a suitable condensing agent such as polyphosphoric acid, hydrofluoric acid, sulfuric acid or stannic chloride, or the acid may be converted to its chloride and heated with a typical Fri.ed.el-Grafts reagent such as aluminum chloride or stannic chloride. The ketones of Formula.XVn where R3 and/or R4 are other than hydrogen can be prepared from ketones XVn where R3 and/or R4 are hydrogen by standard ketone alkylation and halogenation methods as described previously for compounds of Equation 24. Alternatively, as shown in Equation 41, compounds of Formula XVn where n = 0 can be prepared from nitrobenzoates of Formula XXXXVIII. R1, R3 and R4 are as previously defined. Equation 41 EMI49.1 The phenol XXXXVIII is first alkylated with ethyl chloroacetate in the presence of an acid scavenger followed by reaction with a base to effect cyclization to the ketoester XXXXIX. The ketoester is then saponafied and decarboxylated by heating with acid to give the 3-ketobenzofurans XVn (n = 0). 3-Ketobenzofurans are well known in the art, for a review of their synthesis and chemistry see Chemistry of Heterocyclic Compounds, Vol. 29, Interscience Publishers, Inc., New York, 1974, p. 210-296. Benzopyran-4-ones are also well known in the art, for a review see Chemistry of Beterocyclic Compounds, Vol. 31, Interscience Publishers, Inc., New York, 1977. For a review of the synthesis and chemistry of benzoxepin-5-ones see Chemistry of Heterocyclic Compounds, Vol. 26, Interscience Publishers, Inc., New York, 1972. The nitro compounds of Formula XV in Equation 14, where J is J13, J14, J15' J16t J17' 318' Jl9' 520' J21 or J23 can be prepared from the nitro compounds of Formula XV where J is J1, J2 J3' J4 (J24), J5, J7' JS, Jg, J10 or J22' respectively, (n = 1) by the bromination/dehydrobromination sequence described above for sulfonamides IV in Equation 9. Alternately, nitro compounds of Formula XV in Equation 14 where J is J15 can be prepared from nitro compounds of Formula XV where J is J16 by treatment with the appropriate amines R2NH2 as taught by J. Jones and A. Pinder, J. Chem. 'Soc., 2612 (1958). Additionally, the nitro compounds of Formula XV where J is J21 can be prepared as discussed in Equation 33. The nitro compounds of Formula XV in Equation 14 where J is J18 can also be prepared from ketones XXXI by base treatment of its tosylhydrazone derivative as taught by B. Loev, et al., J. Org. Chem., 31, 3531 (1966). The preparation of compounds of Formula I where J is J1 to J12 and J22 and n=2 can be prepared using the procedures outlined above for the analogous compounds where nal. The amines of Formula III in Equations 1 and 4 are also important intermediates for the preparation of the compounds of this invention and are described below. The pyrimidines and triazines of Formula (lIla) to (IIId) below are either known or can be prepared by obvious methods by one skilled in the art. EMI51.1 For a review of the synthesis and reactions of 2-aminopyrimidines (lIla, Z=CR') see The Chemistry of Heterocyclic Compounds, Vol. 16, John Wiley and Sons, New York (1962). For a review of the synthesis and reactions of 2-amino-s-triazines (IIIa, Z=N) see The Chemistry of Heterocyclic Compounds, Vol. 13, John Wiley, New York (1959), F. C. Schaefer, U.S. Patent 3,154,547 and F. C. Schaefer and K. R. Huffman, 3. Org. Chem., 28, 1812 (1963). The synthesis of the bicyclic.amines IIIb and IIIc is taught in. our EP-A-15,683. The synthesis of bicyclic amines IIId is taught in our EP-A-46,677. The amines of Formula III where X is OCF2H, OCH2F, OCF3 or CF3; or X1 is OCF2H and/or Y is OCH2F, OCF3, SCH2F, SCF3 or GCF2T wherein G is O or S and T is H, CHC1F, CHBrF or CHFCF3 can be prepared by methods taught in South African Patent Application 825,045, or by suitable modifications that would be obvious to one skilled in the art. The pyrimidines of Formula IIIa (Z=CH) where Y is -CR6(OCH3)2 -CR6(OCH2CH3)2, EMI52.1 EMI52.2 can be prepared according to the methods taught in our EP-A-84,224 or suitable modifications thereof known to one skilled in the art. The triazine amines of Formula IIIe where X3 is CH3 or OCH3 and R is H or CH3 can be prepared according to the teachings of U.S. Serial No. 472,879, filed March 14, 1983(6-B-A-606,714). EMI52.3 Preparations of 3-amino-1,2,4-triazoles of Formula (IIlf) are known in the art and 1,2,4-triazoles are reviewed in The Chemistry of Heterocyclic Compounds "Triazoles 1,2,4" (John Wiley and Sons, New York, 1981). Commonly used starting materials containing nitrogen are N-aminoguanidine, hydrazine, alkylhydrazines, cyanamide, ethyl cyanoacetimidate, dimethyl cyanodithioimidocarbonate, dimethyl cyanoimidocarbonate, ethoxymethylenecyanamide, and acylhydrazines. Some literature synthesis are illustrated below. Using these techniques or suitable modifications that would be apparent to one skilled in the art, the 3-amino-1,2,4-triazole intermediates can be readily prepared. Heating equimolar amounts of ethyl propionimidate hydrochloride and N-aminoguanidine nitrate in pyridine gives 3-amino-5-ethyltriazole; German Patent 1,073,499 (1960); Berichte, 96, 1064 (1963). EMI53.1 Condensation of hydrazine with ethyl N-cyanoacetimidate yields 3-amino-5-methyltriazole; Journal of Organic Chemistry, 28, 1816 (1963). EMI53.2 U.S. Patent 2,835,581 (1958) teaches the preparation of 3-amino-S- (hydroxymethyl) triazole from N-aminoguanidine and glycolic acid and British Patent 736,568 (1955) describes the synthesis of 3-amino-5-mercaptotriazole. EMI54.1 Condensing hydrazine with dimethyl cyanodithioimidocarbonate in acetonitrile gives 3-amino-5-methylthio1,2,4-triazole while reaction of hydrazine with dimethyl N-cyanoimidocarbonate produces 3-amino-5-methoxy-1.,2,4-triazole; Journal of Organic Chemistry, 39, 1522 (1974). EMI54.2 Reaction of substituted hydrazines with N-cyanothioimidocarbonates (prepared according to the procedure given in D. M. Wieland, Ph.D. Thesis, 1971, pp. 123-124) yields disubstituted aminotriazoles as shown below. EMI55.1 Many of the aminoheterocyclic intermediates of Formula (III) where R is methyl may be prepared by a two-step procedure as described for IIIi in Equation 42. X, Y and Z are as previously defined. Equation 42 EMI55.2 A solution of the amine L in concentrated hydrochloric acid is treated with sodium nitrite solution and the chloro compound LI is isolated in the usual manner by filtration of the acidic solution. A representative procedure is described by Bee and Rose in J. Chem. Soc. C, 2031 (1966), for the case in which Z = CH, and X = Y r OCH3. Displacement of the chlorine of LI may be accomplished by heating with an ex cess of methylamine in water to obtain the methylamino heterocycle (IlIg). Agriculturally suitable salts of compounds of Formula I are also useful herbicides and can be prepared in a number of ways known to the art. For example, metal salts can be made by contacting compounds of Formula I with a solution of an alkali or alkaline earth metal salt having a sufficiently basic anion (e.g., hydroxide, alkoxide, carbonate or hydride). Quaternary amine salts can be made by similar techniques. Salts of compounds of Formula I can also be prepared by exchange of one cation for another. Cationic exchange can be effected by direct contacting of an aqueous solution of a salt of a compound of Formula I (e.g., alkali metal or quaternary amine salt) with a solution containing the cation to be exchanged. This method is most effective when the desired salt containing the exchanged cation is insoluble in water, e.g., a copper salt, and can be separated by filtration. Exchange may also be effected by passing an aqueous solution of a salt of a compound of Formula I (e.g., an alkali metal or quaternary amine salt) through a column packed with a cation exchange resin containing the cation to be exchanged. In this method, the cation of the resin is exchanged for that of the original salt and the desired product is eluted from the column. This method is particularly useful when the desired salt is water-soluble, e.g., a potassium, sodium or calcium salt. Acid addition salts, useful in this invention, can be obtained by reacting a compound of Formula I with a suitable acid, e.g., p-toluenesulfonic acid, trichloroacetic acid or the like. Example 1 2-t-Butyl-3-hydroxy-7-chloro-2,3-dShydro-1,2-benz- isothiazole-l ,l-dioxide To a solution of 49.5 g of N-t-butyl-2-chlorobenzenesulfonamide in 875 mls of dry THF was added 262 ml of a 1.6M hexane solution of n-butyl lithium at -200 to -5 C under an inert atmosphere. The mixture was stirred at 0 C for 1 hour, room temperature for 2 hours, -recooled to -780C and contacted with 38 mls of dry dimethylformamide. The mixture was allowed to warm to room temperature overnight, poured into water, acidified to a ph of ¯3 and ether extracted. The extract was washed with water and brine, dried over MgSO4 and concentrated to give a yellow oil. The oil was dissolved in 50% ether in hexane solution and allowed to stand, giving, after filtration, 38 g of the title compound as colorless crystals, m.p. 139-1410C. 90MHz NMR (CDCl3)# : 7.7-7.2 (m, 3H, arom); 5.9 (br. d, J = 11Hz, 1H, CH or OH); 4.2 (br. d, J = 11Hz, 1H, OH or CH); and 1.5 (s, 9H, CH3's). IR (nujol) 3440 cm-1 Example 2 7-Chloro-1,2-benzisothiazole-1,1-dioxide - -A solution of -37 g of 2-t-butyl-3-hydroxy-7- chloro-2,3-dihydro-1,2-benzisothiazole-1,1-dioxide and 0.2 g of tosic acid in 370 mls of benzene was refluxed through a Dean-Stark water separator for 16 hours, cooled in ice and filtered to give 18.9 g of the title compound as colorless crystals, m.p. 162-1640C. 90MHz NMR (CDC13)o: 9.15 (s, 1H, CH); and 8.0-7.7 (m, 3H, arom) IR (nujol) 1445, 1320, 1170 cm-l Example 3 7-Chloro-2,3-dihydro-2-benzisothiazole-1,1-dioxide A suspension of 17.9 g of 7-chloro-1,2-benziso thiazole-1,1-dioxide in 180 ml of absolute ethanol was cooled to 0 C and treated with 3.33 g of sodium borohydride at such a rate that the temperature remained below 5 C. The mixture was warmed to room temperature for 30 minutes, recooled to 0 C and treated with glacial acetic acid to destroy excess hydride. The mixture was concentrated to dryness, the resulting solid suspended in water, filtered, washed with water and dried in vacuo at 500C for 16 hours to give 17.6 g of the title compound as a white powder, m.p. 159-1610C. 90MHz NMR (CDC13/DMSO)6: 7.9-7.2 (m, 3H, arom); 6.9 (br, 1H, NH); and 4.4 (s, 2H, CH2). IR (nujol) 3220 cm-1 Example 4 2-Methyl-7-chloro-2,3-dihydro-1,2-benzisothiazole l,l-dioxide A solution of 16.6 g of 7-chloro-2,3-dihydro-1,2benzisothiazole-l,l-dioxide in 85 mls of dry dimethylformamide was cooled and treated with 10 g of potassium t-butoxide at such a rate that the temperature remained Delow 60C. The resulting suspension was stirred at 50 to 100C for 30 minutes, treated with 6.1 mls of methyl iodide at 100 to 150C and stirred at room temperature for 16 hours. The mixture was poured into ice water and the resulting solid was filtered, washed with water and dried in vacuo at 50 C for 1.5 hours to give 15.4 g of the title compound as a pinkish solid, m.p. 95-970C. 90MHz NMR (CDCl3) #: 7.8-7.2 (m, 3H, arom); 4.4 (s, 2H, CH2); and 3.0 (s, 3H, CH3). IR (nujol) 1460, 1300, 1165, 1152 cm-1 Example 5 2-Methyl-7- (phenylmethylthio)-2,3-dihydro-l,2-benz- isothiazole-l,l-dioxide To a solution of 12 g of potassium-t-butoxide in 100 ml of dry dimethylformamide was added 12.9 mls of benzyl mercaptan at -5 to 0 C under an inert atmosphere followed by 12.2 g of 2-methyl-7-chloro-2,3dihydro-1,2-benzisothiazole-1,1-dioxide. The mixture was stirred at room temperature for 16 hours and poured into water to give a gummy solid. The water was decanted and extracted with ethyl acetate. The gummy solid was slurried in ethyl acetate and filtered to give 5.9 g of the title compound as a light orange solid, m.p. 119-1220C. The combined ethyl acetate extract and filtrate were washed with water and brine, dried over Mg 504 and concentrated to a solid which was slurried in ether and filtered to give an additional 7.6 g of product, m.p. 121-1240C. Total yield was 13.5 g. 90MHz NMR (CDC13)6: 7.5-7.3 (m, 8H, arom); 4.3 (br. s, 4H, CH2's); and 2.9 (s, 3H, CH3). IR (nujol) 1455, 1290, 1155 cm-1 Example 6 2-Methyl-2,3-dihydro-1,2-benzisothiazole-7-sulfonamide l,l-dioxide To a solution of 9.8 g of 2-methyl-7-(phenyl methylthio)-2,3-dihydro-1,2-benzisothiazole-1,1-dioxide and 1.44 mls of water in 200 mls of 1,2-dichloroethane was added a solution of 12.9 mls of sulfuryl chloride in 50 mls of l,2-dichloroethane, dropwise, at 650 to 70 C. The mixture was heated at 700 to 750C for 2 hours, cooled to oom temperature and concentrated. The residue was dissolved in 100 ml of methylene chloride and added to r solution of 4.0 ml of liquified ammonia in 200 mls of methylene chloride at -78 to -40 C, The mixture was warmed to room temperature, stirred for 16 hours, concentrated and the resulting white solid was suspended in 150 mls of 1N HC1, filtered, washed with water and ether and dried in vacuo at 70C to 5.0 g of the title compound as a white powder, m.p. 195-197 C (a similar preparation had m.p. 2D3-205 C). 90MHz NMR (CDC13/DNsO)6: 8.2-7.7 (m, 3H, arom); 7.5 (b, 2H NH2); 4.4 (s, 2H, CH2); and 2.9 (s, 3H, CH3). IR (nujol) 3330, 3230 cm Example 7 N-(Butylaminocarbonyl)-2-methyl-2,3-dihydro-1,2 benzisothiazole-7-sulfonamide-l ,l-dioxide A suspension of 13.0 g of 2-methyl-2,3-dihydro 1,2-benzisothiazole-7-sulfonamide-l,1-dioxide, 11.2 ml of butyl isocyanate and 13.8 g of potassium carbonate in 200 ml of dry methyl ethyl ketone was heated at reflux for 2 hours. 13.8 g of potassium carbonate was added and heating was continued for an additional 16 hours. The mixture was cooled, the solvent was decanted from the solids, concentrated in vacuo, the residue dissolved in ethyl acetate and washed with saturated aq. NaHCO3. The aqueous wash was added to the original solids diluted with water and acidified to pH s3 with dilute SC1. The mixture was extracted with methylene chloride, the extract was washed with water and brine, dried and concentrated in vacuo leaving a solid which was slurried in ether and filtered to give 13.24 g of the title compound as a white powder, m.p. 162-164 C. 90MHz NMR (CDCl3)#: 8.4-7.5 (m, 3H, arom) ; 6.4 (b, t, 1H, NH) ; 5.8 (b, 1H, NH)s 4.4 (s, 2H, CH2); 3.1 (m, 2H, CH2); 3.0 (s, 3H, CH3); and 1.7-0.7 (m, 7H, alkyl). IR (nujol) 3350, 3240, 1680 cm-1 Example 8 N-((4,6-Dimethoxypyrimidin-2-yl)aminocarbonyl)-2 methyl-2,3-dihydro-1,2-benzisothiazole-7-sulfonamide l,l-dioxide A mixture of 13.2 g N-(butylaminocarbonyl)-2 methyl-2,3-dihydro-l,2-benzisothiazole-7-sulfonamide l,l-dioxide, 3.7 ml of butyl isocyanate and 0.1 g of DABCO was treated with 3.5 ml of phosgene at 135-1380C for 2 hours, purged with N2 and cooled to OOC depo siting a solid which was filtered under nitrogen to give 5.5 g of 2-methyl-2,3-dihydro-1,2-benzisothiazole 7-sulfonyl isocyanate-l,l-dioxide as a cream colored solid, m.p. 176-180 C, IR (nujol) 2220 cm 1. To a solution of 0.69 g of the isocyanate in 10 ml of dry methylene chloride was added 0.31 g of 2 amino-4,6-dimethoxypyrimidine. The mixture was heated to reflux for 1 minute and stirred at 250C for 16 hours. The resulting solid was filtered, washed with methylene chloride -arid ether to give 0.81 g of the title compound as a white powder, m.p. 229-231 C. 90 MHz NMR (TFA-d)# : 8.7-7.9 (m, 3H, aromatic); 6.3 (s, 1H, CH); 4.6 (s, 2H, CH2); 4.2 (s, 6H, OCH3); and 3.15 (s, 3H, CH3). IR (nujol) 1710 cm 1. Example 9 N- ((4 ,6-Dimethoxypyrimidin-2-yl) aminocarbonyl) benzo clfuran-l-one-7-sulfonamide A slurry of 0.8 g of crude phthalide-7-sulfonylisocyanate in 10 ml of dry acetonitrile was combined with 0.53 g of 2-amino-4,6-dimethoxypyrimidine and the mixture stirred at ambient temperature for 18 hours. The mixture was then diluted with 15 ml of acetonitrile, heated to a boil, filtered hot, the filtrate concentrated to 10 ml, allowed to cool, the crystals collected and washed with acetonitrile. Yield 0.69 g, m.p. 210-2150C (dec.). Recrystallization from acetonitrile improved the m.p. to 219-221 C(d). NMR (CDCl3): 4.06 (s, 6H, OCH3's); 5.40 (s, 2H, CH2); 5.84 (s, 1H, pyrimidine C5-H); 7.2 (broad s, lH, NH); 7.8-8.1 (m, 2H); 8.5 (broad d, J=8, 1S); and 13.0 (broad s, lH, NH). IR (nujol) 3430 cm 1 (NH); 1765 (lactone); and 1728, 1708 (sulfonylurea). The following compounds can be prepared according to the procedures of Examples 1-9 and Equations 1-42. Table 1a EMI63.1 W n R R1 R2 R5 X Y O O H H CH3 H CH3 CH3 O O H H CH3 H CH3 OCH3 CH 235-237 O O H H CH3 H OCH3 OCH3 CH 229-231 O O H H CH3 H Cl OCH3 O O H H CH3 H CH3 OCH3 N 210-212 O O H H CH3 H OCH3 OCH3 N 207-209 O O H H CH2CH3 H CH3 CH3 CH 215-217 O O H H CH2CH3 H CH3 OCH3 CH 221-222 O O- H H CH2CH3 H OCH3 OCH3 CH 219-221 O O H H CH2CH3 H Cl OCH3 CH 224-226 O O H H CH2CH3 H CH3 OCH3 N 169-171 O O H H CH2CH3 H OCH3 OCH3 N 180-183 o O H H CH(CH3)2 H CH3 OCH3 CH ,234-236 O O H H CH(CH3)2 H OCH3 OCH3 CH 237-239 O O H H CH(CH3)2 H CH3 CH3 O O H H CH(CH3)2 H Cl OCH3 CH 239-241 O O H H CH(CH3)2 H F OCH3 CH 221-223 O O H H CH(CH3)2 H CH3 OCH3 N 186-188 O O H H CH(CH3)2 H OCH3 OCH3 N 199-201 O O H H CH(CH3)2 H CH3 CH(OCH3)2 CH 170-175 O 0 CH3 H CH(CH3)2 H OCH3 OCH3 CH 200-204 0 O CH3 H CH(CH3)2 H OCH3 OCH3 N 192-195 O 1 H H CH3 H CH3 CH3 CH 0 1 H H CH3 H CH3 OCH3 CH Table la (continued) W n R R1 R2 R5 X Y Z m.p.( C) O 1 H H CH3 H OCH3 OCH, CH 230-235 0 1 H H CH3 H CH3 CH3 N > 215 O 1 H H CH3 H CH3 OCH3 N 0 1 H H CH3 H OCH3 OCH3 N 258-266 O 1 H H CH2CH3 H CH3 CH3 CH O 1 H H CH2CH3 H CH3 OCH3 CH O 1 H H CH2CH3 H OCH3 OCH3 CH 199-200 O 1 H H CH2CH3 H CH3 CH3 N O 1 H H CH2CH3 H CH3 OCH3 N O 1 H H CH2CH3 H OCH3 OCH3 N S O H H CH3 H OCH3 OCH3 CH S 1 H H CH3 H OCH3 OCH3 CH O O CH3 H CH3 H OCH3 OCH3 N 182-188 O O H o-F CH2 H OCH3 CCH3 CH O O H m-Cl CH3 H OCH3 OCH3 CH O O H o-Br CH3 H OCH3 OCH3 CH O O H m-CH3 CH3 H OCH3 OCH3 CH O O H o-OCH3 CH3 H OCH3 OCH3 CH O O H m-CF3 CH3 H OCH3 COH3 CH <RTI ID=64.5> O O H H CH3 H Cl OCH3 CH O O H H CH3 H CH3 CCH2CH3 CH O O H H CH3 H CH3 NH2 CH O O H H CH3 H CH3 NHCH3 CH 0 0 H H CH3 H CH3 N(CH3)2 CH O O H H CH3 H CH3 CH2CH3 CH O O H H CH3 H CH3 CF3 CH O O H H CH3 H CH3 SCH3 CH O O H H CH3 H CH3 OCH2CH=CH2 CH O O H H CH3 H CH3 OCH2O=CH CH O O H H CH3 H CH3 OCH2CF3 CH 193-195 O O H H CH3 H CH3 OCH2CH2OCH3 CH 0. 0 H H CH3 H CH3 CH(OCH3)2 CH Table la (continued) EMI65.1 <tb> <SEP> W <SEP> n <SEP> R <SEP> R1 <SEP> R2 <SEP> R5 <SEP> X <SEP> Y <SEP> Z <SEP> m.p.(OC) <tb> <SEP> 0 <SEP> 1 <SEP> H <SEP> H <SEP> CH(CH3)2 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CH <tb> <SEP> 0 <SEP> 1 <SEP> H <SEP> H <SEP> CH(CH3)2 <SEP> H <SEP> CCH3 <SEP> CH3 <SEP> CH <tb> <SEP> O <SEP> 1 <SEP> H <SEP> H <SEP> CH(CH3)2 <SEP> H <SEP> WH3 <SEP> OCH3 <SEP> CH <SEP> 211-214 <tb> <SEP> 0 <SEP> 1 <SEP> H <SEP> H <SEP> CH(CH3)2 <SEP> H <SEP> C1 <SEP> OCH3 <SEP> CH <tb> <SEP> O <SEP> 1 <SEP> H <SEP> H <SEP> ÇHtCH3)2 <SEP> H <SEP> OCH3 <SEP> CH3 <SEP> N <tb> <SEP> 0 <SEP> 1 <SEP> H <SEP> H <SEP> CH(CH3)2 <SEP> H <SEP> CCH3 <SEP> Coy3 <SEP> N <tb> <SEP> rn <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> CH, <SEP> H <SEP> CH3 <SEP> 3 <SEP> s <SEP> CH <tb> <SEP> CH3 <tb> <SEP> H <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH21XH3 <SEP> CH <SEP> 169-171 <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCH3 <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCH2CH <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CC1 <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CBr <tb> <SEP> O <SEP> 1 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH2CCH3 <SEP> CH <tb> <SEP> O <SEP> 1 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> C1 <SEP> : :H3 <SEP> CH <tb> <SEP> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH2CH2CH3 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CH <SEP> 195-198 <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> CH2CH2CH3 <SEP> H <SEP> CH3 <SEP> OCH <SEP> CH <SEP> 197-199 <tb> <SEP> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH2CH2CH3 <SEP> H <SEP> CCH3 <SEP> OCH <SEP> 3 <SEP> CH <SEP> 206-208 <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> CH2CH2CH3 <SEP> H <SEP> C1 <SEP> CCH3 <SEP> CH <SEP> 199-201 <tb> <SEP> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH2CH2CH3 <SEP> H <SEP> CH3 <SEP> 0CH3 <SEP> N <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> CH2CH223 <SEP> H <SEP> SOCH3 <SEP> OCH3 <SEP> N <SEP> 187-190 <tb> <SEP> 0 <SEP> O <SEP> H <SEP> H <SEP> H2CH2CH2CH3 <SEP> H <SEP> OCH3 <SEP> oCH3 <SEP> N <SEP> 185-187 <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> CH2CH2CH2CH3 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CH <SEP> 193-195 <tb> <SEP> 0 <SEP> .0= <SEP> H <SEP> X <SEP> GH2CH2CH2CXH3 <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> CH <SEP> 167-170 <tb> <SEP> o <SEP> o <SEP> H <SEP> H <SEP> CH2CH2CH2CH3 <SEP> H <SEP> 0cH3 <SEP> OCH3 <SEP> CH <SEP> 214-216 <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> CH2CH2CH2CH3 <SEP> H <SEP> C1 <SEP> OCH3 <SEP> CH <SEP> 195-197 <tb> <SEP> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH2CH2CH2CH3 <SEP> H <SEP> CH3 <SEP> =3 <SEP> N <SEP> 165-168 <tb> o <SEP> ;Q <SEP> Q=H <SEP> H <SEP> H <SEP> H <SEP> )I <SEP> 0CH3 <SEP> H3 <SEP> CH <tb> <SEP> 0 <SEP> o <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCH3 <SEP> OCH3 <SEP> CH <tb> <SEP> O <SEP> O <SEP> H <SEP> m-sCH3 <SEP> CH3 <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> <SEP> 0 <SEP> O <SEP> H <SEP> m-OCF2H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> COi3 <SEP> CH <tb> Table la (continued) EMI66.1 <tb> W <SEP> n <SEP> R <SEP> R1 <SEP> R2 <SEP> e <SEP> X <SEP> Y <SEP> Z <SEP> m,p. <SEP> (OC) <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> F <SEP> OCH3 <SEP> CH <SEP> 224-226 <tb> O <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> Br <SEP> 0CH3 <SEP> CH <SEP> 219-221 <tb> o <SEP> o <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CHZF <SEP> C±H3 <SEP> CH <tb> o <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> OCE2H <SEP> CH3 <SEP> CH <SEP> 228-230 <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CF3 <SEP> SOCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH2CH2CH3 <SEP> H <SEP> OCF91 <SEP> C3 <SEP> CH <SEP> 185-1S9 <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> CH2CH2CH3 <SEP> H <SEP> OCF3H <SEP> OCF2H <SEP> CH <SEP> 207-210 <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH2CH2CH3 <SEP> H <SEP> Br <SEP> OCH3 <SEP> CH <SEP> 190-192 <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH(CH3)CH2CH3 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH(CH3)CH3 <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> CH <tb> o <SEP> 0 <SEP> H <SEP> H <SEP> CH(CH3)CH2CH3 <SEP> H <SEP> CCH3 <SEP> OCH3 <SEP> CH <SEP> 220-222 <tb> o <SEP> o <SEP> H <SEP> H <SEP> CH(CH3)CH2CH3 <SEP> H <SEP> C1 <SEP> OCH3 <SEP> CH <SEP> 221-224 <tb> o <SEP> o <SEP> H <SEP> H <SEP> CH(CH3)CH2CH3 <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> N <SEP> 151-153 <tb> o <SEP> O <SEP> H <SEP> H <SEP> CH(CH3)CH2CH3 <SEP> H <SEP> SOCH3 <SEP> 3 <SEP> N <SEP> 139-142 <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH <tb> <SEP> CH3 <tb> <SEP> CH3 <tb> o <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> O <SEP> O <SEP> CH <tb> <SEP> X <tb> 0 <SEP> o <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> H <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CN <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH(OCH2CH3)2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CCH2 <SEP> CH <tb> o <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> OCF3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CCH2F <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> SCF3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CCF2H <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> OCF2CHClF <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> OCF2CHBrF <SEP> CH <tb> Table la (continued) W n R R1 R2 R5 X Y Z m.p.( C) O O H H CH3 H CH3 OCF2CHFCF3 CH O O H H CH3 H CH3 SCF2H CH O O H H CH3 H CH3 SCF2CHClF CH O O H H CH3 H CH3 SCF2CHBrF CH O O H H CH3 H CH3 SCF2CHFCF3 CH 0 2 H H CH3 H CH3 CH3 CH 0 2 H H CH3 H CH3 OCH3 CH O 2 H H CH3 H OCH3 OCH3 CH O 2 H H CH3 H Cl OCH3 CH 0 2 H H CH3 H CH3 OCH3 N 0 2 H H CH3 H 0CH3 OCH3 N O 0 CH3 H CH3 H OCH3 OCH3 CH 192-194 O O H H CH3 H OCH3 CH(OCH3)2 CH 167-168 O O H H CH3 H OCH2CH3 CH3 CH O O H H CH3 H OCH3 N3 CH Table 2a EMI68.1 W n R R1 R5 X Y Z m.p.( C) O O H H H CH3 CH3 CH O O H H H CH3 OCH3 CH OO H H H OCH3 OCH3 CH O O H H H CH3 CH3 N O O H H H CH3 OCH3 N O O H H H OCH3 OCH3 N O 1 H H H CH3 CH3 CH O 1 H H H CH3 OCH3 CH O 1 H H H OCH3 OCH3 CH O 1 H H H CH3 CH3 N O 1 H H H CH3 OCH3 N O 1 H H H OCH3 OCH3 N S O H H H OCH3 OCH3 CH S 1 H H H OCH3 OCH3 CH O O CH3 H H OCH3 OCH3 N O O H O-F H OCH3 OCH3 CH O O H m-Cl H OCH3 OCH3 CH O O H o-Br H OCH3 OCH3 CH O O H m-CH3 H OCH3 OCH3 CH O O H o-OCH3 H OCH3 OCH3 CH 0 O H m-CF3 H OCH3 OCH3 CH 0 0 H H H Cl OCH3 CH 0 O H H H CH3 OCH2CH3 CH Table 2a (continued) EMI69.1 <tb> W <SEP> fl <SEP> R <SEP> R1 <SEP> R5 <SEP> X <SEP> Y <SEP> Z <SEP> m.p.(OC) <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> NH2 <SEP> CH <tb> OOH <SEP> H <SEP> H <SEP> CH3 <SEP> NHCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> N(CH3)2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH2CH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CF3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH=CH2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2C'CH <SEP> CH <tb> O <SEP> Q <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CF3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> oCH2CH2 <SEP> OCH3 <SEP> CH <tb> OOH <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCH3)2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CC,O <SEP> CH <tb> <SEP> sCH3 <tb> OOHH <SEP> H <SEP> CH3 <SEP> CH2OCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCH3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCH2CH3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CC1 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CBr <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> B <SEP> CH3 <SEP> CH2OCH3 <SEP> CH <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> H <SEP> C1 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> m-SCH3 <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> m-OCF2H <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> F <SEP> OCH3 <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> CH2F <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> OCF <SEP> H <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> OCF3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CF3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0HH <SEP> H <SEP> CH3 <SEP> O <SEP> O <SEP> CH <tb> <SEP> HX <tb> Table 2a (continued) EMI70.1 <tb> W <SEP> n <SEP> R <SEP> 1 <SEP> R5 <SEP> X <SEP> Y <SEP> Z <SEP> m,p. <SEP> (OC) <tb> O <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> Br <SEP> OCH3 <SEP> CH <tb> <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> 3 <SEP> O <SEP> O <SEP> CH <tb> <SEP> 0 <SEP> 0 <tb> o <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH <tb> o <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CN <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCH2CH3)2 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2F <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCR2F <SEP> CR <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF3 <SEP> CR <tb> j0 <SEP> H <SEP> H <SEP> H <SEP> -H <SEP> CH3 <SEP> OCF2H <SEP> CR <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHC1F <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHBrF <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHFCF3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2H <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHC1F <SEP> CR <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHBrF <SEP> CR <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CRFCF3 <SEP> CH <tb> O <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CH <tb> O <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> CH <tb> O <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> O <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> C1 <SEP> OCH3 <SEP> CH <tb> e <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> N <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> N <tb> Table 3a EMI71.1 W n R R1 R2 R5 X Y Z m.p.( C) O O H H CH3 H CH3 CH3 CH 215-216 O O H H CH3 H CH3 OCH3 CH 215-217 O O H H CH3 H OCH3 OCH3 CH 202-204 O O H H CH3 H Cl OCH3 CH 211-213 O O H H CH3 H CH3 OCH3 N 192-193 O O H H CH3 H OCH3 OCH3 N 198-200 O O H H CH(CH3)2 H CH3 CH3 CH 150-153 O O H H CH(CH3)2 H CH3 OCH3 CH 195-197 O O H H CH(CH3)2 H OCH3 OCH3 CH 199-203 O O H H CH(CH3)2 H Cl OCH3 CH 180-183 O O H H CH(CH3)2 H CH3 OCH3 N 181-183 O O H H CH(CH3)2 H OCH3 OCH3 N 203-206 O O H H CH2CH3 H CH3 OCH3 CH O O H H CH2CH3 H OCH3 OCH3 CH 0 1 H H CH3 H CH3 CH3 CH 0 1 H H CH3 H CH3 OCH3 CH 0 1 H H CH3 H OCH3 OCH3 CH 0 1 H H CH3 H CH3 CH3 N 0 1 H H CH3 H CH3 OCH3 N 0 1 H H CH3 H OCH3 OCH3 N O 1 H H CH2CH3 H CH3 CH3 CH O 1 H H CH2CH3 H CH3 OCH3 CH O 1 H H CH2CH3 H OCH3 OCH3 CH O 1 H H CH2CH3 H CH3 CH3 N Table 3a (continued) EMI72.1 <tb> WnR <SEP> R1 <SEP> 2 <SEP> 2z <SEP> X <SEP> Y <SEP> Z <SEP> m.p.(0C) <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> CR2CH3 <SEP> H <SEP> CH3 <SEP> OCH3 <tb> OlR <SEP> H <SEP> CH2CH3 <SEP> H <SEP> nrq3 <SEP> 0CH3 <SEP> N <tb> SOH <SEP> H <SEP> CH3 <SEP> H <SEP> Q:H3 <SEP> OCH3 <SEP> CH <tb> SIR <SEP> H <SEP> 3 <SEP> H <SEP> CCR3 <SEP> 0CR3 <SEP> CH <tb> O <SEP> O <SEP> CH3 <SEP> H <SEP> CH3 <SEP> H <SEP> CCR3 <SEP> OCH3 <SEP> N <tb> O <SEP> O <SEP> H <SEP> o-F <SEP> CH3 <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> m-Cl <SEP> CH3 <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> O <SEP> 0 <SEP> H <SEP> o-8r <SEP> CH3 <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> mrCH3 <SEP> CH3 <SEP> H <SEP> C{3 <SEP> OCR3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> o-OCH3 <SEP> CH3 <SEP> H <SEP> OCR <SEP> OCR3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> m-CF3 <SEP> CH3 <SEP> H <SEP> 3 <SEP> (CR3 <SEP> CK <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> C1 <SEP> (CR3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CCH2CH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> NH2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> NHCH3 <SEP> CH <tb> OO'H <SEP> H <SEP> CH3 <SEP> H <SEP> .CH3 <SEP> N(CH3) <SEP> CR <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CR2CR3 <SEP> CH <tb> OOH <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> (r3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> . <SEP> CH3 <SEP> H <SEP> CH3 <SEP> 92g3 <SEP> CH <tb> OOH <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CCH2CH=CH2 <SEP> CR <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CCH2CCH <SEP> 'CH <tb> OOH <SEP> H <SEP> CH3 <SEP> H <SEP> CE3 <SEP> OSH2CF3 <SEP> CH <tb> O <SEP> C <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> 0CHi <SEP> H20CH3 <SEP> CH <tb> 3 <SEP> E' <SEP> Cur3 <SEP> H <SEP> CH3 <SEP> CH(OCH3)2 <SEP> CH <tb> OCH <SEP> H <SEP> CH3 <SEP> ' <SEP> H <SEP> CH3 <SEP> O <SEP> CH <tb> <SEP> 3 <SEP> C/ <tb> O <SEP> O <SEP> H <SEP> E <SEP> CH3 <SEP> H <SEP> CH3 <SEP> C <SEP> hOCK3 <SEP> CR <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> (CR3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCH <SEP> p <SEP> 3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCI <tb> O <SEP> O <SEP> H <SEP> H <SEP> CR3 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CBr <tb> Table 3a (continued) EMI73.1 <tb> W <SEP> n <SEP> R <SEP> 1 <SEP> R2 <SEP> R5 <SEP> X <SEP> Y <SEP> Z <SEP> ( C) <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> Cur3 <SEP> CH20z3 <SEP> CR <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> C1 <SEP> CH3 <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> CR2CH2CR3 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CH <tb> OOHH <SEP> CH2CH2CH3 <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH2CH2CH3 <SEP> H <SEP> OCR3 <SEP> CCH3 <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> CH2CH2CH3 <SEP> H <SEP> C1 <SEP> 0CH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH2CH2CH3 <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> N <tb> OOHH <SEP> CH2CH2CH3 <SEP> H <SEP> 0CR3' <SEP> OCH3 <SEP> N <tb> OOHR <SEP> O <SEP> H <SEP> H <SEP> CH2CH2CH2CH3 <SEP> CR <SEP> H <SEP> OCR3 <SEP> OCH3 <SEP> N <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SOCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> (033 <SEP> (033 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> C1 <SEP> (033 <SEP> CH <tb> OOHH <SEP> H <SEP> H <SEP> CH3 <SEP> (033 <SEP> N <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> (033 <SEP> (033 <SEP> N <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CE <SEP> H3 <SEP> (033 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> nwS:H3 <SEP> CH3 <SEP> H <SEP> (033 <SEP> CI: :H3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> m < 2H <SEP> CH3 <SEP> H <SEP> (033 <SEP> CCH3 <SEP> CH <tb> OOHH <SEP> CH3 <SEP> H <SEP> F <SEP> (033 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> Br <SEP> (033 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH2F <SEP> (033 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> OCF2H <SEP> (033 <SEP> CH <tb> o <SEP> o <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> Ca'3 <SEP> a:H3 <SEP> CH <tb> 0 <SEP> o <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CF3 <SEP> (033 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> X <SEP> CH <tb> <SEP> IXC <tb> <SEP> CH3 <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> CH; <SEP> H <SEP> CH3 <SEP> CR <tb> <SEP> 3 <tb> Table 31 (continued) W n R R1 p2 R5 X Y Z m.p. ( C) O O H H CH3 H CH3 H CR O O H H CH3 H CH3 CN CH O O H H CH3 H CH3 CH(OCH2CH3)2 CH O O H H CH3 H CH3 OCH2F CH O O H H CH3 H CH3 OCF3 CH O O H H CH3 H CH3 SCH2F CH O O H H CH3 H CH3 SCF3 CH O O H H CH3 H CH3 OCF2H CH O O H H CH3 H CH3 OCF2CHClF CH O O H H CH3 H CH3 OCF2CHBrF CH O O H H CH3 H CH3 OCF2CHFCF3 CH O O H H CH3 H CH3 SCF2H CH O O H H CH3 H CH3 SCF2CHClF CH O O H H CH3 H CH3 SCF2CHBrF CH O O H H CH3 H CH3 SCF2CHFCF3 CH O 2 H H CH3 H CH3 CH3 CH O 2 H H CH3 H CH3 OCH3 CH O 2 H H CH3 H OCH3 OCH3 CH O 2 H H CH3 H Cl OCH3 CH O 2 H H CH3 H CH3 OCH3 N O 2 H H CH3 H OCH3 OCH3 N Table 4a EMI75.1 W n F R1 R5 X Y Z m.p.( C) O O H H H CH3 CH3 CH 185-200 O O H H H CH3 OCH3 CH 209-211 O O H H H OCH3 OCH3 CH 219-221 O O H H H CH3 CH3 N O O H H H CH3 OCH3 N 194-196 O O H H H OCH3 OCH3 N O 1 H H H CH3 CH3 CH 218-220 O 1 H H H CH3 OCH3 CH 219-222 O 1 H H H OCH3 OCH3 CH 210-214 O 1 H H H CH3 CH3 N 202-204 O 1 H H H CH3 OCH3 N 190-197 O 1 H H H OCH3 OCH3 N 204-207 S O H H H OCH3 OCH3 CH S 1 H H H OCH3 OCH3 CH O O CH3 H H OCH3 OCH3 N 198-220 O O@ H o-F H OCH3 OCH3 CH O O H m-Cl H OCH3 OCH3 CH O O H o-Br H OCH3 OCH3 CH O O H m-CH3 H OCH3 OCH CH 0 O H o-OCH3 H OCH3 OCH3 CH O O H m-CF3 H OCH3 OCH3 CH O O H H H Cl OCH3 CH 210-213 0 O H H H CH3 OCH2CH3 CH Table 4a (continued) EMI76.1 <tb> W <SEP> n <SEP> R <SEP> R1 <SEP> R5 <SEP> X <SEP> Y <SEP> Z <SEP> m.p. <SEP> ( C) <tb> o <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> NH2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> NHCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> N <SEP> (CR3)2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CR <SEP> CR <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CF3 <SEP> CR <tb> OOHH <SEP> H <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> OCH3 <SEP> OCR2CH= <SEP> CR2 <SEP> C <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> OCH3 <SEP> OCH2CwCH <SEP> CR <tb> OORH <SEP> H <SEP> OCH3 <SEP> OCH2CF, <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> B <SEP> CH3 <SEP> OCH2CH2OCH3 <SEP> C <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCH3)2 <SEP> CH <SEP> 149-151 <tb> <SEP> 3 <SEP> 2 <tb> O <SEP> O <SEP> H <SEP> H <SEP> B <SEP> CH3 <SEP> Cw <SEP> CH <tb> <SEP> 3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CiI2OCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCR3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCH2CH3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCI <tb> OOHH <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CBr <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> H <SEP> C1 <SEP> OCH3 <SEP> CH <SEP> 175-182 <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> H <SEP> Br <SEP> OCH3 <SEP> CH <SEP> 182-190 <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> m-SCH3 <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> o <SEP> 0- <SEP> H <SEP> m- <SEP> OCF2R <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> OORH <SEP> H <SEP> F <SEP> OCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CR2F <SEP> OCH3 <SEP> CR <tb> 0 <SEP> 0 <SEP> 8 <SEP> H <SEP> H <SEP> CF2H <SEP> OCH3 <SEP> CR <SEP> 230 <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> OCF3 <SEP> SOCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CF3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> On <SEP> CH <tb> <SEP> H <tb> Table 4a (continued) EMI77.1 <tb> W <SEP> n <SEP> P <SEP> R1 <SEP> P5 <SEP> X <SEP> Y <SEP> Z <SEP> m.p.(0C) <tb> O <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> Br <SEP> OCH3 <SEP> CH <tb> <SEP> CH3 <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> (· <SEP> CR <tb> <SEP> o <SEP> o <SEP> Cfi <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CN <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CR(OCR2CH3)2 <SEP> CR <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2F <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCH2F <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2R <SEP> CR <SEP> 208-209 <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> oCF2CRClF <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CRBrF <SEP> CR <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHFCF3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2H <SEP> CR <tb> o <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHC1F <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHBrF <SEP> CH <tb> o <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHFCF3 <SEP> CH <tb> O <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CH <tb> O <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> CR <tb> O <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CR <tb> O <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> C1 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> N <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> OCH3 <SEP> SOCH3 <SEP> N <tb> 0 <SEP> 0 <SEP> CH3 <SEP> H <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <SEP> 230-232 <tb> o <SEP> O <SEP> H <SEP> H <SEP> H <SEP> OCH3 <SEP> CH(OCH3) <SEP> 2 <SEP> CH <SEP> 143-145 <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> OCF2H <SEP> OCF2H <SEP> CH <tb> 0 <SEP> 1 <SEP> CH3 <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> CH <SEP> 203-209 <tb> Table 5a EMI78.1 W n R R1 R5 X Y Z m.p.( C) O O H H H CH3 CH3 CH O O H H H CH3 OCH3 CH 210-212 O O H H H OCH3 OCH3 CH 232-233 O O H H H CH3 CH3 N O O H H H CH2 OCH3 N 193-195 O O H H H OCH3 OCH3 N O 1 H H H CH3 CH3 CH O 1 H H H CH3 OCH3 CH O 1 H H H OCH3 OCH3 CH O 1 H H H CH3 CH3 N O 1 H H H CH3 OCH3 N SO 1 H H H OCH3 OCH3 N S O H H H OCH3 OCH3 CH S 1 H H H OCH3 OCH3 CH O O CH3 H H OCH3 OCH3 N H OCH3 OCH3 CH O O H m-Cl H OCH3 OCH3 CH O O H o-Br H OCH3 OCH3 CH O O H m-CH3 H OCH3 OCH3 CH O O H o-OCH3 H OCH3 OCH3 CH O O H m-CF3 H OCH3 OCH3 CH O O H H H Cl OCH3 CH 218-219 O O H H H CH3 OCH2CH3 CH Table 5a (continued) EMI79.1 <tb> W <SEP> n <SEP> P <SEP> 1 <SEP> Rg <SEP> X <SEP> Y <SEP> Z <SEP> m.p.(0C) <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> NH2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> NHCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> N(CR3)2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH2CH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> - <SEP> H <SEP> CH3 <SEP> CF3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH=CH2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2C-=CH <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH <SEP> CF <SEP> CH <tb> O <SEP> o <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCR2CR2OCR3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCH3)2 <SEP> CH <tb> <SEP> 3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CSO <SEP> CH <tb> <SEP> sCH3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CR2OCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCH3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCR2CR3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CC1 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CBr <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH2OCH3 <SEP> CR <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> H <SEP> C1 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> m-SCH3 <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> m-OCF2H <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> F <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH2F <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> OCF2H <SEP> OCH3 <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> OCF3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CF3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> Q <SEP> CH <tb> <SEP> H <tb> Table 5a (continued) EMI80.1 <tb> W <SEP> n <SEP> R <SEP> R1 <SEP> R. <SEP> x <SEP> Y <SEP> Z <SEP> ¯¯¯¯¯¯¯ <tb> ¯ <SEP> ¯ <SEP> X <SEP> Y <SEP> Z <SEP> ¯ <SEP> ¯ <SEP> ¯ <tb> O <SEP> C <SEP> H <SEP> H <SEP> H <SEP> Br <SEP> OCH3 <SEP> CH <tb> <SEP> CH, <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <tb> HX <tb> O <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH <tb> O <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CN <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H3 <SEP> CH(OCH2CH3)2 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2F <SEP> CH <tb> O <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCH2F <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF3 <SEP> CH <tb> 0 <SEP> 0 <SEP> -0 <SEP> H <SEP> H <SEP> - <SEP> H <SEP> CH3 <SEP> OCF2H <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> 3 <SEP> OCF2CRClF <SEP> 2 <SEP> CH <SEP> CR <tb> o <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHBrF <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHFCF3 <SEP> CH <tb> o <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CR3 <SEP> SCF2H <SEP> CR <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHC1F <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHBrF <SEP> CH <tb> o <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CRFCF3 <SEP> CH <tb> O <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CH <tb> O <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> CH <tb> O <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> O <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> C1 <SEP> OCH3 <SEP> CH <tb> 0- <SEP> . <SEP> H <SEP> H <SEP> H <SEP> fi <SEP> CH3 <SEP> SOCH <SEP> 3 <SEP> N <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> N <tb> Table 6a EMI81.1 W n R R1 R3 R4 R5 X Y Z m.p.( C) O O H H H H H CH3 CH3 CH O O H H H H H CH3 OCH3 CH O O H H H H H OCH3 OCH3 CR O O H H H H H Cl OCH3 CH O O H H H H H CH3 OCH3 N O 0 H H H H H OCH3 OCH3 N O O H H CH3 H H CH3 CH3 CH O O H H CH3 H H CH3 OCH3 CH o O H H CH3 H H OCH3 OCH3 CH O O H H CH3 H H Cl OCH3 CH O O H H CH3 H H CH3 OCH3 N O O H H CH3 H H OCH3 OCH3 N O O H H CH3 CH3 H CH3 CH3 CH O O H H CH3 CH3 H CH3 OCH3 CH O O H H CH3 CH3 H OCH3 OCH3 CH O O H H CH3 CH3 H Cl OCH3 CH O O H H CH3 CH3 H CH3 OCH3 N O O H H CH3 CH3 H OCH3 OCH3 N O 1 H H H H H CH3 CH3 CH O 1 H H H H H CH3 OCH3 CH O 1 H H H H H OCH3 OCH3 CH O 1 H H H H H CH3 OCH3 N 0 1 H H H H H OCH3 OCH3 N Table 6a (continued) m.p. W n R R1 R3 R4 R5 X Y Z ( C) O 1 H H CH3 H H CH3 CH3 CH O 1 H H CH3 H H CH3 OCH3 CH O 1 H H CH3 H H OCH3 OCH3 CH O 1 H H CH3 H H CH3 OCH3 N O 1 H H CH3 H H OCH3 OCH3 N O 1 H H CH3 CH3 H CH3 CH3 CH O 1 H H CH3 CH3 H CH3 OCH3 CH O 1 H H CH3 CH3 H OCH3 OCH3 CH O 1 H H CH3 CH3 H CH3 OCH3 N O 1 H H CH3 CH3 H OCH3 OCH3 N S O H H H H H OCH3 OCH3 N O O CH3 H H H H OCH3 OCH3 N O O H o-F H H H OCH3 OCH3 CH O O H m-Cl H H H OCH3 OCH3 CH O O H o-Br H H H OCH3 OCH3 CH O O H m-CH3 H H H OCH3 OCH3 CH O O H o-OCH3 H H H OCH3 OCH3 CH O O H m-CF3 H H H OCH3 OCH3 CH O O H H H CH2CH3 H OCH3 OCH3 CH O O H H CH2CH2CH H H OCH3 OCH3 CH O O H H H H H CH3 CH3 N O O H H H H H CH3 OCH2CH3 CH O O H H H H H CH3 CH2OCH3 CH O 1 H H H H H CH3 CH2OCH3 CH O O H H H H H CH3 NH2 CH O O H H H H H CH3 NHCH3 CH O O H H H H H CH3 N(CH3)2 CH O O H H H H H CH3 CH2CH3 CH O O H H H H H CH3 CF3 CH Table 6a (continued) EMI83.1 <tb> W <SEP> n <SEP> P <SEP> R1 <SEP> R3 <SEP> a4 <SEP> PS <SEP> X <SEP> Y <SEP> Z <SEP> m.p.(OC) <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> 5CR3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCR2CH"CH2 <SEP> CR <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CCCR <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CCH2CF3 <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H, <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH2CH2ccH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCH3)2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CR3 <SEP> /17 <SEP> CH <tb> <SEP> 0'C-0 <tb> <SEP> / <SEP> H <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCR3 <SEP> OCR3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> OCH3 <SEP> 0CH3 <SEP> CC2H5 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> OCR3 <SEP> SOCH3 <SEP> CCI <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> OCR3 <SEP> OCR3 <SEP> CBr <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> F <SEP> H3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> Br <SEP> OCR3 <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH2F <SEP> OCH3 <SEP> CH <tb> o <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> OCF;H <SEP> OCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> OCF3 <SEP> OCR <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CF3 <SEP> OCH3 <SEP> CH <tb> OORH <SEP> H <SEP> H <SEP> H <SEP> CR3 <SEP> CR <tb> <SEP> 0 <SEP> O <SEP> CH <tb> <SEP> H <tb> <SEP> CH, <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CR3 <SEP> CH <tb> <SEP> O <SEP> O <tb> <SEP> HX <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CN <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(CCH2CH3)2 <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCHF <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> 9CH2F <SEP> CH <tb> Table 6a (continued) W n R R1 R3 R4 R5 X Y Z (m.p.( C) O O H H H H H CH3 BCF3 CH O O H H H H H CH3 OCF2H CH O O H H H H H CH3 OCF2CHClF CH O O H H H H H CH3 OCF2CHBrF CH O O H H H H H CH3 OCF2CHFCF3 CH O O H H H H H CH3 BCF2H CH O O H H H H H CH3 SCF2CHClF CH O O H H H H . H SCF2CHBrF CH O O H H H H H SCF2CHFCF3 CH O O H H H CH3 CH3 OCH3 CH O O H H H CH2CH2CH3 H OCH3 CH 0 O H H H CH2CH2CH2CH3 H OCR3 OCH3 CH O O H m-SCH3 H H H OCH3 OCH3 CH O O H o-CF2H H H H OCH3 OCH3 CH 0 2 H H H H H CH3 CH3 CH O 2 H H H H H CH3 OCH3 CH O 2 H H H H H OCH3 OCH3 CH O 2 H H H H H Cl OCH3 CH 0 2 H H H H H CH3 OCH3 N 0 2 H H H H H OCH3 OCH3 N 0 2 H H CH3 H H CH3 CH3 CH O 2 H H CH3 H H CH3 OCH3 CH O 2 H H CH3 H H OCH3 OCH3 CH O 2 H H CH3 H H Cl OCH3 CH O 2 H H CH3 H H CH3 OCH3 N O 2 H H CH3 H H OCH3 OCH3 N O O H H Cl Cl H CH3 CH3 CH 197-199 O O H H Cl Cl H CH3 OCH3 CH 198-201 O O H H Cl Cl H OCH3 OCH3 CH 154-166 O O H H Br Br H OCR3 OCH3 CH O O H H Cl Cl H OCH3 CH3 N 178-182 Table -7a EMI85.1 W n R R1 R2 R5 X Y Z m.p.( C) O O H H CH3 H CH3 CH3 CH O O H H CH3 H CH3 OCH3 CH O O H H CH3 H OCH3 OCH3 CH O O H H CH3 H Cl OCH3 CH O O H H CH3 H CH3 OCH3 N O O H H CH3 H OCH3 OCH3 N O O H H CH2CH3 H CH3 CH3 CH O O H H CH2CH3 H CH3 OCH3 CH O O H H CH2CH3 H OCH3 OCH3 CH O O H H CH2CH3 H Cl OCH3 CH O O H H CH2CH3 H CH3 OCH3 N O O H H CH2CH3 H OCH3 OCH3 N O O H H CH(CH3)2 H CH3 OCH3 CH O O H H CH(CH3)2 H OCH3 OCH3 CH O 1 H H CH3 H CH3 CH3 CH O 1 H H CH3 H CH3 OCH3 CH O 1 H H CH3 H OCH3 OCH3 CH O 1 H H CH3 H CH3 CH3 N O 1 H H CH3 H CH3 OCH3 N O 1 H H CH3 H OCH3 OCH3 N O 1 H H CH2CH3 H CH3 CH3 CH O 1 H H CH2CH3 H CH3 OCH3 CH O 1 H H CH2CH3 H OCH3 OCH3 CH 0 1 H H CH2CH3 H CH3 CH3 N Table 7a (continued) EMI86.1 <tb> n <SEP> P <SEP> R <SEP> R1 <SEP> R2 <SEP> e <SEP> X <SEP> Y <SEP> Z <SEP> m,p.(OC) <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> CR2CR3 <SEP> H <SEP> CH3 <SEP> CCR3 <SEP> N <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> CR2CR3 <SEP> H <SEP> CCH3 <SEP> OCH3 <SEP> N <tb> S <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CCR3 <SEP> OCH3 <SEP> CH <tb> S <SEP> 1 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> OCH3 <SEP> QCH3 <SEP> CH <tb> O <SEP> O <SEP> CH3 <SEP> H <SEP> CH3 <SEP> H <SEP> 3 <SEP> OCR3 <SEP> N <tb> O <SEP> O <SEP> H <SEP> o-F <SEP> CH3 <SEP> H <SEP> OCH3 <SEP> OCR3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> m-Cl <SEP> CH3 <SEP> H <SEP> SOCH3 <SEP> OCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> o-Br <SEP> CH3 <SEP> H <SEP> OCR3 <SEP> a <SEP> H3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> tCH3 <SEP> CH3 <SEP> H <SEP> OCH3 <SEP> OCR3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> HCH3 <SEP> CH3 <SEP> H <SEP> C3 <SEP> OCR3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> m-CF3 <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CE <SEP> H3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> C1 <SEP> O=H3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> OCR2CR3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> NR2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> NHCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> N <SEP> (CH3)2 <SEP> CR <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH2CH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CF3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> OCR2CR=CH <SEP> C <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CCH2C= < H <SEP> CR <tb> O <SEP> O <SEP> H <SEP> H <SEP> &num; <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CCH2CF3 <SEP> CH <tb> O <SEP> 0 <SEP> H <SEP> H <SEP> CR3 <SEP> H <SEP> CH3 <SEP> QCH2CH2CCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CR(0CR3)2 <SEP> CR <tb> <SEP> FN <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CwO <SEP> CH <tb> <SEP> Hs <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH202H3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCH3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCH2CH3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCI <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CBr <tb> Table 7a (continued) EMI87.1 <tb> W <SEP> n <SEP> R <SEP> R1 <SEP> P2 <SEP> R5 <SEP> X <SEP> Y <SEP> m <SEP> m(oCP; ; <tb> W <SEP> n <SEP> R <SEP> X <SEP> Y <SEP> z <SEP> ("c) <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH2OCH3 <SEP> CH <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> C1 <SEP> OCR3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CR2CHCR3 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH2CH2CH3 <SEP> H <SEP> CH3 <SEP> OCR3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH2CH2CH3 <SEP> H <SEP> OCR3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> CH2CH2CH3 <SEP> H <SEP> C1 <SEP> OCR3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH2CH2CH3 <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> N <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH2CH2CH3 <SEP> H <SEP> OCR3 <SEP> OCR3 <SEP> N <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH2CH2CH2CH3 <SEP> H <SEP> OCR3 <SEP> 3 <SEP> N <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CH <tb> OORR <SEP> H <SEP> H <SEP> CH3 <SEP> SOCH3 <SEP> CH <tb> <SEP> OOHH <SEP> H <SEP> H <SEP> OCH3 <SEP> OCR3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> C1 <SEP> SOCH3 <SEP> CH <tb> OORR <SEP> H <SEP> H <SEP> CH3 <SEP> OCR3 <SEP> N <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> OCH3 <SEP> OCR3 <SEP> N <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> OCH3 <SEP> SOCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> m-SCH3 <SEP> CH3 <SEP> H <SEP> CCR3 <SEP> OCR3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> < H <SEP> CH3 <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> F <SEP> OCR3 <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> Br <SEP> acH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH2 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> OCF > H <SEP> SOCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> OCF3 <SEP> OCR3 <SEP> CH <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CF3 <SEP> OCR3 <SEP> CH <tb> <SEP> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> O <SEP> O <SEP> CH <tb> <SEP> H <tb> <SEP> CH3 <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CR <tb> <SEP> H <tb> Table 7a (continued) W n R R1 R2 R5 X Y Z (m.p. ( C) 0 O H H CH3 H CH3 H CH O O H H CH3 H CH3 CN CH O O H H CH3 H CH3 CH(OCH2CH3)2 CH O O H H CH3 H CH3 OCH2F CH O O H H CH3 H CH3 OCF3 CH O O H H CH3 H CH3 SCH2F CH O O H H CH3 H CH3 SCF3 CH O O H H CH3 H CH3 OCF2H CH O O H H CH3 H CH3 OCF2CHClF CH O O H H CH3 H CH3 OCF2CHBrF CH O O H H CH3 H CH3 OCF2CHFCF3 CH O O H H CH3 H CH3 SCF2H CH O O H H CH3 H CH3 SCF2CHClF CH O O H H CH3 H CH3 SCF2CHBrF CH O O H H CH3 H CH3 SCF2CHRCF3 CH O 2 H H CH3 H CH3 CH3 CH O 2 H H CH3 H CH3 OCH3 CH O 2 H H CH3 H OCH3 OCH3 CH O 2 H H CH3 H Cl OCH3 CH O 2 H H CH3 H CH3 OCH3 N O 2 H H CH3 B OCH3 OCH3 N Table 8a EMI89.1 W n R R1 R5 X Y Z (m.p.( C) O O H H H CH3 CH3 CH O O H H H CH3 OCH3 CH O O H H H OCH3 OCH3 CH 0 O H H H CH3 CH3 N O O H H H CH3 OCH3 N O O H H H OCH3 OCH3 N O 1 H H H CH3 CH3 CH O 1 H H H CH3 OCH3 CH O 1 H H H OCH3 OCH3 CH O 1 H H H CH3 CH3 N O 1 H H H CH3 OCH3 N O 1 H H H OCH3 OCH3 N S O H H H OCH3 OCH3 CH S 1 H H H OCH3 OCH3 CH O O CH3 H H OCH3 OCH3 N O O H o-F H OCH3 OCH3 CH O O H m-Cl H OCH3 OCH3 CH O O H o-Br H OCH3 OCH3 CH O O H m-CH3 H OCH3 OCH3 CH O O H o-OCH3 H OCH3 OCH3 CH O O H m-CF3 H OCH3 OCH3 CH O O H H H Cl OCH3 CH O O H H H CH3 OCH2CH3 CH Table 8a (continued) EMI90.1 <tb> W <SEP> n <SEP> P <SEP> R1 <SEP> 5 <SEP> X <SEP> Y <SEP> Z <SEP> m.p.(0C) <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> NH2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> NHCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> N(CR3)2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH2CH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CF3 <SEP> CR <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH=CH2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2C-CH <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CF3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCR2CH2OCR3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCH3)2 <SEP> CH <tb> <SEP> m <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> O,C/O <SEP> CH <tb> <SEP> H <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH2OCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCR3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCH2CH3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCl <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CBr <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH2OCH3 <SEP> CH <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> H <SEP> C1 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> m-SCH3 <SEP> H <SEP> OCH3 <SEP> OCR3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> m-OCF2H <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> F <SEP> OCH3 <SEP> CH <SEP> > <tb> <SEP> 3 <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH2F <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CF2H <SEP> OCH3 <SEP> CH <tb> o <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> OCF3 <SEP> OCR3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CF3 <SEP> OCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> ( <SEP> AO <SEP> CH <tb> <SEP> HX <tb> Table 8a (continued) EMI91.1 <tb> W <SEP> n <SEP> P <SEP> R1 <SEP> R5 <SEP> X <SEP> Y <SEP> Z <SEP> m.p. <SEP> ( C) <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> Br <SEP> OCH <SEP> 3 <SEP> CH <tb> <SEP> CH3 <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> O <SEP> O <SEP> CH <tb> <SEP> J <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH <tb> <SEP> 3 <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CN <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> 3 <SEP> CH(OCHZCH3) <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCR2F <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH <SEP> 3 <SEP> OCF3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCH2F <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF3 <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2H <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHClF <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CRBrF <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHFCF3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CR3 <SEP> SCF <SEP> 2H <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHC1F <SEP> CR <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CR3 <SEP> SCF2CHBrF <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CBFCF3 <SEP> CH <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CH <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> SOCH3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> C1 <SEP> OCH <SEP> 3 <SEP> CH <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> CR3 <SEP> OCH <SEP> 3 <SEP> N <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> OCH3 <SEP> OCH <SEP> 3 <SEP> N <tb> Table 9a EMI92.1 W n R R1 R2 R5 X Y Z m.p.( C) O O H H CH3 H CH3 CH3 CH O O H H CH3 H CH3 OCH3 CH O O H H CH3 H OCH3 OCH3 CH O O H H CH3 H Cl OCH3 CH O O H H CH3 H CH3 OCH3 N O O H H CH3 H OCH3 OCH3 N O O H H CH2CH3 H CH3 CH3 CH O O H H CH2CH3 H CH3 OCH3 CH O O H H CH2CH3 H OCH3 OCH3 CH O O H H CH2CH3 H Cl OCH3 CH O O H H CH2CH3 H CH3 OCH3 N O O H H CH2CH3 H OCH3 OCH3 N O O H H CH(CH3)2 H CH3 OCH3 CH O O H H CH(CH3)2 H OCH3 OCH3 CH O 1 H H CH3 H CH3 CH3 CH O 1 H H CH3 H CH3 OCH3 CH O 1 H H CH3 H OCH3 OCH3 CH O 1 H H CH3 H CH3 CH3 N O 1 H H CH3 H CH3 OCH3 N O 1 H H CH3 H OCH3 OCH3 N O 1 H H CH2CH3 H CH3 CH3 CH O 1 H H CH2CH3 H CH3 OCH3 CH O 1 H H CH2CH3 H OCH3 OCH3 CH O 1 H H CH2CH3 H CH3 CH3 N Table 9a (continued) EMI93.1 <tb> W <SEP> n <SEP> R <SEP> l <SEP> R1 <SEP> Rs <SEP> X <SEP> Y <SEP> Z <SEP> m.p.(0C) <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> CH2CH3 <SEP> H <SEP> CH3 <SEP> SOCH3 <SEP> N <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> CR2CR3 <SEP> H <SEP> OCH3 <SEP> OCR3 <SEP> N <tb> S <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> S <SEP> 1 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> OCR3 <SEP> OCR3 <SEP> CH <tb> o <SEP> 0 <SEP> CR3 <SEP> H <SEP> CH3 <SEP> H <SEP> OCR3 <SEP> QC <SEP> N <tb> O <SEP> O <SEP> H <SEP> o-F <SEP> CH3 <SEP> H <SEP> SOCH3 <SEP> OCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> m-Cl <SEP> CH3 <SEP> H <SEP> OCH3 <SEP> H3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> o-Br <SEP> CH3 <SEP> H <SEP> OCR3 <SEP> OCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> IrrcH3 <SEP> CH3 <SEP> H <SEP> OCR3 <SEP> OCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> ¯ <SEP> H3 <SEP> CR3 <SEP> H <SEP> OCR3 <SEP> OCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> tCF3 <SEP> CH3 <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> C1 <SEP> SOCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> OCH2QI3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> NH2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> ARCH3 <SEP> CH <tb> 00H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> N <SEP> (CH3)2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH2CH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CF3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CR3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CR3 <SEP> CCH2CH=CH2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> OCH2O <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> OCH2CF3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> aM2CH2CCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH(CCH3)2 <SEP> CH <tb> <SEP> ¯¯ <SEP> / <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> C,O <SEP> CH <tb> <SEP> Hs <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH2C±H3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCR3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CR3 <SEP> CCH2C <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CR3 <SEP> CC1 <tb> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CR3 <SEP> CBr <tb> Table 9a (continued) EMI94.1 <SEP> W <SEP> n <SEP> P <SEP> R, <SEP> R, <SEP> P5 <SEP> m.p. <tb> <SEP> w <SEP> 1 <SEP> R <SEP> R1 <SEP> R2 <SEP> Rs <SEP> X <SEP> Y <SEP> z <SEP> ( <SEP> (Oc) <tb> <SEP> O <SEP> 1 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CR2OCR3 <SEP> CH <tb> <SEP> O <SEP> 1 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> Cl <SEP> OCR3 <SEP> CH <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> CH2CH2CH3 <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CH <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> CR <SEP> CR3 <SEP> H <SEP> CR3 <SEP> CCH3 <SEP> CH <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> CR3 <SEP> H <SEP> OCR3 <SEP> OCR3 <SEP> CH <tb> <SEP> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH2CH2CH3 <SEP> H <SEP> C1 <SEP> OCR3 <SEP> CH <tb> <SEP> 0 <SEP> O <SEP> H <SEP> H <SEP> CR <SEP> CR <SEP> H <SEP> CR3 <SEP> OCH3 <SEP> N <tb> <SEP> 0 <SEP> O <SEP> H <SEP> H <SEP> CH2CH2CH3 <SEP> H <SEP> OCR3 <SEP> OCH3 <SEP> N <tb> <SEP> 3' <tb> <SEP> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CR2CR2CR2CH3 <SEP> H <SEP> OCR3 <SEP> OCH3 <SEP> N <tb> <SEP> 0 <SEP> O <SEP> HH <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CH <tb> <SEP> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCR3 <SEP> CH <tb> <SEP> 0 <SEP> OOH <SEP> H <SEP> z <SEP> H <SEP> H <SEP> OCH3 <SEP> OCR3 <SEP> CH <tb> <SEP> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> C1 <SEP> OCR3 <SEP> CH <tb> <SEP> 0OHH <SEP> H <SEP> H <SEP> CH3 <SEP> OCR3 <SEP> N <tb> <SEP> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> OCR3 <SEP> CX <SEP> H3 <SEP> N <tb> <SEP> 0 <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> OCH3 <SEP> our3 <SEP> CH <tb> <SEP> O <SEP> OH <SEP> m-SCH3 <SEP> CH3 <SEP> H <SEP> OCR3 <SEP> OCR3 <SEP> CH <tb> <SEP> O <SEP> O <SEP> H <SEP> m-OCFcfl <SEP> CH3 <SEP> H <SEP> OCR3 <SEP> OCR3 <SEP> CH <tb> <SEP> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> F <SEP> OCH3 <SEP> CH <tb> <SEP> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> Br <SEP> OCR3 <SEP> CH <tb> <SEP> 0 <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH2F <SEP> C±H3 <SEP> CH <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CU2H <SEP> OCR3 <SEP> CH <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> OCF3 <SEP> H3 <SEP> CH <tb> - <SEP> 0 <SEP> 0' <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CF3 <SEP> OCR3 <SEP> CH <tb> <SEP> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CR <tb> <SEP> CR3 <tb> <SEP> 0 <SEP> 0, <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CR <tb> <SEP> CH <tb> <SEP> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> H <SEP> CH <tb> Table 9a (continued) n R R1 R2 R5 X Y Z m.p.( C) 0 O H H CH3 H CH3 CN CH O O H H CH3 H CH3 CH(OCH2CH3)2 CH O O H H CH3 H CH3 OCH2F CH O O H H CH3 H CH3 OCF3 CH O O H H CH3 H CH3 SCH2F CH O O H H CH3 H CH3 SCF3 CH O O H H CH3 H CH3 OCF2H CH O O H H CH3 H CH3 OCF2CHClF CH O O H H CH3 H CH3 OCF2CHBrF CH O O H H CH3 H CH3 OCF2CHFCF3 CH O O H H CH3 H CH3 SCF2H CH O O H H CH3 H CH3 SCF2CHClF CH O O H H CH3 H CH3 SCF2CHBrF CH O O H H CH3 H CH3 SCF2CHFCF3 CH O 2 H H CH3 H CH3 CH3 CH O 2 H H CH3 H CH3 OCH3 CH O 2 H H CH3 H CH3 OCH3 CH O 2 H H CH3 H CH3 OCH3 CH O 2 H H CH3 H CH3 OCH3 N O 2 H H CH3 H Cl OCH3 N Table lOa EMI96.1 W n R R1 R5 X Y Z m.p.( C) O O H H H CH3 CH3 CH O O H H H CH3 OCH3 CH O O H H H OCH3 OCH3 CH O O H H H CH3 CH3 N O O H H H CH3 OCH3 N O 0 H H H OCH3 O OCH3 N O 1 H H H CH3 CH3 CH O 1 H H H CH3 OCH3 CH O 1 H H H OCH3 OCH3 CH O 1 R H H CH3 CH3 N O 1 H H H H CH3 OCH3 N O 1 H H H OCH3 OCH3 N S O H H H OCH3 OCH3 CH -S 1 H H H OCH3 OCH3 CH O O CH3 H H OCH3 OCH3 N O O H o-F H OCH3 OCH3 CH O O H m-Cl H OCH3 OCH3 CH O O H o-Br H OCH3 OCH3 CH O O H m-CH3 H OCH3 OCH3 CH O O H o-OCH3 H OCH3 OCH3 CH O O H m-CP3 H OCH3 OCH3 CH O O H H H Cl OCH3 CH O O H H H CH3 OCH2CH3 CH Table 10a (continued) EMI97.1 <tb> W <SEP> n <SEP> P <SEP> R1 <SEP> P5 <SEP> X <SEP> Y <SEP> Z <SEP> m.p.( C) <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> R <SEP> CH3 <SEP> NH2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> NHCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> N(CH3)2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH2CH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CF3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH=CH2 <SEP> CH <tb> OORH <SEP> H <SEP> CH3 <SEP> OCH2C'CH <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCR2CF3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH <SEP> CH3 <SEP> OCH2CR2OCR3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCH3)2 <SEP> CH <tb> <SEP> 3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OC-O <SEP> CH <tb> <SEP> H <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CHzOCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCR3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCH2CR3 <tb> OOHH <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CC1 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CBr <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CR2OCR3 <SEP> CH <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> H <SEP> C1 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> m-SCH3 <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> T <SEP> 0 <SEP> H <SEP> m-OCF2H- <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> 3 <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> F <SEP> OCH3 <SEP> CR <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH2F <SEP> OCH3 <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> OCF2H <SEP> OCH3 <SEP> CR <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> OCF <SEP> 3 <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CF3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> X <SEP> CH <tb> <SEP> H <tb> Table 10a (continued) EMI98.1 <tb> w <SEP> n <SEP> R <SEP> R1 <SEP> Rs <SEP> X <SEP> Y <SEP> Z <SEP> m.p.("C) <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> Br <SEP> OCH3 <SEP> CH <tb> <SEP> CH3 <tb> o <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CR3 <SEP> O <SEP> O <SEP> CH <tb> <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CN <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCH2CR3)2 <SEP> CR <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2F <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> fl. <SEP> H <SEP> CH3 <SEP> OCF3 <SEP> CR <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCH2F <SEP> CR <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2H <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CRClF <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CRBrF <SEP> CR <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHFCF3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2H <SEP> CR <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHC1F <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHBrF <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHFCF3 <SEP> CH <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CH <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> C1 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> N <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> N <tb> Table 10b EMI99.1 W n R R1 R5 X Y Z m.p.( C) O O H H H CH3 CH3 CH O O H H H CH3 OCH3 CH O O H H H OCH3 OCH3 CH O O H H H CH3 CH3 N O O H H H CH3 OCH3 N O O H H H OCH3 OCH3 N O 1 H H H CH3 CH3 CH O 1 H H H CH3 OCH3 CH O 1 H H H OCH3 OCH3 CH O 1 H H H CH3 CH3 N O 1 H H H CH3 OCH3 N O 1 H H H OCH3 OCH3 N S O H H H OCH3 OCH3 CH S 1 H H H OCH3 OCH3 CH O O CH3 H H OCH3 OCH3 N O O H o-F H OCH3 OCH3 CH O O H m-Cl H OCH3 OCH3 CH O O H o-Br H OCH3 OCH3 CH O O H m-CH3 H OCH3 OCH3 CH O O H o-OCH3 H OCH3 OCH3 CH O O H m-CF3 H OCH3 OCH3 CH O O H H H Cl OCH3 CH O O H H H CH3 OCH2CH3 CH Table 10b (continued) EMI100.1 <tb> W <SEP> n <SEP> P <SEP> R1 <SEP> R5 <SEP> X <SEP> Y <SEP> Z <SEP> m.p.( c) <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> NH2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> NHCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> N <SEP> (CH3)2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH2CH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CF3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH=CH2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2C--CH <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CR3 <SEP> OCR <SEP> CF <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CR2OCR3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCH3)2 <SEP> CH <tb> <SEP> 2 <tb> O <SEP> O <SEP> H- <SEP> H <SEP> H <SEP> CH3 <SEP> O,C/O <SEP> CR <tb> <SEP> H <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH2OCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCR3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CCH2CH3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CC1 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CBr <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH2OCH3 <SEP> CH <tb> O <SEP> 1 <SEP> H <SEP> H <SEP> H <SEP> C1 <SEP> OCH3 <SEP> CR <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> m-SCH3 <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> m-OCF2H <SEP> H <SEP> OCH <SEP> OCH <SEP> CR <tb> 0 <SEP> 4; <SEP> H <SEP> f3. <SEP> H <SEP> H <SEP> F <SEP> OCH3 <SEP> CR <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH2F <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CF2H <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> OCF3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> -O <SEP> H <SEP> H <SEP> H <SEP> CF3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> X <SEP> CH <tb> Table 10b (continued) EMI101.1 <tb> W <SEP> n <SEP> R <SEP> R1 <SEP> R5 <SEP> X <SEP> Y <SEP> Z <SEP> m.p.(0C) <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> Br <SEP> OCH3 <SEP> CH <tb> <SEP> CH3 <tb> o <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> X <SEP> CH <tb> <SEP> C <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CN <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCH2CH3)2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCR2F <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCH2F <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2H <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHC1F <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CRBrF <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHFCF3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2H <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHC1F <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHBrF <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CRFCF3 <SEP> CH <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CR3 <SEP> CH <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> OCH3 <SEP> OCH <SEP> 3 <SEP> CH <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> C1 <SEP> OCH3 <SEP> CH <tb> 0- <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> N <tb> 0 <SEP> 2 <SEP> H <SEP> H <SEP> H <SEP> SOCH3 <SEP> OCH <SEP> N <tb> Table 11a EMI102.1 W n R R1 R6 R7 X Y Z m.p.( C) O O H H H H CH3 CH3 CH O O H H H H CH3 OCH3 CH O O H H H H OCH3 OCH3 CH O O H H H H Cl OCH3 CH O OH H H H CH3 OCH3 N O O H H H H OCH3 OCH3 N O O H H CH3 H CH3 CH3 CH O O H H H CH3 CH3 OCH3 CH O O H H CH3 H OCH3 OCH3 CH O O H H H CH3 Cl OCH3 CH O O H H CH3 H CH3 OCH3 N O O H H H CH3 OCH3 OCH3 N O O H H CH3 CH3 CH3 CH3 CH O O H H CH3 CH3 CH3 OCH3 CH O O H H CH3 CH3 OCH3 OCH3 CH O O H H CH3 CH3 Cl OCH3 CH O O H H CH3 CH3 CH3 OCH3 N O O H H CH3 CH3 OCH3 OCH3 N O O H H H H CH3 OCH2CH3 CH O O H m-F H H CH3 CH2OCH3 CH O O H o-Cl H H CH3 NH2 CH O O H m-Br H H CH3 NHCH3 CH O O H o-CH3 H H CH3 N(CH3)2 CH O O H m-OCH3 H H CH3 C2H5 CH O O H o-CF3 H H CH3 CF3 CH Table 11a (continued) EMI103.1 W <SEP> n <SEP> P <SEP> R <SEP> 6 <SEP> 7 <SEP> X <SEP> Y <SEP> 2 <SEP> m.p. <tb> ¯ <SEP> 1 <SEP> Y <SEP> ( C) <tb> O <SEP> 0 <SEP> H <SEP> m-SCH3 <SEP> H <SEP> H <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> O <SEP> 0 <SEP> H <SEP> o-OCF2H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH"CH2 <SEP> CH <tb> O <SEP> 0 <SEP> H <SEP> o-OCF2H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2C-CH <SEP> CH <tb> O <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CF3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH2OCH3 <SEP> CR <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CR(OCR3)2 <SEP> CR <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> 02 <SEP> CH <tb> <SEP> 3 <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> gn0 <SEP> CH <tb> <SEP> H <tb> <SEP> CH3 <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> m{CH3 <SEP> CR <tb> <SEP> OyO <tb> <SEP> H <SEP> \ <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CN <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(oCH2CH3)2 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> -H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2F <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCH2F <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF3 <SEP> CH <tb> 0 <SEP> 0- <SEP> H <SEP> -H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2H <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHC1F <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHBrF <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CRFCF3 <SEP> CR <tb> 0 <SEP> 0 <SEP> -- <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2H <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHC1F <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHBrF <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHFCF3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH2F <SEP> CH3 <SEP> CH <tb> Table 11a (continued) R1 R6 R7 X Y Z m.p.( C) O O H H H H F OCH3 CH O O H H H H Br OCH3 CH O O H H H H OCF2H CH3 CH O O H H H H OCF3 CH3 CH O O H H H H CF3 CH3 CH S O H H H H OCH3 OCH3 CH O O CH3 H H H OCH3 OCH3 N O 1 H H H H CH3 CH3 CH O 1 H H H H CH3 OCH3 CH O 1 H H H H OCH3 OCH3 CH O 1 H H H H Cl OCH3 CH O 1 H H H H CH3 OCH3 N O 1 H H H H OCH3 OCH3 N O 1 H H CH3 H CH3 CH3 CH O 1 H H H CH3 CH3 OCH3 CH O 1 H H CH3 H OCH3 OCH3 CH O 1 H H H CH3 Cl OCH3 CH O 1 H H CH3 H CH3 OCH3 N O 1 H H H CH3 OCH3 OCH3 N O 1 H H CH3 CH3 CH3 CH3 CH O 1 H H CH3 CH3 CH3 OCH3 CH O 1 H H CH3 CH3 OCH3 OCH3 CH O 1 H H CH3 CH3 Cl OCH3 CH O 1 H H CH3 CH3 CH3 OCH3 N O 1 H H CH3 CH3 OCH3 OCH3 N O 2 H H H H CH3 CH3 H O 2 H H H H CH3 OCH3 CH O 2 H H H H OCH3 OCH3 CH O 2 H H H H Cl OCH3 CH 0 2 H H H H CH3 OCH3 N 0 2 H H H .. H OCH3 OCH3 N Table llb EMI105.1 W n R R1 R6 R7 X Y Z (m.p.( C) O O H H H H CH3 CH3 CH O O H H H H CH3 OCH3 CH O O H H H H OCH3 OCH3 CH O O H H H H Cl OCH3 CH O O H H H H CH3 OCH3 N O O H H H H OCH3 OCH3 N O O H H CH3 H CH3 CH3 CH O O H H H CH3 CH3 OCH3 CH O O H H CH3 H OCH3 OCH3 CH O O H H H CH3 Cl OCH3 CH O O H H CH3 H CH3 OCH3 N O O H H CH3 OCH3 OCH3 N O O H CH3 CH3 CH3 CH3 CH O O H CH3 CH3 CH3 OCH3 CH O O H CH3 CH3 OCH3 OCH3 CH O O H CH3 CH3 Cl OCH3 CH O O H CH3 CH3 CH3 OCH3 N O 0 H H CH3 CH3 OCH3 OCH3 N O O H H H H CH3 OCH2CH3 CH O O H m-F H H CH3 CH2OCH3 CH O O H o-Cl H H CH3 NH2 CH O O H m-Br H H CH3 NHCH3 CH O O H o-CH3 H H CH3 N(CH3)2 CH O O H m-OCH3 H H CH3 C2H5 CH O O H o-CF3 H H CH3 CF3 CH Table 11b (continued) EMI106.1 <tb> <SEP> W <SEP> n <SEP> R <SEP> R, <SEP> Rg <SEP> R7 <SEP> X <SEP> Y <SEP> 2 <SEP> m.p. <tb> <SEP> W <SEP> n <SEP> R <SEP> P6 <SEP> P7 <SEP> X <SEP> Y <SEP> Z <SEP> ( C) <tb> <SEP> ¯ <SEP> ¯ <SEP> (0C) <tb> <SEP> O <SEP> O <SEP> H <SEP> m- <SEP> SCH3 <SEP> H <SEP> H <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> <SEP> O <SEP> 0 <SEP> H <SEP> o-OCF2H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH2CH2 <SEP> CH <tb> <SEP> O <SEP> o <SEP> H <SEP> o-OCF2R <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2C=CH <SEP> CH <tb> <SEP> 0 <SEP> OHR <SEP> H <SEP> H <SEP> CH3 <SEP> OCR <SEP> 2CF3 <SEP> CH <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH20CH3 <SEP> CH <tb> <SEP> OOHH <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCH3)2 <SEP> CH <tb> <SEP> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> oAo <SEP> CH <tb> <SEP> 0 <SEP> /0 <tb> <SEP> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> O <SEP> CR <tb> <SEP> H <tb> <SEP> CR3 <tb> <SEP> 0 <SEP> OHH <SEP> H <SEP> H <SEP> CH3 <SEP> om$ <SEP> CH <tb> <SEP> 0 <SEP> 0 <tb> <SEP> HX <tb> <SEP> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CN <SEP> CR <tb> <SEP> O <SEP> 0 <SEP> RH <SEP> H <SEP> H <SEP> CH3 <SEP> CH(oCH2CH3)2 <SEP> CH <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2F <SEP> CH <tb> <SEP> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF3 <SEP> CH <tb> <SEP> O <SEP> O <SEP> HH <SEP> H <SEP> H <SEP> CH3 <SEP> SCH2F <SEP> CH <tb> <SEP> 0 <SEP> ORH <SEP> H <SEP> H <SEP> CH3 <SEP> SCF3 <SEP> CH <tb> -O <SEP> 0 <SEP> -H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2H <SEP> CH <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHC1F <SEP> CR <tb> <SEP> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHBrF <SEP> CH <tb> <SEP> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHFCF3 <SEP> CH <tb> <SEP> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2H <SEP> CH <tb> <SEP> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHC1F <SEP> CH <tb> <SEP> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHBrF <SEP> CH <tb> <SEP> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CRFCF3 <SEP> CH <tb> <SEP> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH2F <SEP> CH3 <SEP> CH <tb> Table 11b (continued) W n R R1 R6 R7 X Y Z (m.p. ( C) O O H H H H P OCH3 CH O O H H H H Br OCH3 CH O O H H H H OCF2H CH3 CH O O H H H H OCF3 CH3 CH O O H H H H CF3 CH3 CR S O H H H H OCH3 OCH3 CH O O CH3 H H H OCH3 OCH3 N O 1 H H H H CH3 CH3 CR O 1 H H H H CH3 OCH3 CH O 1 H H H H OCH3 OCH3 CH O 1 H H H H Cl OCH3 CH O 1 H H H H CH3 OCH3 N O 1 H H H H OCH3 OCH3 N O 1 H H CH3 H CH3 CH3 CH O 1 H H H CH3 CH3 OCH3 CH O 1 H H CH3 H OCH3 OCH3 CH O 1 H H H CH3 Cl OCH3 CH O 1 H H CH3 H CH3 OCH3 N O 1 H H H CH3 OCH3 OCH3 N O 1 H H CH3 CH3 CH3 CH3 CH O 1 H H CH3 CH3 CH3 OCH3 CH O 1 H H CH3 CH3 OCH3 OCH3 CH O 1 H H CH3 CH3 Cl OCH3 CH O 1 H H CH3 CH3 CH3 OCH3 N O 1 H H CH3 CH3 OCH3 OCH3 N O 1 H H H H CH3 CH3 CH 0 2 H H H H CH3 OCH3 CH O 2 H H H H OCH3 OCH3 CH O 2 H H H H Cl OCH3 CH O 2 H H H H CH3 OCH3 N 0 2 H H H H OCH3 OCH3 N Table 12a EMI108.1 W n R R1 R5 R6 R7 X Y Z m.p.( C) O O H H H H H CH3 CH3 CH O O H H H H H CH3 OCH3 CH O O H H H H H OCH3 OCH3 CH O O H H H H H Cl OCH3 CH O O H H H H H CH3 OCH3 N O O H H H H H OCH3 CH3 N O O H H H CH3 H CH3 CH3 CH O O H H H H CH3 CH3 OCH3 CH O O H H H CH3 H OCH3 OCH3 CH O O H H H H CH3 Cl OCH3 CH O O H H H CH3 H CH3 OCH3 N O O H H H H CH3 OCH3 OCH3 N O O H H H CH3 CH3 CH3 CH3 CH O O H H H H CH3 CH3 OCH3 CH O O H H H CH3 CH3 OCH3 OCH3 CH O O H H H CH3 CH3 Cl OCH3 CH O O H H H CH3 CH3 CH3 OCH3 N O O H H H CH3 CH3 OCH3 OCH3 N O O H H CH3 H H CH3 OCH2CH3 CH O O H m-F H H H CH3 CH2OCH3 CH O O H o-Cl H H H CH3 NH2 CH O O H m-BR H H H CH3 NHCH3 CH O O H o-CH3 H H H CH3 N(CH3)2 CH O O H m-OCH3 H H H CH3 C2H5 CH 0 0 H o-CF3 H H H CH3 CF3 CH Table 12a (continued) EMI109.1 <tb> W <SEP> n <SEP> R <SEP> R1 <SEP> R6 <SEP> P7 <SEP> R <SEP> X <SEP> Y <SEP> Z <SEP> m.p.("C) <tb> ¯ <SEP> ¯ <SEP> ¯ <SEP> ¯ <SEP> ¯ <SEP> ¯ <SEP> ¯ <SEP> ¯ <SEP> ¯ <SEP> ¯ <tb> O <SEP> O <SEP> H <SEP> m"SCH3 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> H3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> o < F;H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCRR=CH2 <SEP> CR <tb> O <SEP> O <SEP> H <SEP> o-OCFSI <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH2CeCH <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCR2CF3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> 0CH2CH2CCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(CCH3)2 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> 0 <SEP> D <SEP> CH <tb> <SEP> 0 <SEP> 0 <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CR3 <SEP> CH <tb> <SEP> 0 <SEP> 0 <tb> <SEP> H <tb> <SEP> cy, <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> ( <SEP> CH <tb> <SEP> X <tb> <SEP> H <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> ON <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(CCH2CH3)2 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CCH2F <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF3 <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SHzF <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> 9CE3 <SEP> CH <tb> O <SEP> ft-H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCFcJI <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CEI3 <SEP> CCF2t: :HClF <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHBrF <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> a:F2CHFCF3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCR2H <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> sCF2CHC1F <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CBrF <SEP> CR <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCFCHFCF3 <SEP> CH <tb> 0 <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH2F <SEP> CH3 <SEP> CH <tb> Table 12a (continued) W n R R1 R5 R6 R7 X Y Z m.p.( C) O O H H H H H F OCH3 CH O O H H H H H Br OCH2 CH O O H H H H H OCF2H CH3 CH O 0 H H H H H OCF3 CH3 CH O 0 H H H H H CF3 CH3 CH S O H H H H H OCH3 OCH3 CH O O CH3 H H H H OCH3 OCH3 N O 1 H H H H H CH3 CH3 CH O 1 H H H H H CH3 OCH3 CH O 1 H H H H H OCH3 OCH3 CH O 1 H H H H H Cl OCH3 CH O 1 H H H H H CH3 OCH3 N O 1 H H H H H OCH3 OCH3 N O 1 H H H CH3 H CH3 CH3 CH O 1 H H H H CH3 CH3 OCH3 CH O 1 H H H CH3 H OCH3 OCH3 CH O 1 H H H H CH3 Cl OCH3 CH O 1 H H H CH3 H CH3 OCH3 N O 1 H H H H CH3 OCH3 OCH3 N O 1 H H H CH3 CH3 CH3 CH3 CH O 1 H H H CH3 CH3 CH3 OCH3 CH O 1 H H H CH3 CH3 OCH3 OCH3 CH O 1 H H H CH3 CH3 Cl OCH3 CH O 1 H H H CH3 CH3 CH3 OCH3 N O 1 H H H CH2 CH2 OCH3 OCH3 N O 2 H H H H H CH3 CH3 CH O 2 H H H H H CH3 OCH3 CH O 2 H H H H H OCH3 OCH3 CH O 2 H H H H H Cl OCH3 CH O 2 H H H H H CH3 OCH3 N 0 2 H H H H H OCH3 OCH3 N Table 13a EMI111.1 EMI111.2 <tb> W <SEP> R <SEP> R1 <SEP> R2 <SEP> X <SEP> Y <SEP> z <SEP> m.p.(OC) <tb> S <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> OCH2CH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CH2OCR3 <SEP> CR <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> NH2 <SEP> CR <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> NHCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CR3 <SEP> 3 <SEP> N(CH3)2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> 3 <SEP> CR3 <SEP> CH2CH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> 3 <SEP> H3 <SEP> CF3 <SEP> CR <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CR3 <SEP> CH3 <SEP> OCH2CH=CH2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> OCR2C=CH <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> OCH2CF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> OCH2CH2OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CR3 <SEP> CH3 <SEP> CH(OCH3)2 <SEP> CH <tb> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> 0 <SEP> 0 <SEP> CH <tb> <SEP> HX <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> n <SEP> CH <tb> <SEP> CH3 <SEP> 0 > C <tb> <SEP> CH3 <tb> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CR <tb> Table 13a (continued) W R R1 R2 X Y Z m.p. ( C) O H H CH3 CH3 H CH O H H CH3 CH3 CN CH O H H CH3 CH3 CH(OCH2CH3)2 CH O H H CH3 CH3 OCH2F CH O H H CH3 CH3 OCF3 CH O H H CH3 CH3 SCH2F CH O H H CH3 CH3 SCF3 CH O H H CH3 CH3 OCF2H CH O H H CH3 CH3 OCF2CHClF CH O H H CH3 CH3 OCF2CHBrF CH O H H CH3 CH3 OCF2CHFCF3 CH O H H CH3 CH3 SCF2H CH O H H CH3 CH3 SCF2CHClF CH O H H CH3 CH3 SCF2CHBrF CH O H H CH3 CH3 SCF2CHFCF3 CH O H H CH3 CH3 OCH3 CCH3 O H H CH3 CH3 OCH3 CCH2CH3 O H H CH3 CH3 OCH3 CCl O H H CH3 CH3 OCH3 CBr O H H CH3 F OCH3 CH O H H CH3 Br OCH3 CH O H H CH3 CH2F OCH3 CH O H H CH3 OCF2H OCH3 CH O H H CH3 OCF3 OCH3 CH O H H CH3 CF3 OCH3 CH O H m-F CH3 CH3 OCH3 CH O H o-Cl CH3 CH3 OCH3 CH O H m-Br CH3 CH3 OCH3 CH O H o-CH3 CH3 CH3 OCH3 CH O H m-CF3 CH3 CH3 OCH3 CH O H o-SCH3 CH3 CH3 OCH3 CH O H m-OCH3 CH3 CH3 OCH3 CH O H o-OCF2H CH3 CH3 OCH3 CH Table 13a (continued) W R R1 R2 X Y Z (m.p.( C) O CH3 H H CH3 OCH3 CH O H H H CH3 CH3 CH O H H H CH3 OCH3 CH O H H H OCH3 OCH3 CH O H H H Cl OCH3 CH O H H H CH3 OCH3 N O H H H OCH3 OCH3 N O H H CH3 CH3 CH3 CH O H H CH3 CH3 OCH3 CH O H H CH3 OCH3 OCH3 CH 205-210 O H H CH3 Cl OCH3 CH O H H CH3 CH3 OCH3 N O H H CH3 OCH3 OCH3 N O H H CH2CH3 CH3 CH3 CH O H H CH2CH3 CH3 OCH3 CH O H H CH2CH3 OCH3 OCH3 CH O H H CH2CH3 Cl OCH3 CH O H H CH2CH3 CH3 OCH3 N O H H CH2CH3 OCH3 OCH3 N O H H CH2CH2CH3 OCH3 OCH3 CH O H H CH2CH2CH2CH3 OCH3 OCH3 CH Table 14a EMI114.1 EMI114.2 <tb> W <SEP> R <SEP> R1 <SEP> X <SEP> Y <SEP> Z <SEP> m.p.(OC) <tb> S <SEP> H <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH2OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> NH2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> NHCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> N <SEP> (CH3)2 <SEP> CK <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH2CH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH-CH2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2C-CH <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> OCR2CF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH2OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCH3)2 <SEP> CH <tb> o <SEP> H <SEP> H <SEP> CH3 <SEP> X <SEP> CH <tb> <SEP> 0 <SEP> 0 <tb> <SEP> H <tb> 0 <SEP> H <SEP> H <SEP> CR <SEP> 0 <SEP> CH <tb> <SEP> 3 <SEP> 0 <SEP> ,0 <tb> <SEP> CH3 <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH <SEP> CR <tb> <SEP> CH <tb> <SEP> H <tb> Table 14a (continued) R R1 X Y Z (m.p.( C) O H H CH3 H CH O H H CH3 CN CH O H H CH3 CH(OCH2CH3)2 CH O H H CH3 OCH2F CH O H H CH3 OCF3 CH O H H CH3 SCH2F CH o H H CH3 SCF3 CH O H H CH3 OCF2H CH O H H CH3 OCF2CHClF CH O H H CH3 OCF2CHBrF CH O H H CH3 OCF2CHFCF3 CH O H H CH3 SCF2H CH O H H CH3 SCF2CHClF CH O H H CH3 SCF2CHBrF CH O H H CH3 SCF2CHFCF3 CH O H H CH3 OCH3 CCH3 O H H CH3 OCH3 OCH2CH3 O H H CH3 OCH3 CC1 O H H CH3 OCH3 CBr O H H F OCH3 CH O H H Br OCH3 CH O H H CH2F OCH3 CH O H H OCF2H OCH3 CH O H H OCF3 OCH3 CH O H H CF3 OCH3 CH O H m-F CH3 OCH2 CH O H o-Cl CH3 OCH2 CH O H m-Br CH3 OCH2 CH O H o-CH3 CH3 OCH2 CH O H m-CF3 CH3 OCH2 CH O H O-SCH3 CH3 OCH2 CH O H m-OCH3 CH3 OCH3 CR O H o-OCF2H CH3 OCH3 CH Table 14a (continued) W R R1 X Y Z (m.p.( C) O CH3 H CH3 OCH3 CH O H H CH3 CH3 CH O H H CH3 OCH3 CH O H H OCH3 OCH3 CH O H H Cl OCH2 CH O H H CH3 OCH2 N O H H OCH3 OCH3 N Table 15a EMI117.1 EMI117.2 <tb> W <SEP> R <SEP> R1 <SEP> R2 <SEP> X <SEP> Y <SEP> Z <SEP> m.p.(OC) <tb> S <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> OCH2CH3 <SEP> CR <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> C <SEP> 3 <SEP> CH2OCH3 <SEP> CH <tb> o <SEP> H <SEP> H <SEP> 3 <SEP> 3 <SEP> NH2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> NHCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> 3 <SEP> 3 <SEP> N(CH3)2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CR3 <SEP> CR3 <SEP> CH2CH3 <SEP> CR <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> OCH2CH=CH2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> OCH2C-CH <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> OCR2CF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CR3 <SEP> CR3 <SEP> OCH2CH20C83 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CH(OCH3)2 <SEP> CH <tb> rm <tb> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> X <SEP> CH <tb> <SEP> H <tb> O <SEP> H <SEP> H <SEP> CR3 <SEP> CH3 <SEP> o <SEP> CH <tb> <SEP> H <tb> <SEP> CH3 <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> O(D <SEP> CH <tb> <SEP> H <tb> Table 15a (continued) W R R1 R2 X Y Z m.p.( C) O H H CH3 CH3 H CH O H H CH3 CH3 CN CH O H H CH3 CH3 CH(OCH2CH3)2 CH O H H CH3 CH3 OCH2F CH O H H CH3 CH3 OCF3 CH O H H CH3 CH3 SCH2F CH O H H CH3 CH3 SCF3 CH O H H CH3 CH3 OCF2H CH O H H CH3 CH3 OCF2CHClF CH O H H CH3 CH3 OCF2CHBrF CH O H H CH3 CH3 OCF2CHFCF3 CH O H H CH3 CH3 SCF2H CH O H H CH3 CH3 SCF2CHClF CH O H H CH3 CH3 SCF2CHBrF CH O H H CH3 CH3 SCF2CHFCF3 CH O H H CH3 CH3 OCH3 CH O H H CH3 CH3 OCH3 CH O H H CH3 CH3 OCH3 CH O H H CH3 CH3 OCH3 CH O H H CH3 F OCH3 CH O H H CH3 Br OCH3 CH O H H CH3 CH2F OCH3 CH O H H CH3 OCF2H OCH3 CH O H H CH3 OCF3 OCH3 CH O H H CH3 CF3 OCH3 CH O H m-F CH3 CH3 OCH3 CH O H o-Cl CH3 CH3 OCH3 CH O H m-Br CH3 CH3 OCH3 CH O H o-CH3 CH3 CH3 OCH3 CH O H m-CF3 CH3 CH3 OCH3 CH O H o-SCH3 CH3 CH3 OCH3 CH O H m-OCH3 CH3 CH3 OCH3 CH O H o-OCF2H CH3 CH3 OCH3 CH Table 15a (continued) W R R1 R2 X Y Z m.p. ( C) O CH3 H H CH3 OCH3 CH OH H H CH3 CH3 CR O H H H CH3 OCH3 CH O H H H OCH3 OCH3 CH O H H H Cl OCH3 CH O H H H CH3 OCH3 N O H H H OCH3 OCH3 N O H H CH3 CH3 CH3 CH O H H CH3 CH3 OCH3 CH O H H CH3 OCH3 OCH3 CH O H H CH3 Cl OCH3 CH O H H CH3 CH3 OCH3 N O H H CH3 OCH3 OCH3 N O H H CH2CH3 CH3 CH3 CH O H H CH2CH3 CH3 OCH3 CH O H H CH2CH3 OCH3 OCH3 CH O H H CH2CH3 Cl OCH3 CH O H H CH2CH3 CH3 OCH3 N O H H CH2CH3 OCH3 OCH3 N O H H CH2CH2CH3 OCH3 OCH3 CH O H H CH2CH2CH2CH3 OCH3 OCH3 CH Table 16a EMI120.1 EMI120.2 <tb> 4 <SEP> R1 <SEP> R4 <SEP> X <SEP> Y <SEP> Z <SEP> m.p.( C) <tb> S <SEP> H <SEP> H <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH2OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> NH2 <SEP> CR <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> NRCR3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> N <SEP> (CH3)2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CR <SEP> CR <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH=CH2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCR2C=CR <SEP> CR <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH2OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCH3)2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> O/ ò <SEP> 0 <SEP> CH <tb> <SEP> HX <tb> 0. <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> 0XD <SEP> CH <tb> <SEP> H <tb> <SEP> CH3 <tb> O <SEP> H <SEP> H <SEP> H <SEP> CR3 <SEP> CH <tb> Table 16a (continued) W R R1 R4 X Y Z m.p. ( C) 0 H H H CH3 H CH 0 H H H CH3 CN CH 0 H H H CH3 CH(OCH2CH3)2 CH 0 H H H CH3 OCH2F CH 0 H H H CH3 OCF3 CH 0 H H H CH3 SCH2F CH 0 H H H CH3 SCF3 CH 0 H H H CH3 OCF2H CH 0 H H H CH3 OCF2CHClF CH 0 H H H CH3 OCF2CHBrF CH 0 H H H CH3 OCF2CHFCF3 CH 0 H H H CH3 SCF2H CH 0 H H H CH3 SCF2CHClF CH 0 H H H CH3 SCF2CHBrF CH 0 H H H CH3 SCF2CHFCF3 CH O H H H CH3 OCH3 CCR3 O H H H CH3 OCH3 CCH2CH3 O H H H CH3 OCH3 CC1 O H H H CH3 OCH3 CBr 0 H H H F OCH3 CH 0 H H H Br OCH3 CH O H H H CH2F OCH3 CH 0 H H H OCF2H OCH3 CH 0 H H H OCF3 OCH3 CH 0 H H H CF3 OCH3 CH O H m-F H CH3 OCH3 CH O H o-Cl H CH3 OCH3 CH O H m-Br H CH3 OCH3 CH O H o-CH3 H CH3 OCH3 CH O H m-CF3 H CH3 OCH3 CH O H o-SCH3 H CH3 OCH3 CH O H m-OCH3 H CH3 OCH3 CH O H o-OCF2H H CH3 OCH3 CH Table 16a (continued) W R R1 R4 X Y Z m.p.( C) O CH3 H H CH3 OCH3 CH O H H H CH3 CH3 CH O H H H CH3 OCH3 CH O H H H OCH3 OCH3 CH 226-236 O H H H Cl OCH3 CH O H H H CH3 OCH3 N O H H H OCH3 OCH3 N 0 H H CH3 OCH3 OCH3 CH 0 H H CH2CH3 OCH3 OCH3 CH 0 H H CH2CH2CH3 OCH3 OCH3 CH 0 H H CH2CH2CH2CH3 OCH3 OCH3 CH Table 17a EMI123.1 EMI123.2 <tb> W <SEP> R <SEP> R1 <SEP> X <SEP> Y <SEP> Z <SEP> m.p.("C) <tb> S <SEP> H <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH2OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> NH2 <SEP> CR <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> NHCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> N <SEP> (CR3)2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH2CH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH=CH2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2C2CH <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH2OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCR3)2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> 0 <SEP> 0 <SEP> CH <tb> <SEP> C <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> <SEP> X <SEP> <SEP> CH <tb> <SEP> H <tb> <SEP> CH3 <tb> 0 <SEP> H <SEP> H <SEP> CR3 <SEP> <SEP> CH <SEP> CR <tb> <SEP> H <tb> Table 17a (continued) W R R1 X Y Z m.p.( C) O H H CH3 H CH O H H CH3 CN CH 0 H H CH3 CH(OCH2CH3)2 CH 0 H H CH3 OCH2F CH 0 H H CH3 OCF3 CH 0 H H CH3 SCH2F CH 0 H H CH3 SCF3 CH 0 H H CH3 OCF2H CH 0 H H CH3 OCF2CHClF CH 0 H H CH3 OCF2CHBrF CH 0 H H CH3 OCF2CHFCF3 CH 0 H H CH3 SCF2H CH 0 H H CH3 SCF2CHClF CH 0 H H CH3 SCF2CHBrF CH 0 H H CH3 SCF2CHFCF3 CH 0 H H CH3 OCH3 CCH3 O H H CH3 OCH3 CCH2CH3 O H H CH3 OCH3 CC1 O H H CH3 OCH3 CBr O H H F OCH3 CH 0 H H Br OCH3 CH 0 H H CH2F OCH3 CH O H H OCF2H OCH3 CH 0 H H OCF3 OCH3 CH O H H CF3 OCH3 CH O H m-F CH3 OCH3 CH O H o-Cl CH3 OCH3 CH O H m-Br CH3 OCH3 CH O H o-CH3 CH3 OCH3 CH O H m-CF3 CH3 OCH3 CH O H o-SCH3 CH3 OCH3 CH O H m-OCH3 CH3 OCH3 CH O H o-OCF2H CH3 OCH3 CH Table 17a (continued) W R R1 X Y Z m.p.( C) O CH3 H CH3 OCH3 CH O H H CH3 CH3 CH O H H CH3 OCH3 CH O H H OCH3 OCH3 CH O H H Cl OCH3 CH O H H CR3 OCH3 N O H H OCH3 OCH3 N Table 18a EMI126.1 EMI126.2 <tb> W <SEP> R <SEP> R1 <SEP> 2 <SEP> X <SEP> Y <SEP> Z <SEP> m.p( C) <tb> <SEP> S <SEP> H <SEP> H <SEP> CH3 <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> CR3 <SEP> CH3 <SEP> OCR2CR3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> 3 <SEP> CR3 <SEP> CH2OCH3 <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> CR3 <SEP> CR3 <SEP> NR2 <SEP> CR <tb> o <SEP> H <SEP> H <SEP> CR3 <SEP> CR3 <SEP> NHCH3 <SEP> CH <tb> <SEP> o <SEP> H <SEP> H <SEP> 3 <SEP> 3 <SEP> N(CR3)2 <SEP> CR <tb> <SEP> O <SEP> H <SEP> H <SEP> 3 <SEP> 3 <SEP> CH2CH3 <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CF3 <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> OCH2CH=CH2 <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> OCH2C=-CH <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> C <SEP> 3 <SEP> CH3 <SEP> OCH2CF3 <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> OCR2CH2OCR3 <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> CH(OCH3)2 <SEP> CH <tb> <SEP> F' <tb> <SEP> 0 <SEP> H <SEP> H <SEP> CR3 <SEP> CR3 <SEP> CR <tb> <SEP> H <tb> <SEP> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> X <SEP> CH <tb> <SEP> CH3 <tb> <SEP> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> X <SEP> CH <tb> <SEP> 0 <SEP> 0 <tb> Table 18a (continued) W R R1 R2 X Y Z m.p.( C) 0 H H CH3 CH3 H CH 0 H H CH3 CH3 CN CH 0 H H CH3 CH3 CH(OCH2CH3)2 CH 0 H H CH3 CH3 OCH2F CH 0 H H CH3 CH3 OCF3 CH 0 H H CH3 CH3 SCH2F CH 0 H H CH3 CH3 SCF3 CH 0 H H CH3 CH3 OCF2H CH 0 H H CH3 CH3 OCF2CHClF CH 0 H H CH3 CH3 OCF2CHBrF CH 0 H H CH3 CH3 OCF2CHFCF3 CH 0 H H CH3 CH3 SCF2H CH 0 H H CH3 CH3 SCF2CHClF CH 0 H H CH3 CH3 SCF2CHBrF CH 0 H H CH3 CH3 SCF2CHFCF3 CH O H H CH3 CH3 OCH3 CCH3 O H H CH3 CH3 OCH3 CCH2CH O H H CH3 CH3 OCH3 CCl O H H CH3 CH3 OCH3 CBr 0 H H CH3 F OCH3 CH 0 H H CH3 Br OCH3 CH 0 H H CH3 CH2F OCH3 CH 0 H H CH3 OCF2H OCH3 CH 0 H H CH3 OCF3 OCH3 CH 0 H H CH3 CF3 OCH3 CH O H m-F CH3 CH3 OCH3 CH O H o-Cl CH3 CH3 OCH3 CH O H m-Br CH3 CH3 OCH3 CH O H o-CH3 CH3 CH3 OCH3 CH O H m-CF3 CH3 CH3 OCH3 CH O H o-SCH3 CH3 CH3 OCH3 CH O H m-OCH3 CH3 CH3 OCH3 CH O H o-OCF2H CH3 CH3 OCH3 CH Table 18a (continued) W R R1 R2 X Y Z m.p.( C) O CH3 H H CH3 OCH3 CH O H H H CH3 CH3 CH O H H H CH3 OCH3 CH O H H H OCH3 OCH3 CH O H H H Cl OCH3 CR O H H 'H CH3 OCH3 N O H H H OCH3 OCH3 N O H H CH3 CH3 CH3 CH O H H CH3 CH3 OCH3 CH O H H CH3 OCH3 OCH3 CH O H H CH3 Cl OCH3 CH O H H CH3 CH3 OCH3 N -O H H CH3 OCH3 OCH3 N O H H CH2CH3 CH3 CH3 CH O H H CH2CH3 CH3 OCH3 CH O H H CH2CH3 OCH3 OCH3 CH O H H CH2CH3 Cl OCH3 CH O H H CH2CH3 CH3 OCH3 N O H H CH2CH3 OCH3 OCH3 N 0 H H CH2CH2CH3 OCH3 OCH3 CH 0 H H CH2CH2CH2CH3 OCH3 OCH3 CH Table 19a EMI129.1 EMI129.2 <tb> W <SEP> R <SEP> R1 <SEP> X <SEP> Y <SEP> Z <SEP> m.p.( C) <tb> S <SEP> H <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CR3 <SEP> CR <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH2OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> NH2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> NHCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> N(CH3)2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH2CH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH=CH2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2C-CH <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH2OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCH3)2 <SEP> CH <tb> m\ <tb> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> X <SEP> CH <tb> <SEP> H <tb> o <SEP> H <SEP> H <SEP> CR3 <SEP> CR <tb> <SEP> H <tb> <SEP> CH3 <tb> <SEP> l <SEP> t <SEP> 3 <tb> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> / <SEP> \0 <SEP> CH <tb> <SEP> X <tb> <SEP> H <tb> Table 19a (continued) R R1 X Y Z m.p.( C) O H H CH3 H CH O H H CH3 CN CH 0 H H CH3 CH(OCH2CH3)2 CH 0 H H CH3 OCH2F CH 0 H H CH3 OCF3 CH 0 H H CH3 SCH2F CH O H H CH3 SCF3 CH O H H CH3 OCF2H CH 0 H H CH3 OCF2CHClF CH 0 H H CH3 OCF2CHBrF CH 0 H H CH3 OCF2CHFCF3 CH 0 H H CH3 SCF2H CH 0 H H CH3 SCF2CHClF CH 0 H H CH3 SCF2CHBrF CH 0 H H CH3 SCF2CHFCF3 CH O H H CH3 OCH3 CCH3 O H H CH3 OCH3 CCH2CH3 O H H CH3 OCH3 CC1 O H H CH3 OCH3 CBr 0 H H F OCH3 CH O H H Br OCH3 CH 0 H H CH2F OCH3 CH 0 H H OCF2H OCH3 CH O H H OCF3 OCH3 CH O H H CF3 OCH3 CH O H m-F CH3 OCH3 CH O H o-Cl CH3 OCH3 CH O H m-Br CH3 OCH3 CH O H o-CH3 CH3 OCH3 CH O H m-CF3 CH3 OCH3 CH O H o-SCH3 CH3 OCH3 CH O H m-OCH3 CH3 OCH3 CH O H o-OCF2H CH3 OCH3 CH Table 19a (continued) W R R1 X Y Z m.p.( C) O CH3 H CH3 OCH3 CH O H H CH3 CR3 CH O H H CH3 OCH3 CH O H H OCH3 OCH3 CH O H H Cl OCH3 CH O H H CH3 OCH3 N O H H OCH3 OCH3 N Table 20a EMI132.1 EMI132.2 <tb> W <SEP> R <SEP> 1 <SEP> 2 <SEP> X <SEP> Y <SEP> Z <SEP> m. <SEP> p. <SEP> (OC) <tb> <SEP> u <SEP> t <SEP> MH <SEP> ou <tb> S <SEP> H <SEP> H <SEP> CR3 <SEP> OCH, <SEP> SOCH3 <SEP> 3 <tb> O <SEP> H <SEP> H <SEP> CR3 <SEP> 3 <SEP> OCR2CR3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CR3 <SEP> 3 <SEP> CH20CH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> NH2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CR3 <SEP> 3 <SEP> NHCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CR3 <SEP> N(CH3)2 <SEP> CR <tb> O <SEP> H <SEP> H <SEP> CR3 <SEP> 3 <SEP> CH2CH3 <SEP> CR <tb> O <SEP> H <SEP> H <SEP> CR3 <SEP> CR3 <SEP> CF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> OCH2CH=CH2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CR3 <SEP> OCH2C=-CH <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> OCH2CF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> OCH2CH20CH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> ou <SEP> CR3 <SEP> CH(OCH3)2 <SEP> CR <tb> <SEP> 3 <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> O <SEP> O <SEP> CR <tb> <SEP> 3 <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> CH3 <SEP> 0 <SEP> CR <tb> <SEP> 3 <SEP> 'nOXD <tb> <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH <SEP> CH <SEP> CH <SEP> CH <tb> <SEP> 3 <SEP> 3 <SEP> <SEP> X <SEP> <tb> <SEP> H <tb> Table 20a (continued) W R R1 R2 X Y Z m.p.( C) 0 H H CH3 CH3 H CH 0 H H CH3 CH3 CN CH 0 H H CH3 CH3 CH(OCH2CH3)2 CH 0 H H CH3 CH3 OCH2F CH 0 H H CH3 CH3 OCF3 CH 0 H H CH3 CH3 SCH2F CH 0 H H CH3 CH3 SCF3 CH 0 H H CH3 CH3 OCF2H CH 0 H H CH3 CH3 OCF2CHClF CH 0 H H CH3 CH3 OCF2CHBrF CH 0 H H CH3 CH3 OCF2CHFCF3 CH 0 H H CH3 CH3 SCF2H CH 0 H H CH3 CH3 SCF2CHClF CH 0 H H CH3 CH3 SCF2CHBrF CH 0 H H CH3 CH3 SCF2CHFCF3 CH O H H CH3 CH3 OCH3 CCH3 O H H CH3 CH3 OCH3 CCH2CH3 O H H CH3 CH3 OCH3 CCl O H H CH3 CH3 OCH3 CBr 0 H H CH3 F OCH3 CH 0 H H CH3 Br OCH3 CH 0 H H CH3 CH2F OCH3 CH 0 H H CH3 OCF2H OCH3 CH 0 H H CH3 OCF3 OCH3 CH 0 H H CH3 CF3 OCH3 CH O H m-F CH3 CH3 OCH3 CH O H o-Cl CH3 CH3 OCH3 CH O H m-Br CH3 CH3 OCH3 CH O H o-CH3 CH3 CH3 OCH3 CH O H m-CF3 CH3 CH3 OCH3 CH O H o-SCH3 CH3 CH3 OCH3 CH O H m-OCH3 CH3 CH3 OCH3 CH O H o-OCF2H CH3 CH3 OCH3 CH Table 20a (continued) R R1 R2 X Y Z m.p.( C) O CH3 H H CH3 OCH3 CH O H H H CH3 CH3 CH O H H H CH3 OCH3 CH O H H H OCH3 OCH3 CH O H H H Cl OCH3 CH O H H H CH3 OCH3 N O H H H OCH3 OCH3 N O H H CH3 CH3 CH3 CH O H H CH3 CH3 OCH3 CH O H H CH3 OCH3 OCH3 CH O H H CH3 Cl OCH3 CH O H H CH3 CH3 OCH3 N O H H CH3 OCH3 OCH3 N O H H CH2CH3 CH3 CH3 CH O H H CH2CH3 CH3 OCH3 CH O H H CH2CH3 OCH3 OCH3 CH O H H CH2CH3 Cl OCH3 CH O H H CH2CH3 CH3 OCH3 N O H H CH2CH3 OCH3 OCH3 N 0 H H CH2CH2CH3 OCH3 OCH3 CH 0 H H CH2CH2CH2CH3 OCH3 OCH3 CH Table 21a EMI135.1 EMI135.2 <tb> W <SEP> R <SEP> 1 <SEP> 3 <SEP> X <SEP> Y <SEP> Z <SEP> m.p.(OC) <tb> S <SEP> H <SEP> H <SEP> H <SEP> OCH <SEP> SOCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OC <SEP> 2 <SEP> 3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH2OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> NR2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> NHCH <SEP> 3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> N(CH3)2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH2CH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CF3 <SEP> CH <SEP> <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH <SEP> 3 <SEP> SCH <SEP> 3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH=CH2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2C-CH <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH <SEP> 3 <SEP> OCR2CR2OCR3 <SEP> 3 <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCH3)2 <SEP> CH <tb> <SEP> F' <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> X <SEP> CH <tb> <SEP> 3 <SEP> 0 <SEP> 0 <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> lt <SEP> CH <tb> <SEP> 3 <SEP> 0 <SEP> .0 <tb> <SEP> H <tb> <SEP> C <SEP> H, <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> ( <SEP> CH <tb> <SEP> X <tb> <SEP> H <tb> Table 21a (continued) W R R1 R3 X Y Z m.p.( C) O H H H CH3 H CH O H H H CH3 CN CH 0 H H H CH3 CH(OCH2CH3)2 CH O H H H CH3 OCH2F CH 0 H H H CH3 OCF3 CH 0 H H H CH3 SCH2F CH 0 H H H CH3 SCF3 CH 0 H H H CH3 OCF2H CH 0 H H H CH3 OCF2CHClF CH 0 H H H CH3 OCF2CHBrF CH 0 H H H CH3 OCF2CHFCF3 CH 0 H H H CH3 SCF2H CH 0 H H H CH3 SCF2CHClF CH 0 H H H CH3 SCF2CHBrF CH 0 H H H CH3 SCF2CHFCF3 CH O H H H CH3 OCH3 CCH3 O H H H CH3 OCH3 CCH2CH3 O H H H CH3 OCH3 CCl O H H H CH3 OCH3 CBr O H H H F OCH3 CH O H H H Br OCH3 CH O H H H CH2F OCH3 CH O H H CH3 OCF2H OCH3 CH 213-216 0 H H H OCF3 OCH3 CH O H H H CF3 OCH3 CH O H m-F H CH3 OCH3 CH O H o-Cl H CH3 OCH3 CH O H m-Br H CH3 OCH3 CH O H o-CH3 H CH3 OCH3 CH O H m-CF3 H CH3 OCH3 CH O H o-SCH3 H CH3 OCH3 CH O H m-OCH3 H CH3 OCH3 CH O H o-OCF2H H CH3 OCH3 CH Table 21a (continued) W R R1 R3 X Y Z m.p.( C) O CH3 H H CH3 OCH3 CH O H H H CH3 CH3 CH 221-223 O H H H CH3 OCH3 CH 234-236 O H H H OCH3 OCH3 CH O H H H Cl OCH3 CH 243-246 O H H H CH3 OCH3 N 202-205 O H H H OCH3 OCH3 N 207-210 0 H H CH3 CH3 CH3 CH 227-229 0 H H CH3 CH3 OCH3 CH 221-223 O H H CH3 OCH3 OCH3 CH 228-230 0 H H CH3 Cl OCH3 CH 246-249 O H H CH3 CH3 OCH3 N 201-203 0 H H CH3 OCH3 OCH3 N 187-200 0 H H CH2CH3 OCH3 OCH3 CH 209-211 O H H CH2CH2CH3 OCH3 OCH3 CH 0 H H CH2CH2CH2CH3 OCH3 OCH3 CH 0 H H H CH3 CH3 N 199-202 0 H H H OCF2H OCH3 CH 216-218 0 H H Cl OCH3 OCH3 CH 0 H H Br OCH3 OCH3 CH Table 22a EMI138.1 W n R R1 R3 R4 X Y Z m.p.( C) O O H H H H CH3 CH3 CH O O H H H H CH3 OCH3 CH O O H H H H OCH3 OCH3 CH O O H H H H Cl OCH3 CH O O H H H H CH3 OCH3 N O O H H H H OCH3 OCH3 N O O H H CH3 H CH3 CH3 CH O O H H CH3 H CH3 OCH3 CH O O H H CH3 H OCH3 OCH3 CH O O H H CH3 H Cl OCH3 CH O O H H CH3 H CH3 OCH3 N O O H H CH3 H OCH3 OCH3 N O O H H CH3 CH3 CH3 CH3 CH O O H H CH3 CH3 CH3 OCH3 CH O O H H CH3 CH3 OCH3 OCH3 CH O O H H CH3 CH3 Cl OCH3 CH O O H H CH3 CH3 CH3 OCH3 N O O H H CH3 CH3 OCH3 OCH3 N O 1 H H H H CH3 CH3 CH O 1 H H H H CH3 OCH3 CH O 1 H H H H OCH3 OCH3 CH O 1 H H H H CG3 OCH3 N O 1 H H H H OCH3 OCH3 N Table 22a (continued) m.p. W n R R1 R3 R4 X Y Z ( C) O 1 H H CH3 H CH3 CH3 CH O 1 H H , CH3 H CH3 OCH@ CH O 1 H H CH3 H OCH3 OCH3 CH O 1 H H CH3 H CH3 OCH3 N O 1 H H CH3 H OCH3 OCH3 N O 1 H H CH3 CH3 CH3 CH3 CH O 1 H H CH3 CH3 CH3 OCH3 CH O 1 H H CH3 CH3 OCH3 OCH3 CH O 1 H H CH3 CH3 CH3 OCH3 N O 1 H H CH3 CH3 OCH3 OCH3 N S O H H H H OCH3 OCH3 CH O O CH3 H H H OCH3 OCH3 N O O H o-F H H OCH3 OCH3 CH O O H m-Cl H H OCH3 OCH3 CH O O H o-Br H H OCH3 OCH3 CH O O H m-CH3 H H OCH3 OCH3 CH O O H o-OCH3 H H OCH3 OCH3 CH O O H m-CF3 H H OCH3 OCH3 CH O O H H H CH2CH3 OCH3 OCH3 CH O O H H CH2CH2CH3 H OCH3 OCH3 CH O O H H H H CH3 CH3 N O O H H H H CH3 OCH2CH3 CH O O H H H H CH3 CH2OCH3 CH O 1 H H H H CH3 CH2OCH3 CH O O H H H H CH3 NH2 CH O O H H H H CH3 NHCH3 CH O O H H H H CH3 N(CH3)2 CH O O H H H H CH3 CH2CH3 CH O O H H H H CH3 CF3 CH Table 22a (continued) EMI140.1 <tb> W <SEP> n <SEP> R <SEP> R1 <SEP> P3 <SEP> 4 <SEP> X <SEP> Y <SEP> z <SEP> m.p.("C) <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH=CH2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CCR <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCR2CF3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH2OCH3 <SEP> C <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CR <SEP> (OCR3)2 <SEP> CR <tb> O <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CR3 <SEP> CR <tb> 0 <SEP> O <tb> <SEP> H <tb> O <SEP> O <SEP> R <SEP> H <SEP> H <SEP> H <SEP> OCR3 <SEP> OCH3 <SEP> CCR3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> OCR3 <SEP> OCH3 <SEP> CC2H5 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> OCR3 <SEP> OCH3 <SEP> CC1 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> OCR3 <SEP> OCH3 <SEP> CBr <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> F <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> Br <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH2F <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> OCF2H <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> OCF3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CF3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> Ç <SEP> O <SEP> CH <tb> <SEP> CR3 <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> | <SEP> 3 <SEP> CH <tb> <SEP> 0D <tb> <SEP> 0\/*0 <tb> <SEP> H <SEP> A <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CN <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCH2CH3)2 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2F <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF3 <SEP> CR <tb> 0 <SEP> 0- <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCR2F <SEP> CH <tb> Table 22a (continued) m.p. W n R R1 R3 R4 X Y Z ( C) 0 0 H H H H CH3 SCF3 CH 0 0 H H H H CH3 OCF2H CH 0 0 H H H H CH3 OCF2CHClF CH 0 0 H H H H CH3 OCF2CHBrF CH 0 0 H H H H CH3 OCF2CHFCF3 CH 0 0 H H H H CH3 SCF2H CH 0 0 H H H H CH3 SCF2CHClF CH 0 0 H H H H CH3 SCF2CHBrF CH O O H H H H CH3 SCF2CHFCF3 CH 0 O H H H CH2CH2CH3 OCH3 OCH3 CH 0 0 H H H CH2CH2CH2CH3 OCH3 OCH3 CH 0 0 H m-SCH3 H H OCH3 OCH3 CH 0 0 H o-CF2H H H OCH3 OCH3 CH 0 2 H H H H CH3 CH3 CH 0 2 H H H H CH3 OCH3 CH 0 2 H H H H OCH3 OCH3 CH 0 2 H H H H Cl OCH3 CH 0 2 H H H H CH3 OCH3 N 0 2 H H H H OCH3 OCH3 N 0 2 H H CH3 H CH3 CH3 CH 0 2 H H CH3 H CH3 OCH3 CH 0 2 H H CH3 H CH3 OCH3 CH 0 2 H H CH3 H Cl OCH3 CH 0 2 H H CH3 H CH3 OCH3 N 0 2 H H CH3 H OCH3 wH3 N 0 0 H H Cl Cl OCH3 OCH3 CH 0 O H H Br Br OCH3 OCH3 CH Table 22b EMI142.1 n R R1 R3 R4 X Y Z m.p.( C) O O H H H H CH3 CH3 CH O O H H H H CH3 OCH3 CH O O H H H H OCH3 OCH3 CH O 0 H H H R Cl OCH3 CH O O H H H H CH3 OCH3 N O O H H H H OCH3 OCH3 N O O H H CH3 H CH3 CH3 CH O O H H CH3 H CH3 OCH3 CH O O H H CH3 H OCH3 OCH3 CH O O H H CH3 H Cl OCH3 CH O O H H CH3 H CH3 OCH3 N O O H H CH3 H OCH3 OCH3 N O O H H CH3 CH3 CH3 CH3 CH O O H H CH3 CH3 CH3 OCH3 CH O O H H CH3 CH3 OCH3 OCH3 CH O O H H CH3 CH3 Cl OCH3 CH O O H H CH3 CH3 CH3 OCH3 N O O H H CH3 CH3 OCH3 OCH3 N O 1 H H H H CH3 CH3 CH O 1 H H H H CH3 OCH3 CH O 1 H H H H OCH3 OCH3 CH 0 1 H H H H CH3 OCH3 N 0 1 H H H H OCH3 OCH3 N Table 22b (continued) m.p. W n R R1 R3 R4 X Y Z ( C) O 1 H H CH3 H CH3 CH3 CH O 1 H H CH3 H CH3 OCH3 CH O 1 H H CH3 H CH3 OCH3 CH O 1 H H CH3 H CH3 OCH3 N O 1 H H CH3 H OCH3 OCH3 N O 1 H H CH3 CH3 CH3 CH3 CH O 1 H H CH3 CH3 CH3 OCH3 CH O 1 H H CH3 CH3 OCH3 OCH3 CH O 1 H H CH3 CH3 CH3 OCR3 N O 1 H H CH3 CH3 OCH3 OCH3 N S O H H H H OCH3 OCH3 CH O O CH3 H H H OCH3 OCH3 N O O H o-F H H OCH3 OCH3 CH O O H m-Cl H H OCH3 OCH3 CH O O H o-Br H H OCH3 OCH3 CH O O H m-CH3 H H OCH3 OCH3 CH O O H o-OCH3 H H OCH3 OCH3 CH O O H m-CF3 H H OCH3 OCH3 CH O O H H H CH2CH3 OCH3 OCH3 CH O O H H CH2CH2CH3 H OCH3 OCH3 CH O O- H H H H CH3 CH3 N O O H H H H CH3 OCH2CH3 CH O O H H H H CH3 CH2OCH3 CH O 1 H H H H CH3 CH2OCH3 CH O O H H H H CH3 NH2 CH O O H H H H CH3 NHCH3 CH O O H H H H CH3 N(CH3)2 CH O O H H H H CH3 CH2CH3 CH O O H H H H CH3 CF3 CH Table 22b (continued) EMI144.1 <tb> W <SEP> n <SEP> R <SEP> R1 <SEP> R3 <SEP> R4 <SEP> X <SEP> Y <SEP> Z <SEP> m.p. <SEP> (DC) <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2Cn-CH2 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2ClCH <SEP> CR <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCR2CF3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH2OCH3 <SEP> CH <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCR3)2 <SEP> CR <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> C'O <SEP> CH <tb> <SEP> H <tb> <SEP> 3 <SEP> 'H <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CCR3 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CC2H, <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> OCH <SEP> 3 <SEP> OCH <SEP> 3 <SEP> CC1 <tb> O <SEP> O <SEP> H <SEP> H <SEP> H- <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CBr <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> F <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> Br <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CR2F <SEP> OCH <SEP> 3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> OCF2H <SEP> OCH <SEP> 3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> OCF3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CF3 <SEP> OCH <SEP> 3 <SEP> CR <tb> 0 <SEP> 'O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH <SEP> 3 <SEP> CR <tb> <SEP> 3 <SEP> 0 <SEP> 0 <tb> <SEP> HX <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> ( <SEP> CH <tb> <SEP> O <SEP> O <tb> <SEP> HX <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CN <SEP> CR <tb> O <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCH2CH3)2 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2F <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF3 <SEP> CH <tb> 0 <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCH2F <SEP> CH <tb> Table 22b (continued) m.p. W n R R1 R3 R4 X Y Z ( C) 0 0 H H H H CH3 SCF3 CH 0 0 H H H H CH3 OCF2H CH O O H H H H CH3 OCF2CHClF CH O O H H H H CH3 OCF2CHBrF CH 0 0 H H H H CH3 OCF2CHFCF3 OH O O H H H H CH3 SCF2H CH O O H H H H CH3 SCF2CHClF CH 0 0 H H H H CH3 SCF2CHBrF CH 0 0 H H H H CH3 SCF2CHFCF3 CH 0 0 H H H CH2CH2CH3 OCH3 OCH3 CH 0 0 H H H CH2CH2CH2CH3 OCH3 OCH3 CH 0 0 H m-SCH3 H H OCH3 OCH3 CH 0 0 H o-CF2H H H OCH3 OCH3 CH 0 2 H H H H CH3 CH3 CH 0 2 H H H H CH3 OCH3 CH 0 2 H H H H OCH3 OCH3 CH 0 2 H H H H Cl OCH3 CH 0 2 H H H H CH3 OCH3 N 0 2 H H H H OCH3 OCH3 N 0 2 H H CH3 H CH3 CH3 CH 0 2 H H CH3 H CH3 OCH3 CH 0 2 H H CH3 H OCH3 OCH3 CH 0 2 H H CH3 H Cl OCH3 CH 0 2 H H CH3 H CH3 OCH3 N 0 2 H H CH3 H OCH3 OCH3 N 0 0 H H Cl Cl OCH3 OCH3 CH 0 0 H H Br Br OCH3 OCH3 CH Table 23a EMI146.1 EMI146.2 <tb> W <SEP> R <SEP> 1 <SEP> 3 <SEP> X <SEP> Y <SEP> z <SEP> m.p.("C) <tb> S <SEP> H <SEP> H <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH2OCH3 <SEP> CR <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> NH2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> NHCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> N <SEP> (CR3)2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH2CH3 <SEP> CR <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH=CH2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2C=-CH <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH2OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CR(OCH3)2 <SEP> CK <tb> <SEP> Im <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> O <SEP> O <SEP> CH <tb> <SEP> 00 <tb> O <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> n <SEP> CH <tb> <SEP> HX <tb> <SEP> CH3 <tb> 0 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> o <SEP> O <SEP> CH <tb> <SEP> H <tb> Table 23a (continued) W R R1 R3 X Y Z m.p.( C) O H H H CH3 H CH O H H H CH3 CN CH 0 H H H CH3 CH(OCH2CH3)2 CH 0 H H H CH3 OCH2F CH 0 H H H CH3 OCF3 CH 0 H H H CH3 SCH2F CH 0 H H H CH3 SCF3 CH 0 H H H CH3 OCF2H CH 0 H H H CH3 OCF2CHClF CH 0 H H H CH3 OCF2CHBrF CH 0 H H H CH3 OCF2CHFCF3 CH 0 H H H CH3 SCF2H CH 0 H H H CH3 SCF2CHClF CH 0 H H H CH3 SCF2CHBrF CH 0 H H H CH3 SCF2CHFCF3 CH O H H H CH3 OCH3 CCH3 O H H H CH3 OCH3 CCH2CH3 O H H H CH3 OCH3 CC1 O H H H CH3 OCH3 CBr o H H H F OCH3 CH 0 H H H Br OCH3 CH 0 H H H CH2F OCH3 CH 0 H H H OCF2H OCH3 CH O H H H OCF3 OCH3 CH 0 H H H CF3 OCH3 CH O H m-F H CH3 OCH3 CH O H o-Cl H CH3 OCH3 CH O H m-Br H CH3 OCH3 CH O H o-CH3 H CH3 OCH3 CH O H m-CF3 H CH3 OCH3 CH O H o-SCH3 H CH3 OCH3 CH O H m-OCH3 H CH3 OCH3 CH O H o-OCF2H H CH3 OCH3 CH Table 23a (continued) W R R1 R3 X Y Z m.p.( C) O CH3 H H CH3 OCH3 CH O H H H CH3 CH3 CH O H H H CH3 OCH3 CH O H H H OCH3 OCH3 CH O H H H Cl OCH3 CH O H H H CH3 OCH3 N O H H H OCH3 OCH3 N 0 H H CH3 OCH3 OCH3 CH 0 H H CH2CH3 OCH3 OCH3 CH 0 H H CH2CH2CH3 OCH3 OCH3 CH 0 H H CH2CH2CH2CH3 OCH3 OCH3 CH 0 H H Cl OCH3 OCH3 CH 0 H H Br OCH3 OCH3 CH Table 24a EMI149.1 W R R1 R4 R5 X Y Z m.p.( C) O H H CH3 H CH3 CH3 CH 233-237 OH H CH3 H CH3 OCH3 CH 198-205 O H H CH3 H C13 OCR3 CH 204-207 O H H CH3 H CH3 CH3 N 212-217 O H H CH3 H CH3 OCH3 N 208-212 OH H CH3 H OCH3 OCH3 N 212-215 O H H CH3 CH3 CH3 CH3 CH O H H CH3 CH3 CH3 OCH3 CH O H H CH3 CH3 OCH3 OCH3 CH O H H CH3 CH3 Cl OCH3 CH O H H CH3 CH3 CH3 OCH3 N O H H CH3 CH3 OCH3 OCH3 N S H H CH3 H OCH3 OCH3 CH O CH3 H CH3 H CH3 OCH3 CH 140-143 O H o-F CH3 H OCH3 OCH3 CH O H m-Cl CH3 H OCH3 OCH3 CH O H o-Br CH3 H OCH3 OCH3 CH O H m-CH3 CH3 H OCH3 OCH3 CH O H o-OCH3 CH3 H OCH3 OCH3 CH O H m-CF3 CH3 H OCH3 OCH3 CH O H H CH3 CH2CH3 OCH3 OCH3 CH O H H CH2CH2CH3 H OCH3 OCH3 CH O H H CH3 H CH3 CH3 N O H H CH3 H CH3 OCH2CH3 CH Table 24a (continued) EMI150.1 <tb> W <SEP> R <SEP> 1 <SEP> 4 <SEP> s <SEP> X <SEP> Y <SEP> Z <SEP> m,p. <SEP> (OC) <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CR2OCR3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> NH2 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> NHCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> N(CH3)2 <SEP> CR <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CR2CH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> 8CH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> OCH2CH=CH2 <SEP> CR <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> OCH2C=CH <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> <SEP> 2 <SEP> 3 <SEP> CR <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> OCR2CR2OCH3 <SEP> CR <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CH(OCH3)2 <SEP> CH <tb> 0 <SEP> H <SEP> H <SEP> CR3 <SEP> H <SEP> CR3 <SEP> CR <tb> O <SEP> H <SEP> H <SEP> CH3 <tb> <SEP> / <SEP> H <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CCR3 <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CC2H5 <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CC1 <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> OCH3 <SEP> OCH3 <SEP> CBr <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> F <SEP> OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> Br <SEP> OCH3 <SEP> CR <tb> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH2F <SEP> OCH3 <SEP> CH <tb> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> OCF2H <SEP> OCH3 <SEP> CH <tb> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> OCF3 <SEP> OCH3 <SEP> CH <tb> OH <SEP> H <SEP> CH3 <SEP> H <SEP> CF3 <SEP> OCH3 <SEP> CH <tb> 0 <SEP> ) <SEP> H <SEP> CR3 <SEP> H <SEP> CR3 <SEP> CR <tb> <SEP> HY <tb> <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH3 <SEP> CR3 <SEP> CH <tb> <SEP> X <tb> <SEP> H <tb> Table 24a (continued) W R R1 R4 R5 X Y Z m.p.( C) 0 H H CH3 H CH3 H CH O H H CH3 H CH3 CN CH 0 H H CH3 H CH3 CH(OCH2CH3)2 CH 0 H H CH3 H CH3 OCH2F CH 0 H H CH3 H CH3 OCF3 CH 0 H H CH3 H CH3 SCH2F CH 0 H H CH3 H CH3 SCF3 CH 0 H H CH3 H CH3 OCF2H CH 0 H H CH3 H CH3 OCF2CHClF CH 0 H H CH3 H CH3 OCF2CHBrF CH 0 H H CH3 H CH3 OCF2CHFCF3 CH 0 H H CH3 H CH3 SCF2H CH 0 H H CH3 H CH3 SCF2CHClF CH 0 H H CH3 H CH3 SCF2CHBrF CH 0 H H CH3 H CH3 SCF2CHFCF3 CH 0 H H H CH2CH2CH3 OCH3 OCH3 CH 0 H H H CH2CH2CH2CH3 OCH3 OCH3 CH 0 H m-SCH3 CH3 H OCH3 OCH3 CH 0 H o-CF2H CH3 H OCH3 OCH3 CH Table 25a EMI152.1 W R R1 R6 R7 X Y Z m.p.( C) O H H H H CH3 CH3 CH O H H H H CH3 OCH3 CH O H H H H OCH3 OCH3 CH O H H H H Cl OCH3 CH O H H H H CH3 OCH3 N O H H H H OCH3 OCH3 N O H H CH3 H CH3 CH3 CH O H H H CH3 CH3 OCH3 CH O H H CH3 H OCH3 OCH3 CH O H H H CH3 Cl OCH3 CH O H H CH3 H CH3 OCH3 N O H H H CH3 OCH3 OCH3 N O H H CH3 CH3 CH3 CH3 CH O H H CH3 CH3 CH3 OCH3 CH O H H CH3 CH3 OCH3 OCH3 CH O H H CH3 CH3 Cl OCH3 CH O H H CH3 CH3 CH3 OCH3 N O H H CH3 CH3 OCH3 OCH3 N O H H H H CH3 OCH2CH3 CH O H m-F H H CH3 CH2OCH3 CH O H o-Cl H H CH3 NH2 CH O H m-Br H H CH3 NHCH3 CH O H o-CH3 H H CH3 N(CH3)2 CH O H m-OCH3 H H CH3 C2H5 CH O H o-CF3 H H CH3 CF3 CH Table 25a (continued) EMI153.1 <tb> w <SEP> 6 <SEP> R1 <SEP> P6 <SEP> P7 <SEP> X <SEP> :n'p. <tb> O <SEP> H <SEP> m-SCH3 <SEP> H <SEP> H <SEP> CH3 <SEP> sCH3 <SEP> CH <tb> Q <SEP> H <SEP> o-OCF2H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CHiCH2 <SEP> CH <tb> O <SEP> H <SEP> o-OCF2H <SEP> H <SEP> H <SEP> CH3 <SEP> OCR2CICH <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCR2CF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CR2OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCH3)2 <SEP> CR <tb> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> o <SEP> O <SEP> CR <tb> <SEP> H <tb> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> no <SEP> CH <tb> <SEP> C)33 <tb> <SEP> CH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH <tb> <SEP> O <SEP> 0 <tb> <SEP> aY <tb> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH <tb> 0 <SEP> H <SEP> H <SEP> H <SEP> K <SEP> CH3 <SEP> CN <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH(oCH2CH3)2 <SEP> CH <tb> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2F <SEP> CH <tb> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF3 <SEP> CH <tb> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCH2F <SEP> CH <tb> O <SEP> HH <SEP> H <SEP> H <SEP> CH3 <SEP> SCF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> cH3 <SEP> OCF2H <SEP> CH <tb> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHC1F <SEP> CH <tb> 0 <SEP> RH <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHBrF <SEP> CH <tb> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CRFCF3 <SEP> CH <tb> O <SEP> RH <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2H <SEP> CH <tb> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHC1F <SEP> CH <tb> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CRBrF <SEP> CH <tb> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHFCF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH2F <SEP> CH3 <SEP> CH <tb> Table 25a (continued) R R1 R6 R7 X Y Z m.p.( C) O H H H H F OCH3 CH O H H H H Br OCH3 CH O H H H H OCF2H CH3 CH O H H H H OCF3 CH3 CH O H H H H CF3 CH3 CH S H H H H OCH3 OCH3 CH O CH3 H H H OCH3 OCH3 N O H H H H CH@ CH@ CR O H H H H CH3 OCH3 CH O H H H H OCH3 OCH3 CH O H H H H Cl OCH3 CH O H H H H CH3 OCH3 N O H H H H OCH3 OCH3 N O H H CH3 H CH3 CH3 H O H H H CH3 CH3 OCH3 CH O H H CH3 H OCH3 OCH3 CH O H H H CH3 Cl OCH3 CH O H H CH3 H CH3 OCH3 N O H H H CH3 OCH3 OCH3 N O H H CH3 CH3 CH3 CH3 CH O H H CH3 CH3 CH3 OCH3 CH O H H CH3 CH3 OCH3 OCH3 CH O H H CH3 CH3 Cl OCH3 CH O H H CH3 CH3 CH3 OCH3 N O H H CH3 CH3 OCH3 OCH3 N O H H H H CH3 CH3 CH O H H H H CH3 OCH3 CH O H H H H OCH3 OCH3 CH O H H H H Cl OCH3 CH O H H H H CH3 OCH3 N O H H H H OCH3 OCH3 N Table 25 EMI155.1 W R R1 R6 R7 X Y 2 m.p.( C) O H H H H CH3 CH3 CH O H H H H CH3 OCH3 CH O H H H H OCH3 OCH3 CH O H H H H Cl OCH3 CH O H H H H CH3 OCH3 N O H H H H OCH3 OCH3 N O H H CH3 H CH3 CH3 CH O H H H CH3 CH3 OCH3 CH O H H CH3 H OCH3 OCH3 CH O H H H CH3 Cl OCH3 CH O H H CH3 H CH3 OCH3 N O H H H CH3 OCH3 OCH3 N O H H CH3 CH3 CH3 CH3 CH O H H CH3 CH3 CH3 OCH3 CH O H H CH3 CH3 OCH3 OCH3 CH O H H CH3 CH3 Cl OCH3 CH O H H CH3 CH3 CH3 OCH3 N O H H CH3 CH3 OCH3 OCH3 N O H H H H CH3 OCH2CH3 CH O H m-F H H CH3 CH2OCH3 CH O H o-Cl H H CH3 NH2 CH O H m-Br H H CH3 NHCH3 CH O H o-CH3 H H CH3 N(CH3)2 CH O H m-OCH3 H H CH3 C2H5 CH O H o-CF3 H H CH3 CF3 CH Table 25b (continued) EMI156.1 <tb> <SEP> R <SEP> R <SEP> R <SEP> > P <tb> <SEP> W <SEP> R <SEP> 1 <SEP> P6 <SEP> P7 <SEP> X <SEP> Y <SEP> Z <SEP> ( C) <tb> <SEP> I <SEP> (Oc) <tb> <SEP> O <SEP> H <SEP> m-SCH3 <SEP> H <SEP> H <SEP> CH3 <SEP> 6CH3 <SEP> CH <tb> <SEP> O <SEP> H <SEP> o-OCF2H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CHsCH2 <SEP> CH <tb> <SEP> O <SEP> H <SEP> o-OCF2H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2C=CH <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CF3 <SEP> CH <tb> ¯¯¯0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH2OCH3 <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CH <SEP> (OCH3) <SEP> 2 <SEP> CH <tb> <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> <SEP> X <SEP> <SEP> CH <tb> <SEP> CH <tb> <SEP> RX <tb> <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> <SEP> X <SEP> <SEP> CR <tb> <SEP> H <tb> <SEP> CH3 <tb> <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CR <tb> <SEP> 0 <SEP> 0 <tb> <SEP> LI <tb> <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CR3 <SEP> H <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> CN <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CR3 <SEP> CH(OCH2CH3) <SEP> 2 <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2F <SEP> CH <tb> <SEP> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF3 <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCH2F <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF3 <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2H <SEP> CH <tb> <SEP> r0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHC1F <SEP> -CR <tb> <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHBrF <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CRFCF3 <SEP> CH <tb> <SEP> O <SEP> RH <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2H <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CRClF <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CRBrF <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CRFCF3 <SEP> CH <tb> <SEP> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH2F <SEP> CH3 <SEP> CH <tb> Table 25b (continued) R1 R6 R7 X Y Z m.p.( C) O H H H H F OCH3 CH O H H H H Br OCH3 CH O H H H H OCF2H CH3 CH O H H H H OCF3 CH3 CH O H H H H CF3 CH3 CH S H H H H OCH3 OCH3 CH O CH3 H H H OCH3 OCH3 N O H H H H CH3 CH3 CH O H H H H CH@ OCR3 CH O H H H H OCH3 OCH3 CH O H H H H Cl OCH3 CH O H H H H CH3 OCH3 N O H H H H OCH3 OCH3 N 0 H H CH3 H CH3 CH3 CH O H H H CH3 CH3 OCH3 CH O H H CH3 H OCH3 OCH3 CH O H H H CH3 Cl OCH3 CH O H H CH3 H CH3 OCH3 N O H H H CH3 OCH3 OCH3 N O H H CH3 CH3 CH3 CH3 CH O H H CH3 CH3 CH3 OCH3 CH O H H CH3 CH3 OCH3 OCH3 CH O H H CH3 CH3 Cl OCH3 CH O H H CH3 CH3 CH3 OCH3 N O H H CH3 CH3 OCH3 OCH3 N O H H H H CH3 CH3 H O H H H H CH3 OCH3 CH O H H H H OCH3 OCH3 CH O H H H H Cl OCH3 CH O H H H H CH3 OCH3 N O H H H H OCH3 OCH3 N Table 26 EMI158.1 W R R1 R2 R6 R7 X Y Z m.p.( C) O H H H H H CH3 CH3 CH O H H H H H CH3 OCH3 CH O H H H H H OCH3 OCH3 CH O H H H H H Cl OCH3 CH O H H H H H CH3 OCH3 N O H H H- H H OCH3 OCH3 N O H H H CH3 H CH3 CH3 CH O H H H H CH3 CH3 OCH3 CH O H H H CH3 H OCH3 OCH3 CH O H H H H CH3 Cl OCH3 CH O H H H CH3 H CH3 OCH3 N O H H H H CH3 OCH3 OCH3 N O H H H CH3 CH3 CH3 CH3 CH O H H H CH3 CH3 CH3 OCH3 CH O H H H CH3 CH3 OCH3 OCH3 CH O H H H CH3 CH3 Cl OCH3 CH O H H H CH3 CH3 CH3 OCH3 N O H H H CH3 CH3 OCH3 OCH3 N O H H H H H CH3 OCH2CH3 CH O H m-F H H H CH3 CH2OCH3 CH O H o-Cl H H H CH3 NH2 CH O H m-Br H H H CH3 NHCH3 CH O H o-CH3 H H H CH3 N(CH3)2 CH O H m-OCH3 H H H CH3 C2H5 CH O H o-CF3 H H H CH3 CF3 CH Table 26 (continued) EMI159.1 WP <SEP> R <SEP> P2 <SEP> P6 <SEP> R7 <SEP> RazzX <SEP> Y <SEP> 2 <SEP> m.p. <tb> ¯¯ <SEP> (Oc) <tb> O <SEP> H <SEP> m-SCH3 <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> sCH3 <SEP> CH <tb> O <SEP> H <SEP> o-OCF2H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CH-CH2 <SEP> CH <tb> O <SEP> H <SEP> o-OCF2H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2C-CH <SEP> CH <tb> OHH <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCR2CF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2CR2OCH3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> H <SEP> H <SEP> R <SEP> CH3 <SEP> CR <SEP> (OCR3)2 <SEP> CH <tb> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> <SEP> X <SEP> <SEP> CH <tb> <SEP> 0 <SEP> 0 <tb> <SEP> H <tb> OHH <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> <SEP> X <SEP> <SEP> CH <tb> <SEP> CH3 <tb> 0 <SEP> H <SEP> H <SEP> H <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH <tb> <SEP> CH <tb> <SEP> 3 <tb> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> CH <tb> 0HH <SEP> CH3 <SEP> H <SEP> H <SEP> CH3 <SEP> CN <SEP> CH <tb> OHH <SEP> CH3 <SEP> H <SEP> H <SEP> CH3 <SEP> CH(OCH2CH3)2 <SEP> CH <tb> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> H <SEP> CH3 <SEP> OCH2F <SEP> CH <tb> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> H <SEP> CH3 <SEP> OCF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> H <SEP> CH3 <SEP> SCH2F <SEP> CH <tb> OHH <SEP> CH3 <SEP> H <SEP> H <SEP> CH3 <SEP> SCF3 <SEP> CH <tb> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2H <SEP> CH <tb> O <SEP> H <SEP> H- <SEP> CH3 <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHC1F <SEP> CH <tb> OHH <SEP> CH3 <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHBrF <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> H <SEP> CH3 <SEP> OCF2CHFCF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2H <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHC1F <SEP> CH <tb> 0 <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CHBrF <SEP> CH <tb> 0 <SEP> H <SEP> H <SEP> CHt <SEP> H <SEP> H <SEP> CH3 <SEP> SCF2CRFCF3 <SEP> CH <tb> O <SEP> H <SEP> H <SEP> CH3 <SEP> H <SEP> H <SEP> CR2F <SEP> CH3 <SEP> CH <tb> Table 26 (continued) R1 R2 R6 R7 X Y Z m.p.( C) O H H H H H F OCH3 CH O H H H H H Br OCH3 CH O H H H H H OCF2H CH3 CH O H H H H H OCF3 CH3 CH O H H H H H CF3 CH3 CH S H H H H H OCH3 OCH3 CH O CH3 H H H H OCH3 OCH3 N O H H CH3 H H CH3 CH3 CH O H H CH3 H H CH3 OCH3 CH O H H CH3 H H OCH3 OCH3 CH O H H CH3 H H Cl OCH3 CR O H B CH3 H H CH3 OCH3 N O H H CH3 B H OCH3 OCH3 N O H H CH3 CH3 H CH3 CH3 CH O H H CH3 H CH3 CH3 OCH3 CH O H H CH3 CH3 H OCH3 OCH3 CH O H H CH3 H CH3 Cl OCH3 CH O H H CH3 CH3 H CH3 OCH3 N O H H CH3 H CH3 OCH3 OCH3 N O H H CH3 CH3 CH3 CH3 CH3 CH O H H CH3 CH3 CH3 CH3 OCH3 CH O H H CH3 CH3 CH3 OCH3 OCH3 CH O H H CH3 CH3 CH3 Cl OCH3 CH O H H CH3 CH3 CH3 CH3 OCH3 N O H H CH3 CH3 CH3 OCH3 OCH3 N O H H CH2CH3 H H CH3 CH3 CH O H H CH2CH3 H H CH3 OCH3 CH O H H CH2CH3 H H OCH3 OCH3 CH O H H CH2CH3 H H Cl OCH3 CH O H H CH2CH3 H H CH3 OCH3 N O H H CH2CH3 H H OCH3 OCH3 N Table 27a EMI161.1 J W1 n R R1 R2 R3 R4 R5 X1 Y1 m.p.( C) J-1 - O H H CH3 - - H CH3 O 201-203 J-1 - O H H CH3 - - H OCH3 O J-1 - O H H CH3 - - H CH3 CH2 J-1 - O H H CH3 - - H OCH3 CH2 J-2 - O H H - - - H CH3 O J-2 - O H H - - - H OCH3 O J-2 - O H H - - - H CH3 CH2 J-2 - O H H - - - H OCH3 CH2 J-3 - O H H CH3 - - H CH3 O J-3 - O H H CH3 - - H OCH3 O J-3 - O H H CH3 - - H CH3 CH2 J-3 - O H H CH3 - - H OCH3 CH2 J-4 - O H H - - - H CH3 O J-4 - O H H - - - H OCH3 O J-4 - O H H - - - H CH3 CH2 J-4 - O H H - - - H OCH3 CH2 J-5 - O H H - - - H CH3 O J-5 - O H H - - - H OCH3 O J-5 - O H H - - - H CH3 CH2 J-5 - O H H - - - H OCH3 CH2 J-6 - O H H - CH3 CH3 H CH3 O J-6 - O H H - CH3 CH3 H OCH3 O J-6 - O H H - CH3 CH3 H CH3 CH2 J-6 - O H H - CH3 CH3 H OCH3 CH2 J-7 - O H H CH3 - - H CH3 O J-7 - O H H CH3 - - H OCH3 O Table 27a (continued) J W1 n R R1 R2 R3 R4 R5 X1 Y1 J-7 - O H H CH3 - - H CH3 CH2 J-7 - O H H CH3 - - H OCH3 CH2 J-8 - O H H - - - H CH3 O J-8 - O H H - - - H OCH3 O J-8 - O H H - - - H CH3 CH2 J-8 - O H H - - - H OCH3 CH2 J-9 - O H H - - - H CH3 O J-9 - O H H - - - H OCH3 O J-9 - O H H - - - H CH3 CH2 J-9 - O H H - - - H OCH3 CH2 J-10 O O H H - - - H CH3 O J-10 0 O H H 8 - - H OCH3 O J-10 O O H H - - - H CH3 CH2 J-10 O O H H - - - H OCH3 CH2 J-22 O O H H - H H - OCH3 CH2 J-23 - - H H - H H - OCH3 CH2 J-24 8 8 H H <RTI ID=162.4> - - CH3 H CH3 0 136-141 J-10 S O H H - - - H CH3 O J-10 S O H H - - - H OCH3 O J-10 S O H H - - - H CH3 CH2 J-10 S O H H - - - H OCH3 CH2 Table 27b EMI163.1 J W1 n R R1 R2 R5 R6 R7 X1 Y1 m.p.( C) J-ll 0 O H H 8 - H H CH3 O J-11 O O H H - - H H OCH3 O J-ll 0 O H H 8 - H H CH3 CH2 J-11 S O H H - - H H OCH3 CH2 J-12 - O H H - H H H CH3 O J-12 - O H H - H H H OCH3 O J-12 - O H H - H H H CH3 CH2 J-12 - O H H - H H H OCH3 CH2 J-13 - - H H CH3 - - - CH3 O J-13 - - H H CH3 - - - OCH3 O J-13 - - H H CH3 - - - CH3 CH2 J-13 - - H H CH3 - - - OCH3 CH2 J-14 - - H H - - - - CH3 O J-14 - - H H - - - - OCH3 O J-14 - - H H - - - - CH3 CH2 J-14 - - H H - - - - OCH3 CH2 J-15 - - H H CH3 - - - CH3 O J-15 - - H H CH3 - - - OCH3 O J-15 - - H H CH3 - - - CH3 CH2 J-15 - - H H CH3 - - - OCH3 CH2 J-16 - - H H - - - - CH3 O J-16 - - H H - - - - OCH3 O J-16 - - H H - - - - CH3 CH2 J-16 - - H H - - - - OCH3 CH2 J-17 - - H H - - - - CH3 O J-17 - - H H - - - - OCH3 0 Table 27b (continued) J W1 n R R1 R2 R5 R6 R7 X1 Y1 m.p.( C) J-17 - - H H - - - - CH3 CH2 J-17 - - H H - - - - OCH3 CH2 J-18 - - H H CH3 - - - CH3 O J-18 - - H H CH3 - - - OCH3 O J-18 - - H H CH3 - - - CH3 CH2 J-18 - - H H CH3 - - - OCH3 CH2 J-19 - - H H - - - - CH3 O J-19 - - H H - - - - OCH3 O J-19 - - H H - - - - CH3 CH2 J-19 - - H H - - - - OCH3 CH2 J-20 - - H H CH3 - - - CH3 O J-20 - - H H CH3 - - - OCH3 O J-20 - - H H CH3 - - - CH3 CH2 J-20 - - H H CH3 - - - OCH3 CH2 J-21 - - H H - - - - CH3 O J-21 - - H H - - - - OCH3 O J-21 - - H H - - - - CH3 CH2 J-21 - - H H - - - - OCH3 CH2 J-25 O - H H - - H H CH3 O J-25 0 8 H H - - H H OCH3 O J-25 O - H H - - H H CH3 CH2 J-25 O - H H - - H H OCH3 CH2 J-25 S - H H - - H H OCH3 O J-25 S - H H - - H H OCH3 CH2 J-26 - - H H CH3 - H H CH3 O J-26 - - H H CH3 - H H OCH3 O J-26 - - H H CH3 - H H CH3 CH2 J-26 - - H H CH3 - H H OCH3 CH2 Table 28a EMI165.1 J W1 n R R1 R2 R3 R4 R5 X1 m.p.( C) J-1 - 0 H H CH3 - - H CH3 J-1 - 0 H H CH3 - - H OCH3 J-2 - 0 H H - - - H CH3 J-2 - 0 H H - - - H OCH3 J-3 - 0 H H CH3 - - H CH3 J-3 - 0 H H CH3 - - H OCH3 J-4 - 0 H H - - - H CH3 J-4 - 0 H H - - - H OCH3 J-5 - 0 H H - - - H CH3 J-5 - 0 H H - - - H OCH3 J-6 - 0 H H - CH3 CH3 H CH3 J-6 - 0 H H - CH3 CH3 H OCH3 J-7 - 0 H H CH3 - - H CH3 J-7 - 0 H H CH3 - - H OCH3 J-8 - 0 H H - - - H CH3 J-8 - 0 H H - - - H OCH3 J-9 - 0 H H 8 - - H CH3 J-9 - 0 H H 8 - - H OCH3 J-10 0 0 H H - - - H CH3 J-10 0 0 H H - - - H OCH3 J-22 0 0 H H - H H - OCH3 J-23 - - H H - H H - OCH3 J-24 - - H H - - CH3 H OCH3 J-10 S 0 H H - - - H CH3 J-10 S 0 H H - - - H OCH3 Table 28b EMI166.1 J W1 n R R1 R2 R5 R6 R7 X1 m.p.( C) J-11 O O H H - - H H CH3 J-11 O O H H - - H H OCH3 J-12 - O H H - H H H CH3 J-12 - O H H - H H H OCH3 J-13 - O H H CH3 - - - CH3 J-13 - - H H CH3 - - - OCH3 J-14 - - H H - - - - CH3 J-14 - - H H - - - - OCH3 J-15 - - H H CH3 - - - CH3 J-15 - - H H CH3 - - - OCH3 J-16 - - H H - - - - CH3 J-16 - - H H - - - - OCH3 J-17 - - H H - - - - CH3 J-17 - - H H - - - - OCH3 J-18 - - H H CH3 - - - CH3 J-18 - - H H CH3 - - - OCH3 J-19 - - H H - - - - CH3 J-19 - - H H - - - - OCH3 J-20 - - H H CH3 - - - CH3 J-20 - - H H CH3 - - - OCH3 J-21 - - H H - - - - CH3 J-21 - - H H - - - - OCH3 J-25 O - H H - - H H CH3 J-25 O - H H - - H H OCH3 J-25 S - H H - - H H CH3 J-25 S - H H - - H H OCH3 J-26 - - H H CH3 - H H CH3 J-26 - - H H CH3 - H H OCH3 Table 29a EMI167.1 J W1 n R R1 R2 R3 R4 R5 X1 m.p.( C) J-1 - O H H CH3 - - H CH3 220-222 J-1 - O H H CH3 - - H OCH3 J-2 - O H H - - - H CH3 J-2 - O H H - - - H OCH3 J-3 - O H H CH3 - - H CH3 J-3 - O H H CH3 - - H OCH3 J-4 - O H H - - - H CH3 J-4 - 0 H H - - - H OCH3 J-5 - O H H - - - H CH3 J-5 - O H H - - - H OCH3 J-6 - O H H - CH3 CH3 H CH3 J-6 - O H H - CH3 CH3 H OCH3 J-7 - O H H CH3 - - H CH3 J-7 - O H H CH3 - - H OCH3 J-8 - O H H - - - H CH3 J-8 - O H H - - - H OCH3 J-9 - O H H - - - H CH3 J-9 - O H H - - - H OCH3 J-10 O O H H - - - H CH3 J-10 O O H H - - - H OCH3 J-22 O O H H - H H - OCH3 J-23 - - H H - H H - OCH3 J-24 - - H H - - CH3 H OCH3 Table 29b EMI168.1 J W1 n R R1 R2 R5 R6 R7 X1 m.p.( C) J-11 O O H H - - H H CH3 J-ll 0 O H H - - H H OCH3 J-12 - O H H - H H H CH3 J-12 - O H H - H H H OCH3 J-13 - - H H CH3 - - - CH3 J-13 - - H H CH3 - - - OCH3 J-14 - - H H - - - - CH3 J-14 - - H H - - - - OCH3 J-15 - - H H CH3 - - - CH3 J-15 - - H H CH3 - - - OCH3 J-16 - - H H - - - - CH3 J-16 - O H H - - - - OCH3 J-17 O O H H - - - H CH3 J-17 O O H H - - - H OCH3 J-18 O O H H CH3 - - - CH3 J-18 - - H H CH3 - - - OCH3 J-19 - - H H - - - - CH3 J-19 - - H H - - - - OCH3 J-20 - - H H CH3 - - - CH3 J-20 - - H H CH3 - - - OCH3 J-21 - - H H - - - - CH3 J-21 - - H H - - - - OCH3 J-25 O - H H - - H H CH3 J-25 O - H H - - H H OCH3 J-26 - - H H CH3 - H H CH3 J-26 - - H H CH3 - H H OCH3 Table 30a EMI169.1 J W1 n R R1 R2 R3 R4 R5 X1 Y2 m.p.( C) J-1 - O H H CH3 - - H CH3 CH3 J-1 - O H H CH3 - - H CH3 OCH3 208-210 J-1 - O H H CH3 - - H CH3 OCH2CH3 J-1 - O H H CH3 - - H CH3 SCH3 J-2 - O H H - - - H CH3 CH3 J-2 - O H H - - - H CH3 OCH3 J-2 - O H H - - - H CH3 OCH2CH3 J-2 - O H H - - - H CH3 SCH3 J-3 - O H H CH3 - - H CH3 CH3 J-3 - O H H CH3 - - H CH3 OCH3 J-3 - O H H CH3 - - H CH3 OCH2CH3 J-3 - O H H CH3 - - H CH3 SCH3 J-4 - O H H - - - H CH3 CH3 J-4 - O H H - - - H CH3 OCH3 J-4 - O H H - - - H CH3 OCH2CH3 J-4 - O H H - - - H CH3 SCH3 J-5 - O H H - - - H CH3 CH3 J-5 - O H H - - - H CH3 OCH3 J-5 - O H H - - - H CH3 OCH2CH3 J-5 - O H H - - - H CH3 SCH3 J-6 - O H H - CH3 CH3 H CH3 CH3 J-6 - O H H - CH3 CH3 H CH3 OCH3 J-6 - O H H - CH3 CH3 H CH3 OCH2CH3 J-6 - O H H - CH3 CH3 H CH3 SCH3 J-7 - O H H CH3 - - H CH3 CH3 J-7 - O H H CH3 - - H CH3 OCH3 Table 30a (continued) J W1 n R R 1 R2 R3 R4 R5 X2 Y2 m.p. ( C) J-7 - O H H CH3 - - H CH3 OCH2CH3 J-7 - O H H CH3 - - H CH3 SCH3 J-8 - O H H - - - H CH3 CH3 J-8 - O H H - - - H CH3 OCH3 J-8 - O H H - - - H CH3 OCH2CH3 J-8 - O H H - - - H CH3 SCH3 J-9 - O H H - - - H CH3 CH3 J-9 - O H H - - - H CH3 OCH3 J-9 - O H H - - - H CH3 OCH2CH3 J-9 - O H H - - - H CH3 SCH3 J-10 O O H H - - - H CH3 CH3 J-10 O O H H - - - H CH3 OCH3 J-10 O O H H - - - H CH3 OCH2CH3 J-10 O O H H - - - H CH3 SCH3 J-22 O O H H - H H - CH3 OCH3 J-23 - - H H - H H - CH3 OCH3 J-24 - - H H - - CH3 H CH3 OCH3 Table 30b EMI171.1 J W1 n R R1 R2 R5 R6 R7 X2 Y2 m.p.( C) J-11 O O H H - - H H CH3 CH3 J-11 O O H H - - H H CH3 OCH3 J-11 O O H H - - H H CH3 OCH2CH3 J-11 O O H H - - H H CH3 SCH3 J-12 - 0 H H 8 H H H CH3 CH3 J-12 - O H H - H H H CH3 OCH3 J-12 - O H H - H H H CH3 OCH2CH J-12 - O H H - H H H CH3 SCH3 J-13 - - H H CH3 - - - CH3 CH3 J-13 - - H H CH3 - - - CH3 OCH3 J-13 - - H H CH3 - - - CH3 OCH2CH J-13 - - H H CH3 - - - CH3 SCH3 J-14 - - H H - - - - CH3 CH3 J-14 - - H H - - - - CH3 OCH3 J-14 - - H H - - - - CH3 OCH2CH J-14 - - H H - - - - CH3 SCH3 J-15 - - H H CH3 - - - CH3 CH3 J-15 - - H H CH3 - - - CH3 OCH3 J-15 - - H H CH3 - - - CH3 OCH2CH J-15 - - H H CH3 - - - CH3 SCH3 J-16 - - H H - - - - CH3 CH3 J-16 - - H H - - - - CH3 OCH3 J-16 - - - H H H - - - - CH3 OCH2CH3 J-16 - - H H - - H H CH3 SCH3 J-17 - - H H - - H H CH3 CH3 J-17 - - H H - - H H CH3 OCH3 Table 30b (continued) J W1 n R R1 R2 R5 R6 R7 X2 Y2 m.p.( C) J-17 - - H H - - - - CH3 OCH2CH3 J-17 - - H H - - - - CH3 SCH3 J-18 - - H H CH3 - - - CH3 CH3 J-18 - - H H CH3 - - - CH3 OCH3 J-18 - - H H CH3 - - - CH3 OCH2CH3 J-18 - - H H CH3 - - - CH3 SCH3 J-19 - - H H - - - - CH3 CH3 J-19 - - H H - - - - CH3 OCH3 J-19 - - H H - - - - CH3 OCH2CH3 J-19 - - H H - - - - CH3 SCH2 J-20 - - H H CH3 - - - CH3 CH3 J-20 - - H H CH3 - - - CH3 OCH3 J-20 - - H H CH3 - - - CH3 OCH2CH3 J-20 - - H H CH3 - - - CH3 SCH3 J-21 - - H H - - - - CH3 CH3 J-21 - - H H - - - - CH3 OCH3 J-21 - - H H - - - - CH3 OCH2CH3 J-21 - - H H - - - - CH3 SCH2 J-25 O - H H - - H H CH3 CH3 J-25 O - H H - - H H CH3 OCH3 J-25 O - H H - - H H CH3 OCH2CH3 J-25 O - H H - - H H CH3 SCH3 J-26 - - H H CH3 - H H CH3 CH3 J-26 - - H H CH3 - H H CH3 OCH3 J-26 - - H H CH3 - H H CH3 OCH2CH3 J-26 - - H H CH3 - H H CH3 SCH3 Table 31a EMI173.1 J W1 n R R1 R2 R3 R4 R5 X3 m.p.( C) J-1 - O H H CH3 - - H CH3 J-1 - O H H CH3 - - H OCH3 J-2 - O H H - - - H CH3 J-2 - O H H - - - H OCH3 J-3 - O H H CH3 - - H CH3 J-3 - O H H CH3 - - H OCH3 J-4 - O H H - - - H CH3 J-4 - O H H - - - H OCH3 J-5 - O H H - - - H CH3 J-5 - O H H - - - H OCH3 J-6 - O H H - CH3 CH3 H CH3 J-6 - O H H - CH3 CH3 H OCH3 J-7 - O H H CH3 - - H CH3 J-7 - O H H CH3 - - H OCH3 J-8 - O H H - - - H CH3 J-8 - 0 H H - - - 8 OCH¯ J-9 - O H H - - - H CH3 J-9 - O H H - - - H OCH3 J-10 O O H H - - - H CH3 J-10 0 0 H H - - - H OCH J-22 O O H H - H H - CH3 J-23 - - H H - H H - CH3 J-24 - - H H - - CH3 H CH3 Table 31b EMI174.1 J W1 n R R1 R2 R5 R6 R7 X3 J-11 O O H H - - H H CH3 J-11 O O H H - - H H OCH3 J-12 - O H H - H H H CH3 J-12 - O H H - H H H OCH3 J-13 - - H H CH3 - - - CH3 J-13 - - H H CH3 - - - OCH3 J-14 - - H H - - - - CH3 J-14 - - H H - - - - OCH3 J-15 - - H H CH3 - - - CH3 J-15 - - H H CH3 - - - OCH3 J-16 - - H H - - - - CH3 J-16 - - H H - - - - OCH3 J-17 - - H H - - - - CH3 J-17 - - H H - - - - OCH3 J-18 - - H H CH3 - - - CH3 J-18 - - H H CH3 - - - OCH3 J-19 - - H H - - - - CH3 J-19 - - H H CH3 - - - OCH3 J-20 - - H H CH3 - - - CH3 J-20 - - H H - - - - OCH3 J-21 - - H H - - - - CH3 J-21 - - H H - - - - OCH3 J-25 O - H H - - H H CH3 J-25 O - H H - - H H OCH3 J-26 - - H H CH3 - H H CH3 J-26 - - H H CH3 - H H OCH3 Formulations Useful formulations of the compounds of Formula I can be prepared in conventional ways. They include dusts, granules, pellets, solutions, suspensions, emulsions, wettable powders, emulsifiable concentrates and the like. Many of these may be applied directly. Sprayable formulations can be extended in suitable media a-nd used at spray volumes of from a few liters to several hundred liters per hectare. High strength compositions are primarily used as intermediates for further formulation. The formulations, broadly, contain about 0.1% to 99% by weight of active ingredient(s) and at least one of (a) about 0.1% to 20% surfactant(s) and (b) about 18 to 99.9% solid or liquid inert diluent(s). More specifically, they will contain these ingredients in the following approximate proportions: Table 32 Weight Percent* Active Ingredient Diluent(s) Surfactant(s) Wettable Powders 20-90 0-74 1-10 Oil Suspensions, 3-50 40-95 0-15 Emulsions, Solutions, (including Emulsifiable Concentrates) Aqueous Suspension 10-50 40-84 1-20 Dusts 1-25 70-99 0-5 Granules and Pellets 0.1-95 5-99.9 0-15 High Strength 90-99 0-10 0-2 Compositions * Active ingredient plus at least one of a Surfactant or a Diluent equals 100 weight percent. Lower or higher levers of active ingredient can, of course, be present depending on the intended use and the physical properties of the compound. Higher ratios of surfactant to active ingredient are sometimes desirable, and are achieved by incorporation into the formulation or by tank mixing. Typical solid diluents are described in Watkins, et al., "Handbook of Insecticide Dust Diluents and Carriers", 2nd Ed., Dorland Books, Caldwell, New Jersey, but other solids, either mined or manufactured, may be used. The more absorptive diluents are preferred for wettable powders and the denser ones for dusts. Typical liquid diluents and solvents are described in Marsden, "Solvents Guide,"- 2nd Ed., Interscience, New York, 1950. Solubility under 0.1% is preferred for suspension concentrates; solution concentrates are preferably stable against phase separation at OOC. "McCutcheon's Detergents and Emulsifiers Annual", MC Publishing Corp., Ridgewood, New Jersey, as well as Sisely and Wood, "Encyclopedia of Surface Active Agents", Chemical Publishing Co., Inc., New York, 1964, list surfactants and recommended uses. All formulations can contain minor amounts of additives to reduce foaming, caking, corrosion, microbiological growth, etc. The methods of making such compositions are well known. Solutions are prepared by simply mixing the ingredients. Fine solid compositions are made by blending and, usually, grinding as in a hammer or fluid energy mill. Suspensions are prepared by wet milling (see, for example, Littler, U.S. Patent 3,060,084) Granules and pellets may be made by spraying the active material upon preformed granular carriers or by agglomeration techniques. See J. E. Browning, "Agglomeration", Chemical Engineering, December 4, 1967, gp. 147ff. and "Perry's Chemical Engineer's Handbook , 5th Ed., McGraw-Hill, New York, 1973, pp. 8-57ff. For further information regarding the art of formulation, see for example: H. M. Loux, U.S. Patent 3,235,361, February 15, 1966, Col. 6, line 16 through Col. 7, line 19 and Examples 10 through 41; R. W. Luckenbaugh, U.S. Patent 3,309,192, March 14, 1967, Col. 5, line 43 through Col. 7, line 62 and Examples 8, 12, 15, 39, 41, 52, 53, 58, 132, 138-140, 162-164, 166, 167 and 169-182; H. Gysin and E. Knusli, U.S. Patent 2,891,855, June 23, 1959, Col. 3, line 66 through Col. 5, line 17 and Examples 1-4; G. C. Klingman, "Weed Control as a Science", John Wiley and Sons, Inc., New York, 1961, pp. 81-96; and J. D. Fryer and S. A. Evans, "Weed Control Handbook", 5th Ed., Blackwell Scientific Publications, Oxford, 1968, pp. 101-103. In the following examples, all parts are by weight unless otherwise indicated. Example 10 Wettable Powder N-1(4-chloro-6-methoxypyrimidin-2-yl)aminocarbonyl]- 2,3-dihydro-2-methyl-1,2-benzisothiazole-7-sulfon- amide, l,l-dioxide 80% sodium alkylnaphthalenesulfonate 2% sodium ligninsulfonate 2% synthetic amorphous silica 3% kaolinite 13% The ingredients are blended, hammer-milled until all the solids ar essentially under 50 microns, reblended, and packaged. Example 11 Wettable Powder N ,6-dimethoxypyrimidin-2-ylXaminocarbonyl]-2,3- dihydro-2-methyl-1, 2-benzisothiazole-7-sulfonamide, 1,1-dioxide 50% sodium alkylnaphthalenesulfonate 2% low viscosity methyl cellulose 2% diatomaceous earth 46% The ingredients are blended, coarsely hammermilled and then air-milled to produce particles essentially all below 10 microns in diameter. The product is reblended before packaging. Example 12 Granule Wettable Powder of Example 11 5% attapulgite granules 95% (U.S.S. 20-40 mesh; 0.84-0.42 mm) A slurry of wettable powder containing ¯ 25% solids is sprayed on the surface of attapulgite granules in a double-cone blender. The granules are dried and packaged. Example 13 Extruded Pellet N-lf4-methoxy-6-methylpyrimidin-2-yl)aminocarbOnyl]- 2,3-dihydro-2-propyl-1,2-benzisothiazole-7-sulfon- amide, 1,1-dioxide 25% anhydrous sodium sulfate 10% - crude calcium ligninsulfonate 5% sodium alkylnaphthalenesulfonate 1% calcium/magnesium bentonite 59% The ingredients are blended, hammer-milled and then moistened with about 12% water. The mixture is extruded as cylinders about 3 mm diameter which are cut to produce pellets about 3 mm long. These may be used directly after drying, or the dried pellets may ,be crushed to pass a U.S.S. o. 20 sieve (0.84 mm openings). The granules held on r Us.s. No. 40 sieve (0,42 mm openings) may be packaged for use and the fines recycled. Example 14 Oil Suspension N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl] 3,4-dihydro-2-meth1-2H-1,2-benzothiazine-8-ulfon- amide, l,l-dioxide 25% polyoxyethylene sorbitol hexaoleate 5% highly aliphatic hydrocarbon oil 70% The ingredients are ground together in a sand mill until the solid particles have been reduced to under about 5 microns. The resulting thick suspension may be applied directly, but preferably after being extended with oils or emulsified in water. Example 15 Wettable Powder N-1(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]- 2,3-dihydro-2-(1-methylethyl)-1,2-benzisothiazole- 7-sulfonamide, l,l-dioxide 20% sodium alkylnaphthalenesulfonate 4% sodium ligninsulfonate 4% low viscosity methyl cellulose 3% attapulgite 69% The ingredients are thoroughly blended. After grinding in a hammer-mill to produce particles essentially all below 100 microns, the material is re blended and sifted through a U.S.S. No. 50 sieve (0.3 mm opening) and packaged. Example 16 Low Strength Granule N-l(4,6-dimethoxypyrimidin-2-yl)aminocarbonylJ-1,3- dihydro-3-oxoisobenzofuran-4-sulfonamide 14 N,N-dimethylformamide 9% attapulgite granules 90% (U.S.S. 20-40 sieve) The active ingredient is dissolved in the solvent and the solution is sprayed upon dedusted granules in a double cone blender. After spraying of the solution has been completed, the blender is allowed to run for a short period and then the granules are packaged. Example 17 Aqueous Suspension N-lt4-methoxy-6-methyl-1,3,5-triazin-2-yl)aminocar- bonyll-2,3-dihydro-2-(1-methylethyl)-1,2-benziso- thiazole-7-sulfonamide, 1, l-dioxide 40% polyacrylic acid thickener 0.3% dodecylphenol polyethylene glycol ether 0.58 disodium phosphate 1% monosodium phosphate 0.5% polyvinyl alcohol 1.0% water 56.7% The ingredients are blended and ground together in a sand mill to produce particles essentially all under 5 microns in size. Example 18 Solution N-l(4-methoxy-6-methyl-1,3,5-triazin-2-yl)aminocar bonyll-2,3-dihydro-2-methyl-1,2-benzisothiazole- 7-sulfonamide, l,l-dioxide, sodium salt 5% water 95% The salt is added directly to the water with stirring to produce the solution, which may then be packaged for use. Example 19 Low Strength Granule N-l(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyll 1,3-dihydro-2-methyl-l-oxo-l-isoindole- amide, 0.1% attapulgite granules 99.98 (U.S.S. 20-40 mesh) The active ingredient is dissolved in a solvent and the solution is sprayed upon dedusted granules in a double-cone blender. After spraying of the solution has been completed, the material is warmed to evaporate the solvent. The material is allowed to cool and then packaged. Example 20 Granule N-1(4-methoxy-6-methyl-1,3,5-triazin-2-yl)aminocar- bonyll-2,3-dihydro-2-ethyl-1,2-ben2isothiazole-7- sulfonamide, l,l-dioxide 80% wetting agent 18 crude ligninsulfonate salt (containing 10% 5-20% of the natural sugars) attapulgite clay 9% The ingredients are blended and milled to pass through a 100 mesh screen. This material is then added to a fluid bed granulator, the air flow is adjusted to gently fluidize the material, and a fine spray of water is sprayed onto the fluidized material. The fluidization and spraying are continued until granules of the desired size range are made. The spraying is stopped, but fluidization is continued, optionally with heat, until the water content is reduced to the desired level, generally less than 1%. The material is then discharged, screened to the desired size range, generally 14-100 mesh (1410-149 microns), and packaged for use. Example 21 High Strength Concentrate N-l(4-chloro-6-methoxypyrimidin-2-yl)amirlocarbonyl]- 2,3-dihydro-2-methyl-l,2-benzisothiazole-7-sulfon- amide, l,l-dioxide 99% silica aerogel 0.58 synthetic amorphous silica 0.5t The ingredients are blended and ground in a hammer-mill to produce a material essentially all passing a U.S.S. No. 50 screen (0.3 mm opening). The concentrate may be formulated further if necessary. Example 22 Wettable Powder N-[(4-chloro-6-methoxypyrimidin-2-yl)aminocarbonyl] 2, 3-dihydro-2-methyl-1 ,2-benzisothiazole-7-sulfon- amide, l,l-dioxide 90% dioctyl sodium sulfosuccinate 0.1% synthetic fine silica 9.98 The ingredients are blended and ground in a hammer-mill to produce particles essentially all below 100 microns. The material is sifted through a U.S.S. No. 50 screen and then packaged. Example 23 Wettable Powder N-t(4,6-dimethoxypyrimidin-2-yl)aminocarbonyll-2,3- dihydro-2-methyl-l,2-benzisothiazole-7-sulfonamide, l,l-dioxide 40% sodium ligninsulfonate 20% montmorillonite clay 40% The ingredients are thoroughly blended, coarsely hammer-milled and then air-milled to produce particles essentially all below 10 microns in size. The material is reblended and then packaged. Example 24 Oil Suspension N-1(4-methoxymethyl-6-methylpyrimidin-2-ylsaminocar- bonyll-2,3-dihrdro-2-methyl-1,2-benzisothiazole-7- sulfonamide, l,l-dioxide 35% blend of polyalcohol carboxylic 6% esters and oil soluble petroleum sulfonates xylene 59% The ingredients are combined and ground together in a sand mill to produce particles essentially all below 5 microns. The product can be used directly, extended with oils, or emulsified in water. Utility Test results indicate that the compounds of the present invention are active herbicides. They should have utility for broad-spectrum pre- and/or post-emergence weed control in areas where complete control of all vegetation is desired, such as around fuel storage tanks, ammuni-tion depots, industrial storage areas, parking lots, drive-in theaters, around billboards, highway and railroad structures, or on fallow land. Alternatively, some of the subject compounds should be useful for the selective pre- or post-emergence weed control in crops, especially wheat, cotton and soybeans. The rates of application for the compounds of the invention are determined by a number of factors, including their use as selective or general herbicides, the crop species involved, the types of weeds to be controlled, weather and climate, formulations selected, mode of application, amount of foliage present, etc. In general terms, the subject compounds should be applied at levels of around 0.001 to 5 kg/ha, the lower rates being suggested for use on lighter soils and/or those having a low organic matter content, for selective weed control or for situations where only- short-term persistence is required. The compounds of the invention may be used in combination with any other commercial herbicide; exam ples of which are those of the triazine, triazole, --uracil, utea,-----tnride1- diphenylether, carbamate and bipyridylium types. They also may be used in combina- tion with me flu idide. The herbicidal properties of the subject com pounds were discovered in a number of greenhouse tests. The test procedures and results follow. Test A Seeds- of-vrabg-rass (Digitaria sp.), barnyard grass (Echinochloa crusgalli), wild oats (Avena fatua), sicklepod (Cassia obtusifolia), morningglory (Ipomoea sp.), cocklebur (Xanthium pensylvanicum), sorghum, corn, soybean, sugar beet, rice, wheat, pur ple nutsedge (Cyperus rotundus) tubers, and in certain cases, cotton were planted and treated pre-emergence with the test chemicals dissolved in a non-phytotoxic solvent. At the same time, these crop and weed spe cies, along with cotton and bush bean, were treated with a soil/foliage application. At the time of treatment, the plants ranged in height from 2 to 18 cm. Treated plants and controls were maintained in a greenhouse for sixteen days, after which all species were compared to controls and visually rated for response to treatment. The ratings, summarized in Table A, are based on a numerical scale extending from o = no injury, to 10 = complete kill. The accompany ing descriptive symbols have the following meanings: C = chlorosis/necrosis; E g emergence inhibition; G - growth retardation; H - formative effects; L s lodging; U = unusual pigmentation; X = axillary stimulation; and 6Y = abscised flowers or buds. The data show that most of the compounds tested are highly active herbicides with growth modifying properties and that some of the compounds tested provide selective weed control in crops such as wheat, cotton and soybeans. Compounds Compound 1 Compound 2 Compound 3 Compound 4 EMI186.1 Compounds (continued) Compound 5 Compound 6 Compound 7 Compound 8 EMI187.1 Compounds (continued) Compound 9 Compound 10 Compound 11 Compound 12 EMI188.1 Compounds (continued) Compound 13 Compound 14 Compound 15 Compound 16 EMI189.1 Compounds (continued) Compound 17 Compound 18 Compound 19 Compound 20 EMI190.1 Compounds (continued) Compound 21 Compound 22 Compound 23 Compound 24 EMI191.1 Compounds (continued) Compound 25 Compound 26 Compound 27 Compound 28 EMI192.1 Compounds (continued) Compound 29 Compound 30 Compound 31 Compound 32 EMI193.1 Compounds (continued) Compound 33 Compound 34 Compound 35 Compound 36 EMI194.1 Compounds (continued) Compound 37 Compound 38 Compound 39 Compound 40 EMI195.1 Compounds (continued) Compound 41 Compound 42 Compound 43 Compound 44 EMI196.1 Compounds (continued) Compound 45 Compound 46 Compound 47 Compound 48 EMI197.1 Compounds (continued) Compound 49 Compound 50 Compound 51 Compound 52 EMI198.1 Compounds (continued) Compound 53 Compound 54 Compound 55 Compound 56 EMI199.1 Compounds (continued) Compound 57 Compound 58 Compound 59 EMI200.1 Compounds (continued) Compound 60 Compound 61 Compound 62 EMI201.1 Compounds (contined) Compound 63 Compound 64 Compound 65 Compound 66, EMI202.1 Compounds (continued) Compound 67 Compound 68 Compound 69 Compound 70 EMI203.1 Compounds (continued) Compound 71 Compound Compound 73 Compound 74 EMI204.1 Compounds (continued) Compound 75 Compound 76 Compound 77 Compound 78 EMI205.1 Table A Cmpd. 1 Cmpd. 2 Cmpd. 3 Cmpd. 4 Rate g/ha 50 50 50 50 POST-EMERGENCE Bush bean 6C,9G,6Y 9C 4C,8G,6Y 4C,7G,6Y Cotton 5C,9G 6C,9G 4C,5H 2C,3H Morningglory 6C,9G 10C 2C,5G 1C Cocklebur 6C,9G 9C 2C,7G 4G Sicklepod 4C,9G 9C 2C,5G 3C,8G Nutsedge 9C 9C 6G 8G Crabgrass 9C 9C 2G 2C,7G Barnyardgrass 9C 9C 5C,9H 9C Wild Oats 9C 9C 3C,9G 9C Wheat 9C 9C 9C 4C,9G Corn 9C 9C 6C,9G 9C Soybean 5C,9G 6C,9G 3C,9G 3C,8H Rice 6C,9G 6C,9G 3C,9G 5C,9G Sorghum 5C,9G 9C 2C,9G 2C,9G Sugar beet 9C 9C 3C,9G 4C,9G PRE-EMERGENCE Morningglory 9G 9C 3H 2G Cocklebur 9H 9H 3G 2G Sicklepod 8G 9G 8G 7G Nutsedge 10E 10E 0 0 Crabgrass 3G 5C,9G 0 0 Barnyardgrass 2C,7H 6C,9H 2C 1C Wild Oats 5C,8H 6C,9H 2C,8G 2C,8G Wheat 5C,9G 10H 2C,9G 8G Corn 5C,9G 10E 4C,9G 2C,9G Soybean 4C,3H 9H 1C,2G 0 Rice 10E 10E 10E 10E Sorghum 5C,9H 6C,9H 4C,9G 2C,9G Sugar beet 5C,9G 6C,9G 8G 4C,9G Table A (continued) Cmpd. 5 Cmpd. 6 Cmpd. 7 Cmpd. 8 Rate g/ha 50 50 50 50 POST-EMERGENCE Bush bean 9C 9C 5C,9G,6Y SC,9G,6Y Cotton 6C,9G 9C 5C,9G 2C,2H Morningglory 9C 10C 5C,9G 2C,4G Cocklebur 9C 10C 9C 1C,3G Sicklepod 9C 9C 5C,8G 3C Nutsedge 10C 10C 3C,9G 5C,9G Crabgrass 9C 9C 6C,9G 2C,5G Barnyardgrass 9C 9C 9C 5C,9H Wild Oats 9C 4C,9G 9C 5C,9G Wheat 9C 9C 9C '9C Corn 9C 9C 5U,9C 3U,9G Soybean 6C,9G 3C,9G 5C,9G 4C,9G Rice 9C 6C,9G 5C,9G 5C,9G Sorghum 10C 9C 4C,9G 2C,9G Sugar beet 9C 9C 9C 2C,8G PRE-EMERGENCE Morningglory 9C 9C 9C 1C Cocklebur 9H 9H 9H 2C,8G Sicklepod 9C 9G 9G 3G Nutsedge 10E lOE 10E 3G Crabgrass 6C,9G 5C,9G 2C,5G 1C,9G Barnyardgrass 6C,9H 6C,9H 2C,9G 2C Wild Oats 6C,9H 5C,9G 4C,9G 2C,7G Wheat 10H 3C,9G 9H 2C,8G Corn 10H 4C,9H 5C,9H 2C,7H Soybean 9H 6H 4C,5H 1C Rice 10E 10E 10E 5C,9H Sorghum 10H 6C,9H 5C,9H 2C,5G Sugar beet 9C 10E 5C,9G 7G Table A (continued) Cmpd. 9 Cmpd. 10 Cmpd. 11 Cmpd. 12 Rate g/ha 50 50 50 50 POST-EMERGENCE Bush bean - - - Cotton 4C,9H 5C,9G 9C 4C,8G Morningglory 4C,8H 10C 9C 5C,9H Cocklebur 3C,7H 9C 10C 2C,5G Sicklepod 3C,7H 9C 9C 3C,5H Nutsedge 2C,8G 4C,9G 2C,9G 5G Crabgrass 4C,9G 9C 9C 2C,5G Barnyardgrass 5C,9G 9C 9C 5C,9H Wild Oats 9C 9C 9C 6C,9G Wheat 10C 10C 9C 5C,9G Corn 5C,9G 10C 10C 5U,9G Soybean 2C,9G,5X 5C,9G 9C 3C,8G,5X Rice 6C,9G 9C 6C,9G 5C,9G Sorghum 4C,9H 9C 9C 5C,9G Sugar beet 4C,8H 9C 9C 9C PRE-EMERGENCE Morningglory 3C,8H 9C 10E 7H Cocklebur 2C,3H 9H 9H 0 Sicklepod 2C 9G 9G 7G Nutsedge 5C,8G 10E 10E 2G Crabgrass 5C,9G 9C 6C,9G 0 Barnyardgrass 5C,9H 5C,9H 10H 4C,5G Wild Oats 10C 9C 6C,9H 2C,9G Wheat 10C 10C 10E 5C,9G Corn 2U,8G 5C,9H 10H 5C,9H Soybean 3C 9H 9H 1C,2H Rice 10E 10E lOE 10E Sorghum 10C 5C,9H 10E 5C,9H Sugar beet 9C 10C 10E 9C Cotton 3C,4H 9G 2C,9G 5G Table A (continued) Cmpd. 13 Cmpd. 14 Cmpd. 15 Cmpd. 16 Rate g/ha 50 50 50 50 POST-EMERGENCE Bush bean - - - Cotton 4C,9G 3C,9G 3C,9H 10C Morningllory 4C,8H 4C,8G 5C,9G 9C Cocklebur 8H 4C,9G 4C,9H 10C Sicklepod 3G 9G 5C,9G 9C Nutsedge 3C,7G 5G 9G 4C,9G Crabgrass 5C, 9G 3C,9G 6C,9G 5C,9G Barnyardgrass 9C 5C,9H 6C,9G 9C Wild Oats 2C,9G 9C 6C,9G 9C Wheat 5C,9G 9C 9C 9C Corn 10C 4U,9G 5U,9C 9C Soybean 2C,6G 5C,9G 5C,9G 9C Rice 5C,9G 3C,9G 5C,9G 5C,9G Sorghum 9C 2C,9G 5C,9G 4U,9C Sugar beet 9C 5C,9G 9C 9C PRE-EMERGENCE Morningglory 9C 9G 2C,6H 9H Cocklebur 9H 8H 2C,3H 9H Sicklepod 8G 8G 8G 9C Nutsedge 10E 10E 10E 10E Crabgrass 5C,9G 4C,8G 5C,8G 5C,9G Barnyardgrass 10H 2C,8H 9H 9H Wild Oats 5C,9G 2C,8G 5C,8H 5C,9H Wheat 4C,9G 2C,8G 4C,9H 9H Corn 5C,9H 8G 3C,9G 5C,9H Soybean 2C,3G 1C,1H 2C,4G 9H Rice 10E 10E 10E 10E Sorghum 7C,9H 2C,9G 4C,9H 5C,9H Sugar beet 9C 3C,9G 4C,9G 10E Cotton 8G 2G 3G <RTI ID=209.10> 9H Table A (continued) Cmpd. 17 Cmpd. 18 Cmpd. 19 Cmpd. 20 Rate g/ha 50 50 50 50 POST-EMERGENCE Bush bean - - - Cotton 10C 10C 10C 3C,7H Morningglory 10C 10C 10C 2C,5H Cocklebur 9C 10C 10C 2G Sicklepod 9C 9C 10C 3C,6H Nutsedge 10C 5C,9G 9C 1C,2G Crabgrass 9C 5C,9G 9C 3G Barnyardgrass 9C 9C 9C 3C,9H Wild Oats 9C 9C 5C,9G 5C,9G Wheat 9C 9C 6C,9G 5C,9G Corn 5U,9C 10C 9C 5C,9G Soybean 6C,9G 6C,9G 6C,9G 2C,2H Rice 9C 9C 6C,9G 5C,9G Sorghum 4U,9G 9C 9C 3C,9H Sugar beet 9C 9C 9C 3C,7G PRE-EMERGENCE Morningglory 9H 10E 9G 8G Cocklebur 9H 9H 9H 8H Sicklepod 9G 9C 9G 8G Nutsedge 10E 10E 3C,8G 0 Crabgrass 5C,9G 6C,9G 5C,9G 0 Barnyardgrass 6C,9H 6C,9H 6C,9H 3C,3H Wild Oats 9C 6C,9H 6C,9H 3C,9H Wheat 10E 10E 10H 2C,9H Corn 10E 10E 6C,9H 3C,9G Soybean 9H 9H 9H 3G Rice 10E 10E 10E 10E Sorghum 10E 10E 10E 5C,9H Sugar beet 10E 10E 10E 8G Cotton 5C,9G 9C 3C,9G 3G Table A (continued) Cmpd. 21 Cmpd. 22 Cmpd. 23 Cmpd. 24 Rate g/ha 50 50 50 50 POST-EMERGENCE Bush bean - - - - Cotton 9C 0 4C,9H 4C,9G Morningglory 9C 2C,5G 4C,8H 5C,9G Cocklebur 9C 3G 2C,7H 4C,9H Sicklepod 9C 0 4C,8G 2C,6G Nutsedge 9C 0 2C,8G 9C Crabgrass 6C,9G 2C,5G 4C,9G 9C Barnyardgrass 9C 5C,9H 9C 9C Wild Oats 5C,9G 9C 9C 9C Wheat 10C 2C,8G 2G 2C,5G Corn 10C 2U,8H 7U,9C 10C Soybean 5C,9G 2C,5G 5C,9G 4C,9G Rice 6C,9G 4C,9G 6C,9G 5C,9G Sorghum 9C 4C,9H 5C,9G 8C,9H Sugar beet 9C 0 0 3C,7G PRE- EMERGENCE Morningglory 9H 2C,4G 4C,8H 5C,9G Cocklebur 9H 0 5C,9H 9H Sicklepod 2C,9G 0 2C,5G 3C,9H Nutsedge 10E 0 8G 10E Crabgrass 2C,5G 2C,6G 6G 5C,9G Barnyardgrass 5C,9H 2C 3C,8H SC,9H Wild Oats 2C,9G 5C,9H 5C,9H 6C,9H Wheat 4C,9H 5G 0 2C,9G Corn 2C,9H 3C,8H 2C,9G 5C,9H Soybean 9H 2C 4C,7H 4C,8G Rice 10E 5C,9H 10E 10E Sorghum 10H 3C,6H 3C,9H 2C,9H Sugar beet 3C,9G 5G 3C,8H 9C Cotton 3C,9G 1C 6G 9G Table A (continued) Cmpd. 25 Cmpd. 26 Cmpd. 27 Cmpd. 28 Rate g/ha 50 50 50 50 POST-EMERGENCE Bush bean - - - Cotton 2C,7H 0 0 9C Morningglory 2C,4G 3G 0 9C Cocklebur 4G 3G 0 9C Sicklepod 2C,2G 3G 0 5C,9G Nutsedge 0 0 0 10C Crabgrass 2C,8G 2G 0 9C Barnyardgrass 9C 5C,9H 3C,8H 9C Wild Oats 9C 9C 3C,8G 0 Wheat 0 0 0 0 Corn 6C,9H 3U,9G 2C,8H 10C Soybean 4C,8H 0 1C 2C,7G Rice 6C,9G 5C,9G 7G 9C Sorghum 7C,9H 3C,9H 2C,6G 9C Sugar beet 1C 0 0 9C PRE-EMERGENCE Morningglory 4C,8G 0 0 9G Cocklebur 2C,5G 2C,3G 0 9H Sicklepod 2C 0 0 9G Nutsedge 8G 0 0 10E Crabgrass 3C,8G 3G 2G 5C,9G Barnyardgrass 3C,9H 2H 0 6C,9H Wild Oats 3C,8G 4G 5G 2C,5G Wheat 3C,8G 0 0 0 Corn 3C,9H 2C,7G 3G 3C,9H Soybean 3C,6H 0 0 3C,6G Rice 10E 3C,7H 2C,7G <RTI ID=212.8> 10E Sorghum 5C,9H 9H 0 10H Sugar beet 8G 0 0 10E Cotton 6G- 0 -0 9G Table A (continued) Cmpd. 29 Cmpd. 30 Cmpd. 31 Cmpd.32 Rate g/ha 50 50 50 2000 POST-EMERGENCE Bush b.ean Cotton 5C,9G 6C,9G 3C,8H 3C,9G Morningglory 9C 5C,9G 3C,7H 3C,9H Cocklebur 10C 10C 7G 3C,9H Sicklepod 9C 2C,8G 8G 3C,9G Nutsedge 10C 5C,9G 2C,5G 2C,9G Crabgrass 10C 5C,9G 4G 3C,9H Barnyardgrass 10C 9C 2C,8G 9C Wild Oats 9C 9C 2C,3G 4C,8G Wheat 9C 9C 2G 9C Corn 10C 9C 2C,6H 9C Soybean 5C,9G 5C,9G 2H 3C,9H Rice 6C,9G 6C,9G 5G 6C,9G Sorghum 9C 9C 2C,8H 2C,9G Sugar beet 9C 9C 0 3C,8G PRE-EMERGENCE Morningglory 9G 9H 8H 10C Cocklebur 2C,9H 8H 9H 9H Sicklepod 9C 9G 5C,9G 9C Nutsedge 10E 10E 7G 3G Crabgrass 9C 4C,7G 6G 0 Barnyardgrass 6C,9H SC,9H 4C,8H 4C,6H Wild Oats 6C,9H 5C,9H 9G 3C,9G Wheat 10E 5C,9H 9G 3C,9G Corn 10E 9H 3C,9H 3U,9G Soybean 9H 2C,7H 1C,3G 4G Rice 10E 10E 10E 3C,8G Sorghum 10H 10H 9H 3C,9H Sugar beet 6C,9G 5C,9G 7G 8G Cotton 9G 9G 9G 8G Table A (continued) Cmpd. 33 Cmpd. 34 Cmpd. 35 Cmpd. 36 Rate g/ha 50 50 50 50 POST-EMERGENCE Bush bean - - Cotton 1C 9C 9C 4G Morningglory 2C 4C,9H 5C,9G 2C,8G Cocklebur 1C 5C,9G 2C,8G 6G Sicklepod 0 2C,4G 2C,7G 3C,8H Nutsedge 0 4C,9G 10C 9C Crabgrass 0 0 1C 3C,9H Barnyardgrass 2C,6H 3C,8H 3C,8H 9C Wild Oats 2C,7G 3C,8G 3C,9G 3C,9G Wheat 2C,4G 5C,9G 9C 5C,9G Corn 9C 3H,5L 3H,5L 10C Soybean 0 4C,8H 4C,9G 3C,8H rice 4C,9G 5C,9G 4C,9G 3C,9G Sorghum 2C,9G 2U,9H 9G 5U,9G Sugar beet 2C,3H 9C 5C,9G 2C,9G PRE-EMERGENCE Morningglory 1C 3C,8G 2C 2C,8G Cocklebur 4H 2C,8H 2C,7H 3C,9H Sicklepod 0 8G 2G 4C,8G Nutsedge 0 0 0 10E Crabgrass 0 0 0 3C,7G Barnyardgrass 0 0 0 5C,9H Wild Oats 0 0 0 3C,9G Wheat 0 0 0 10H Corn 2C,8H 0 2G 9H Soybean 0 0 0 3C,8H Rice 2C,8H 5G 7H 10E Sorghum 8H 2C,8G 2C,9H 6C,9H Sugar beet 0 2C,8G 7H 9G Cotton 0 2G 2G 8G Table A (continued) Cmpd. 37 Cmpd. 38 Cmpd. 39 Cmpd. 40 Rate g/ha 50 50 50 50 POST-EMERGENCE Bush bean - - - Cotton 4C,8G 0 5G 0 Morningglory 2C,8H 1C 2C,3G 3H Cocklebur 2C,5G 2G 4G 4G Sicklepod 4C,4H 1C 4G 1C Nutsedge 0 0 8G 5C,9G Crabgrass 3G 2C,8G 5C,9G 9C Barnyardgrass 9C 2C,9H 10C 9C Wild Oats 9C 5C,9G 5C,9G 6C,9G Wheat 9C 9C 8G 9G Corn 6U,9C 2C,7H 5C,9G 2C,8H Soybean 4C,8G 2G 1C,3H 5G Rice 5C,9G 5C,9G 9C 9C Sorghum 4C,9G 4C,9H 9C 3C,9G Sugar beet 9C 0 4C,9H 2C,5G PRE-EMERGENCE Morningglory 8H 0 3G 2C,2H Cocklebur 9H 0 3G 6H Sicklepod 6G 0 3G 3G Nutsedge 3G 0 8G 7G Crabgrass 0 0 3C,8G 4G Barnyardgrass 3C,8H 1H 5C,9H 3C,8H Wild Oats 5C,9G 2C 3C,9G 2C,9G Wheat 3C,9G 0 7G 8G Corn 5C,9H 2G 9G 2C,8G Soybean 2C 0 1C,3G 2G Rice 10E 5G 10E 10E Sorghum 6C,9H 0 10H 5C,9H Sugar beet 4C,9G 0 7G 5G Cotton 7G 0 2G 1C Table A (continued) Cmpd. 41 Cmpd. 42 Cmpd. 43 Cmpd. 44 Rate g/ha 50 50 50 50 POST-EMERGENCE Bush bean - - Cotton 0 0 2C,5G 6C,9G Morningglory 5G 0 2G 6C,9G Cocklebur 3G 0 3G 9C Sicklepod 2G 0 2G 9C Nutsedge 3G 0 5G 3C,9G Crabgrass 3G 2G 6G 9C Barnyardgrass 4C,9H 3C,8H 2C,8H 5C,9G Wild Oats 4C,9H 3C,9H 4C,8H 9C Wheat 9C 3C,9H 9C 10C Corn 2C,8H 0 2C,9H 9C Soybean 0 0 6H 5C,9G Rice 3C,9G 9G 4C,9G 6C,9G Sorghum 3C,9H 0 3C,8H 9C Sugar beet 0 0 2C 9C PRE-EMERGENCE Morningglory 2C 0 3H 9G Cocklebur O 0 2H 9H Sicklepod 0 0 0 8G Nutsedge 0 0 0 3C,9G Crabgrass 0 0 0 5C,9G Barnyardgrass 2H 0 3G 3C,9H Wild Oats 2C,4G 2G 2G 5C,9G Wheat 8G 2G 2G 6C,9H Corn 4G 0 0 5C,9H Soybean 0 0 3G 4C,8H Rice 5G 0 0 10E Sorghum 2G 0 0 5C,9H Sugar beet 0 0 0 5C,9G Cotton - 0¯¯ 0 0 8G Table A (continued) Cmpd. 45 Cmpd. 46 Cmpd. 47 Cmpd. 48 Rate g/ha 50 50 50 50 POST-EMERGENCE Bush bean - - - - Cotton 10C 5C,9G 0 3C,8H Morningglory 5C,9G 4C,9G 1C 2C,7H Cocklebur 9C 9C 1C 3C,8H Sicklepod 9C 5C,9G 0 1C,3H Nutsedge 3C,9G 2C,8G 0 3C,8G Crabgrass 9C 2C,9G 0 2H Barnyardgrass 9C 9C 3C,7H 4C,9H Wild Oats 9C 9C 2C,5G 5C,9G Wheat 10C 10C 6G 9C Corn 9C 10C 2C,8H 2C,8H Soybean 9C 5C,9G 0 3C,6H Rice 6C,9G 5C,9G 3C,9G 6C,9G Sorghum 9C 10C 2C,8H 6H Sugar beet 9C 9C 1C 2C,5G PRE-EMERGENCE Morningglory 9H 9G 1C 0 Cocklebur 9H 8H 0 0 Sicklepod 9G 9G 0 0 Nutsedge 10E 8G 0 0 Crabgrass 5C,9G 2C,7G O 1C Barnyardgrass 9H 3C,9H 0 0 Wild Oats 5C,9H 3C,8G 0 -3C,9H Wheat 10E 4C,9H 0 9H Corn 5C,9G 5C,9H 2C,3G 3C,6H Soybean 9H 4C,5H 0 2C,3H Rice 10E 10E 2C,5G 8H Sorghum 5C,9H 4C,9H 2C,8G 2C,9H Sugar beet 5C,9G 5C,9G 1C 3C,4H Cotton 9G 8G 0 0 Table A (continued) Cmpd. 49 Cmpd. 50 Cmpd. 51 Cmpd. 52 Rate g/ha 50 50 50 50 POST-EMERGENCE Bush bean Cotton 7G 3G 3C,9H 3C,9G Morningglory 2C,5G 1H 3C,8G 9C Cocklebur 4H 2C,4G 3C,9H 9C Sicklepod 2G 2C 3C,9G 9C Nutsedge 2C,9G 2C,8G 9C 9C Crabgrass O 3C,9G 6C,9G 9C Barnyardgrass 7H 9C 9C 9C Wild Oats 3C,9H 9C 9C 9C Wheat 5C,9H 9C 9C 9C Corn 2C,5H 3U,9G 6C,9G 9C Soybean 3C,8H 2C,7G 3C,9G 9C Rice 4C,9G 5C,9G 6C,9G 9C Sorghum 2C,7H 3C,9H 4U,9G 9C Sugar beet 2C,3G 2C,6G 9C 9C PRE-EMERGENCE Morningglory 0 3H 9G 9G Cocklebur 0 1H 9H 9H Sicklepod O 0 8G 8G Nutsedge O 0 3C,8G 10E Crabgrass 0 7G 5C,9G 6C,9H Barnyardgrass 0 2G 2C,9H 5C,9H Wild Oats 0 2C,8G 5C,9H 6C,9H Wheat 0 2C,5H 5C,9H 10E Corn <RTI ID=218.9> O 3C,7G 4C,9H 4C,9H Soybean O 0 3C,6G 3C,7H Rice 0 5C,9H 10E 10E Sorghum 0 3C,7G 5C,9H 6C,9H Sugar beet 0 3G 5C,9G 6C,9G Cotton 0 0 8G 3C,9G Table A (continued) Cmpd. 53 Cmpd. 54 Cmpd. 55 Cmpd. 56 Rate g/ha 50 50 50 50 POST-EMERGENCE Bush bean - - Cotton 3C,9H 2C,7G 3C,9G 2C,8G Morningglory 3C,8G 3C,7G 5C,9G 4C,8G Cocklebur 4C,9H 3G 5C,9G 5C,9G Sicklepod 3C,7G 1C,2G 3C,8G 3C,9H Nutsedge 9C lC,3G 2C,8G 6C,9G Crabgrass 9C 2G 2G 3C,8G Barnyardgrass 10C 9C 2C,8H 4C,9H Wild Oats 9C 0 0 5C,9G Wheat 9C 9G 0 5C,9G Corn 9C 2C,9H 0 9C Soybean 4C,9G 3C,8H 5C,9G 4C,9G Rice 9 4C,9H 5G 9C Sorghum 10C 3C,6G 2C,5G 4C,9H Sugar beet 9C 5C,9G 3C,9G 9C PRE-EMERGENCE Morningglory 8G 0 0 9G Cocklebur 9H 0 0 9H Sicklepod 7G 0 0 6G Nutsedge 10E 0 0 0 Crabgrass 6C,9G 0 0 2C,3G Barnyardgrass 6C,9H 0 0 3C,4H Wild Oats 4C,9G 0 0 4C,9G Wheat 3C,8G 0 0 2C,9G Corn 3C,9H 0 0 3C,9H Soybean 5G 0 0 4C,6G Rice 10E 0 0 9H Sorghum 10H 0 0 2C,9H Sugar beet 6C,9G 0 0 5C,9G Cotton 8G 0 0 7G Table A (continued) Cmpd. 57 Cmpd. 58 Cmpd. 59 Rate g/ha 50 50 50 POST-EMERGENCE Bush bean - - Cotton 2C,8H SG 10C Morningglory 5C,9G 3C,7G 9C Cocklebur SC,9G 2C,8H 9C Sicklepod 2C,5G 6G lOC Nutsedge 2C,9G 8G 9C Crabgrass 2C,3H 7G 7G Barnyardgrass 4C,9H 3C,9H 10C Wild Oats 9C 2C,6G 4C,9G Wheat 9C 2C,6G 9C Corn 9C 3C,9H 10C Soybean 4C,9H 2H,5G 9C Rice 9C 3C,9G 9C Sorghum 4C,9G 3U,9G 10C Sugar beet 5C,9G 5G 9C PRE- EMERGENCE Morningglory 9H 8G 9G Cocklebur 2C,8H 2C,8H 9H Sicklepod 1C 8G 5C,9G Nutsedge 2C,6G 8G 10E Crabgrass 2C,2G 3C,6G lC,3G Barnyardgrass 2C,3H 4C,9H 5C,9H Wild Oats 5C,9H 3C,9H 5C,8G Wheat 9C 2C,8G 5C,9H Corn 9G 3C,9H 3C,9G Soybean 2C,3G 1C,6G 3C,8H Rice 5C-9H 10E 10E Sorghum 5C,9H 2C,8H 5C,9R Sugar beet 5C,9G 8G 9C Cotton 8G 8G 9G Table A (continued) Cmpd. 60 Cmpd. 61 Cmpd. 62 Rate g/ha 50 50 50 POST-EMERGENCE Bush bean Cotton 9G,2C 8G 2C,5G Morningglory 3C,8H 1C,3G 2C Cocklebur 9C 3C,9H 3C,7H Sicklepod 3C,8H 3G 2C Nutsedge 2C,8G 5G 0 Crabgrass 4C,9G 2C,8G 1H Barnyardgrass 5C,9H 5C,9H 2C,9H Wild Oats 9C 4G 0 Wheat 9C 2C,5G 10C Corn 2C,9G 2C,9G 3U,9G Soybean 3C,9G 2G 4C,9G Rice 5C,9G 5C,9G @C,9G Sorghum 5C,9H 3C,9H 2C,9H Sugar beet 5C,9G 2C,4G 3C,3H PRE-EMERGENCE Morningglory 9G 5G 2C,6G Cocklebur 2C,9H 8H 8H Sicklepod 3C,6H 4G 5G Nutsedge 5G 4G 0 Crabgrass 3C,7G 5G 0 Barnyardgrass 3C,9H 9H 2C,6H Wild Oats 4C,9G 1C,3G 2C,5G Wheat 5C,9G 2C,8G 9G Corn 2C,9G 2C,9G 9G Soybean 2C,7H 1H 2C,3G Rice 5C,9H 10E 5C,9H Sorghum 5C,9G 2C,9H 3C,9H Sugar beet 5C,9G 2C,8G 3C,8G Cotton 8G 5G 5G Table A Cmpd. 63 Cmpd. 64 Cmpd. 65 Cmpd. 66 Rate g/ha 50 50 50 50 POST-EMERGENCE Bush bean - - - Cotton - 2G 3C,9G 5C,9G 2C,7G Morningglory 2C,2H 9C 10C 2C,8G Cocklebur 3C,SG 5C,9G 5C,9G 5C,9G Sicklepod 2C 5C,9G 5C,9G 2C,8G Nutsedge 4G 4C,9G 3C,9G 9C Crabgrass 3G 2C,9G 7H 2C,7G Barnyardgrass 3C,9H 2C,9H 5C,9H 10C Wild Oats 2C,8G 3C,9G 5C,9G 1C Wheat 9C 2C,9G 5C,9G 1C Corn 5C,9G 10C 10C 10C Soybean 2C,7G 5C,9G 4C,9G 2C,8G Rice 5C,9G 6C,9G 6C,9G 5C,9G Sorghum 2C,9H 6C,9G 6C,9G 10C Sugar beet 0 5C,9G 9C 5C,9G PRE-EMERGENCE Morningglory 2C,4H 10C 5C,9G 9G Cocklebur 7H 2C,9H 4C,9H 9H Sicklepod 3C,5G 5C,9G 2C,9G 8G Nutsedge 0 9G 10E 2C,7G Crabgrass 2C 3C,8G 4C,6G 1C Barnyardgrass 2C,4H 9H 5C,9H 3C,9H Wild Oats 3C,7G 6C,9G 4C,9R 1C Wheat 9G 10E 10E 4G Corn 1C,9G 5C,9H 5C,9H 9H Soybean 2C,5G 4C,9G 2C,6H 4G Rice 5C,9H 10E 10E 10E Sorghum 2C,9G 7C,9H 10H 3C,9H Sugar beet 3G 3C,9G 9G 2C,9G Cotton 2G 9G 9G 8G Table A (continued) Cmpd. 67 Cmpd. 68 Cmpd.69 Cmpd.70 Rate g/ha 50 50 50 50 POST-EMERGENCE Bush bean - - - - Cotton 4C,9G 9C 10C 9C Morningglory 9C 9C 9C 9C Cocklebur 6C,9G 9C 9C 10C Sicklepod 5C,9G 10C 9C 10C Nutsedge 2C,8G 10C 10C 10C Crabgrass 9C 9C 9C 9C Barnyardgrass 9C 9C 9C 9C Wild Oats 0 9C 9C 9C Wheat 5C,9H 9C 9C 9C Corn 10C 10C 10C 10C Soybean 5C,9G 6C,9G 9C 9C Rice 5C,9G 9C 6C,9G 6C,9G Sorghum 10C 9C 9C 10C Sugar beet 9C 9C 9C 9C PRE-EMERGENCE Morningglory 5C,9G 9C 9C 10C Cocklebur 9H 9H 9H 9H Sicklepod 9C 9C 9C 9C Nutsedge 7G 10E 10E 10E Crabgrass 4C,9G 6C,9G 9C 9C Barnyardgrass 4C,9H 6C,9H 6C,9H 2C,9H Wild Oats 2C,5G 6C,9H 9C 7C,9H Wheat 2C,9H 10H 10H 10H Corn 3C,9H 10H 10H 10H Soybean 3C,9H 9H 4C,9H 3C,9H Rice 10E 10E 10E 10E Sorghum 7C,9H 10H 9C 10H Sugar beet 5C,9G 10C 10C 10E Cotton 9G 9C 9C 9G,4C Table A (continued) Cmpd. 71 Cmpd. 72 Cmpd. 73 Cmpd. 74 Rate g/ha 50 50 50 50 POST-EMERGENCE Bush bean - - - Cotton 9C 10C 9C 10C Morningglory 10C 6C,9G 10C 9C Cocklebur 10C 10C 10C 10C Sicklepod 9C 9C 9C 9C Nutsedge 9C 9C 9C 9C Crabgrass 9C 10C 10C 10C Barnyardgrass 9C 9C 9C 9C Wild Oats 9C 9C 6C,9G 9C Wheat 10C 10C 6C,9G 9C Corn 10C 10C 10C 10C Soybean 9C 9C 6C,9G 6C,9G Rice 6C,9G 9C 9C 9C Sorghum 9C 9C 10C 10C Sugar beet 9C 9C 10C 9C PRE-EMERGENCE Morningglory 9C 9H 9C 9C Cocklebur 9H 9H 4C,9G 9H Sicklepod 9C 9C 9C 9C Nutsedge 5C,9G 10E 9G 9G Crabgrass 9C 9C 9C 4C,9G Barnyardgrass 5C,9H 5C,9H 9C 5C,9H Wild Oats 10C 6C,9H 6C,9G 9C Wheat 10H 10H 10E 10C Corn 5C,9H 9C 10E 5C,9H Soybean 3C,9H 9H 9H 8H Rice 10E 10E 10E 10E Sorghum 10H 10H 9C 10H Sugar beet 10C 10C 10E 6C,9G Cotton 10C 9G 9G 9C Table A (continued) Cmpd. 75 Cmpd. 76 Cmpd. 77 Cmpd. 78 Rate g/ha 50 50 50 50 POST-EMERGENCE Bush bean - - - Cotton 9C 1C 2C,8H 4C,9H Morningglory 4C,8H 5G 3C,9G 4C,9G Cocklebur 9C 5G 3C,8H 4C,9H Sicklepod 9C 3C,6G 4C,9G 5C,9G Nutsedge 9C 2C 3C,7G 3C,8G Crabgrass SC,9G 2C,8H 2C,8G 9G Barnyardgrass 9C 3C,9H 9C 9C Wild Oats 5C,9G 3C,8G 2C,8G 5C,9G Wheat 6C,9G 5C,9G 2C,9G 2C,9G Corn 10C 4U,9G 10C 10C Soybean 5C,9G 3C,8G 4C,9G 4C,9G Rice 9C 4C,9G 4C,9G 6C,9G Sorghum 10C 3C,9G 4C,9G 9C Sugar beet 9C 3C,8G 9C 9C PRE-EMERGENCE Morningglory 9C 2C,7G 4C,9G 9G Cocklebur 5C,9H 9H 3C,9H 9H Sicklepod 9C 3C,8G 5C,9G 8G Nutsedge 10E 2C,5G 2C,8G 2C,9G Crabgrass 2C,5G 2C,3H 5C,9G 2C,8G Barnyardgrass 4C,9H 3C,9H 5C,9H 9H Wild Oats 9G 3C,9G 4C,9G 2C,9G Wheat 10H 2C,9G 10H 4C,9H Corn 5C,9G 2C,8G 3C,9H 2C,9H Soybean 4C,9H 2G 3C,9H 3C,7H Rice 10E 9H 10E 10E Sorghum 9C 3C,9H 10H 4C,9H Sugar beet 9C 2C,8G 9C 9C Cotton 9C 8G 9G 9G Test B Two plastic bulb pans were filled with fertilized and limed Woodstown sandy loam soil. One pan was planted with corn, sorghum, Kentucky bluegrass and several grass weeds. The other pan was planted with cotton, soybeans, purple nutsedge (Cyperus rotundus), and several broadleaf weeds. The following grass and broadleaf weeds were planted: crabgrass (Digitaria sanguinalis), barnyardgrass (Echinochloa crusgalli), wild oats (Avena fatua), johnsongrass (Sorghum halepense), dallisgrass (Paspalum dilatatum), giant foxtail (Setaria faberii), cheatgrass (Bromus secalinus), mustard (Brassica arvensis), cocklebur (Xanthium pensylvanicum), morningglory (Ipomoea hederacea), sicklepod (Cassia obtusifolia), teaweed (Sida spinosa), velvetleaf (Abutilon theophrasti), and jimsonweed (Datura stramonium). - A 12.5 cm diameter plastic pot was also filled with prepared soil and planted with rice and wheat. Another 12.5 cm pot was planted with sugar beets. The above four containers were treated pre-emergence with several test compounds within the scope of the invention. Twenty-eight days after treatment, the plants were evaluated and visually rated for response to the chemical treatments utilizing the rating system described previously for Test A. The data are summarized in Table B. Table B PRE-EMERGENCE ON WOODSTOWN SANDY LOAM Compound 1 Rate g/ha 1 4 16 62 250 Crabgrass 0 0 4G 7G 8G Barnyardgrass 0 0 2G 8G 9G Sorghum - - - - Wild Oats 0 0 2G 7G 9G Johnsongrass 0 0 8G 8G 9G Dallisgrass - - - Giant foxtail 0 0 7G 9G 9G Ky. bluegrass - - - - Cheatgrass - - - - Sugar beets 0 3G 7G 7G 9G Corn 3G 3G 9G 9G 10G Mustard - - - - Cocklebur 0 5G 7G 8G 8G Pigweed - - - - Nutsedge 6G 9G 10G 10G 10G Cotton 0 0 0 3G 9G Morningglory 0 0 6G 8G 9G Sicklepod 0 0 2G 8G 9G Teaweed 0 0 0 2G 9G Velvetleaf 0 1G 6G 6G 9G Jimsonweed 0 0 6G 9G 9G Soybean 0 0 2G 1G 9G Rice 8G 9G 10G 10G 10G Wheat 0 2G 8G 9G 9G Table B (continued) PRE-EMERGENCE ON WOODSTOWN SANDY LOAM Compound 2 Rate g/ha 1 4 16 62 250 Crabgrass 0 3G 8G 8G 9G Barnyardgrass 0 0 7G 8G 9G Sorghum - - - - Wild Oats 0 0 6G 8G 8G Johnsongrass 0 0 8G 7G 9G Dallisgrass - - - - Giant foxatil 4G 9G 9G 8G 9G Ky. bluegrass - - - - Cheatgrass - - - - Sugar beets 6G 7G 8G 9G 9G Corn 5G 8G 8G 10G 10G Mustard - - - - Cocklebur 0 7G 8G 9G 9G Pigweed - - - - Nutsedge 8G 9G 10G 10G 10G Cotton 0 0 8G 9G 9G Morningglory 0 3G 7G 9G 9G Sicklepod 0 4G 7G 9G 9G Teaweed 0 0 8G 9G 9G Velvetleaf 0 0 8G 9G 9G Jimsonweed 0 7G 8G 9G 9G Soybean 0 3G 7G 9G 9G Rice 9G 9G 10G 10G 10G Wheat 8G 9G 9G 10G 10G Table B (continued) PRE-EMERGENCE ON WOODSTOWN SANDY LOAM Compound 5 Rate g/ha 4 31 Crabgrass 10C 10C Barnyardgrass 10C 10C Sorghum 10C 10C Wild Oats 9G 9G Johnsongrass 9G 10C Dallisgrass 9G 10C Giant bluegrass 9G 10C Ky. bluegrass 10C 10C Cheatgrass 9G 10C Sugar beets 10C 10C Corn 10C 10C Mustard 8G 9G Cocklebur 6G 9G Pigweed Nutsedge 10C 10C Cotton 7G 9G Morningglory 9G 9G Sicklepod 7G 9G Teaweed 6G 9G Velvetleaf 6G 9C Jimsonweed 8G 9G Soybean 7G,5H 9G Rice 10C 10C Wheat 10C 10C Test C The test chemicals, dissolved in a non-phytotoxic solvent, were applied in an overall spray to the foliage and surrounding soil of selected plant species. One day after treatment, plants were observed for rapid burn injury. Approximately fourteen days after treatment, all species were visually compared to untreated controls and rated for response to treatment. The rating system was as described previously for Test A. The data are presented in Table C. All plant species were seeded in Woodstown sandy loam soil and grown in a greenhouse. The following species were grown in soil contained in plastic pots (25 cm diameter by 13 cm deep): soybeans, cotton, corn, rice, wheat, velvetleaf (Abutilon theophrasti), sesbania (Sesbania exaltata), sicklepod (Cassia obtusifolia), morningglory (Ipomoea hederacea), jimsonweed (Datura stramonium), cocklebur (Xanthium pensylvanicum), crabgrass (Digitaria sp.), nutsedge (Cyperus -rotundus), barnyardgrass (Echinochloa crusgalli), giant foxtail (Setaria faberii) and wild oats (Avena fatua). Sugar beets were grown separately in soil in a paper cup (12 cm diameter by 13 cm deep). All plants¯ were sprayed approximately 14 days after planting. Additional plant species are sometimes added to this standard test in order to evaluate unusual selectivity. Table C Over-the-Top Soil/Foliage Tratment Compound 1 Rate g/ha 1 4 16 62 Soybeans 2G 0 10C 10C Velvetleaf 0 8C 9G 9C Sesbania 2G 2G 7G 7G Sicklepod 2G 4G 4G 9G Cotton 3G 3G 4G 7G Morningglory 3G 8G 9G 10G Alfalfa - - - Jimsonweed 0 0 - Cocklebur 2G 2G 9G 10G Sunflower - - - Mustard - - Sugar beets 8G 10G 10C 10C Corn 6U 10C 10C 10C Crabgrass 0 4G 7G 8G Rice 3C 7G 8C 8C Nutsedge 5H 6G 6C 6G Barnyardgrass 5G 8C 10G 10C Wheat 2G 4G 6C 7C Giant foxtail 3G 6G 6G 7G Wild Oats 2G 6G 8G 9C Sorghum - - Johnsongrass 6U 9U 10C 10C Field Bindweed - - Table C (continued) Over-the-Top Soil/Foliage Treatment Compound 2 Rate g/ha 1 4 16 62 Soybeans 8G 10G 10G 10G Velvetleaf 0 9G 9C 9C Sesbania 5G 7G 8G 10C Sicklepod 5G 7G 9G 10G Cotton 0 8G 9G 10G Morningglory 7G 9G 9G 10G Alfalfa - - - Jimsonweed 0 - - Cocklebur 0 5G 10G 10C Sunflower - - - Mustard - - - Sugar beets 7G 10G 10C 10C Corn 7C 10C 10C 10U Crabgrass 2G 7G 9C 8C Rice 5G 8C 9C 8G Nutsedge 0 1G 2G 5C Barnyardgrass 6G - 9C 9C Wheat 3G 4G 5G 6C Giant foxtail 4G 7G 8G 7C Wild Oats 6G 6G 8C 7G Sorghum - - - Johnsongrass 8U 10U 10U 10U Field Bindweed - - - Table C (continued) Over-the-Top Soil/Foliage Treatment Compound 5 Rate g/ha 1 4 4 16 16 62 Soybeans 8G 10G 10C 10G 10C 10C Velvetleaf 8G 10G 9C 10G 10C 10C Sesbania - - - - - Sicklepod 6G 10G 9G 10G 10C 10C Cotton 7G 10G 10C 10G 10C 10C Morningglory 5G 9G 8G 10G 9G 10C Alfalfa - - - - - Jimsonweed 7G 10G 9C 10G 10C 10C Cocklebur 5G 7G 9C 10G 10C 10C Sunflower - - - - - Mustard - - - - - Sugar beets 10G 10G 10C 10G 10C 10C Corn 9G 10G 9C 10G 9C 10C Crabgrass 8G 10G 9G 10G 10C 10C Rice 6G 10G 9C 10G 9C 10C Nutsedge 0 8G 7G 10G 7G 8G Barnyardgrass 8G 10G 10C 10G 10C 10C Wheat 8G 9G 7G 10G 7G 8G Giant foxtail 8G 9G 10C 10G 10C 10C Wild Oats 7G 9G 7G 10G 8C 8G Sorghum - - - - - Johnsongrass 10G 10G 10C 10G 10C 10C Field bindweed - - - - - Table C (continued) Over-the-Top Soil/Foliaqe Treatment Compound 6 Rate g/ha 1 4 16 62 Soybeans 2G 8G 9G 10G Velvetleaf 4G 8G 9C 9G Sesbania 6G 7G 8G 10G Sicklepod 2G 6G 9G 10G Cotton 0 3G 7G 10G Morningglory 2G 6G 9G 10G Alfalfa - - - Jimsonweed 0 3G 8G Cocklebur 0 0 5G 10C Sunflower - - - - Mustard - - - - Sugar beets 5G 10C 10G 10C Corn 6C 9G 10U 10U Crabgrass 0 3G 7G 8G Rice 3G 6G 8C <RTI ID=234.6> 8C Nutsedge 0 0 4G 4G Barnyardgrass 6C 9G 9G 9G Wheat 0 0 0 4G Giant foxtail 0 0 5G 6G Wild Oats 0 0 0 5G Sorghum - - - - Johnsongrass 10U 10U 10U 10U Field Bindweed - - - Table C (continued) Over-the-Top Soil/Foliage Treatment Compound 7 Rate g/ha 1 4 16 62 Soybeans 0 4G 10G 10G Velvetleaf 1C 5C 8G 8G Sesbania 2G 4G 7G 8G Sicklepod 2G 8G 8G Cotton 3G 7G 7G 9G Morningglory 0 4G 8G 9G Alfalfa - - - Jimsonweed 0 7G - Cocklebur 0 3G 6G Sunflower - - - Mustard Sugar beets 3G 7C 10G 10G Corn 4G 7U 10U 10U Crabgrass 0 2G 7G 8G Rice 3G 8G 8C 8C Nutsedge 0 0 4G 3G Barnyardgrass 4G 6G 9G 9G Wheat 1G 6G 7C 7C Giant foxtail 3G 5G 7C 8G Wild Oats 0 4G 7G 8G Sorghum - - - Johnsongrass 8U 9U 10C 10C Field Bindweed - - - Test D Post-emergence phase Two round pans (25 cm diameter by 12.5 cm deep) were filled with Woodstown sandy loam soil. One pan was planted with sugar beets, nutsedge (Cyperus rotundus) tubers, crabgrass (Digitaria sanguinalis), sicklepod (Cassia obtusifolia), teaweed (Sida spinosa), jimsonweed (Datura stramonium), velvetleaf (Abutilon theophrasti), and giant foxtail (Setaria faberii). The other pan was planted with wheat, cotton, rice, corn, soybean, wild oats (Avena fatua), cocklebur (Xanthium pensylvanicum), morningglory (Ipomoea hederacea), johnsongrass (Sorghum halepense) and barnyardgrass (Echinochloa crusgalli). The plants were grown for approximately fourteen days, then sprayed post-emergence with the chemicals dissolved in a non-phytotoxic solvent. Pre-emergence phase Two round pans (25 cm diameter by 12.5 cm deep) were filled with Woodstown sandy loam soil. One pan was planted with sugar beets, nutsedge, crabgrass, sicklepod, teaweed, jimsonweed, velvetleaf and giant foxtail. The other pan was planted with wheat, cotton, rice, corn, soybeans, wild oats, cocklebur, morningglory, johnsongrass and barnyardgrass. The two pans were sprayed pre-emergence with the chemicals dissolved in a non-phytotoxic solvent. Treated plants and controls were maintained in the greenhouse for 28 days, then all treated plants were compared to controls and visually rated for response utilizing the rating system as described above for Test A. The data are given in Table D. It will be seen that the compounds tested have utility for weed control in cotton. Table D PRE-EMERGENCE Compound 14 Rate g/ha 4 16 62 250 Corn 0 3G 6G 8G Wheat 0 2G 8G 9G Rice 3G 8G 10G 10G Soybean 0 2G 6G 8G Cotton 0 3G 4G 6G Sugar beet 0 3G 7G 9G Crabgrass 0 5G 8G 9G Johnsongrass 0 3G 9G 9G Barnyardgrass 0 3G 8G 9G Nutsedge 0 2G 7G 9G Giant Foxtail - - - Wild Oats 0 3G 8G 8G Cocklebur 0 4G 5G 7G Morningglory 0 0 0 3G Teaweed 0 2G 6G 8G Sicklepod 0 4G 4G 5G Jimsonweed 0 0 4G 8G Velvetleaf 0 0 0 3G PRE-EMERGENCE Compound 15 Rate g/ha 4 16 62 250 Corn 0 0 0 0 Wheat 0 0 8G 10G Rice 0 6G 10G 10G Soybean 0 0 2G 4G Cotton 0 0 0 0 Sugar beet 0 0 3G 9G Crabgrass 0 7G 8G 9G Johnsongrass 0 3G 7G 8G Barnyardgrass 0 0 8G 8G Nutsedge 0 0 8G 0 Giant Foxtail 0 3G 7G 9G Wild Oats 0 4G 8G 8G Cocklebur 0 0 0 0 Morningglory 0 0 2G 5G Teaweed 0 5G 6G 6G Sicklepod 0 0 4G 9G Jimsonweed 0 0 4G 6G Velvetleaf 0 0 0 0 Table D (continued) POST-EMERGENCE Compound 14 Rate g/ha 1 4 16 62 Corn 3G 9G 10C 10C Wheat 0 3G BG 8G Rice 0 SG 9G 10G Soybean 3G 9G 9G 9G Cotton 0 2G 3G 4G Sugar beet 0 6G 10G 10G Crabgrass 0 5G 10C 10G Johnsongrass 0 5G 9C 10C Barnyardgrass 0 5G 9C 9C Nutsedge 0 0 4G 6G Giant Foxtail 0 0 3G 9G Wild Oats 0 4G 9G 9G Cocklebur 0 2G 5G 8G Morningglory 0 4G 5G 7G Teaweed 0 5G 9G 10G Sicklepod 0 3G 7G 8G Jimsonweed 0 3G 7G 10G Velvetleaf 0 3G 3G 8G POST-EMERGENCE Compound 15 Rate g/ha 1 4 16 62 Corn 0 6G 10G 10G Wheat 0 0 10G 10G Rice 3G 8G 10G 10G Soybean 0 7G 10G 10G Cotton 0 0 0 0 Sugar beet 0 4G 10G 10C Crabgrass 3G 7G 10C 10C Johnsongrass 0 3G 10C 10C Barnyardgrass 0 7G 9C 10C Nutsedge 0 0 5G 6G Giant Foxtail 0 3G 8G 10C Wild Oats 0 5G 9C 10C Cocklebur 0 0 0 5G Morningglory 0 0 7G 8G Teaweed 0 0 3G 10C Sicklepod 0 5G 10G 10C Jimsonweed 0 0 0 5G Velvetleaf 0 0 7G 8G Test E This test was conducted to evaluate compounds for potential utility in fallow weed control. Plastic pots lined with polyethylene bags were filled with Woodstown sandy loam and planted to kochia (Kochia scoparia) and Russian thistle (Salsola kali). About 10 days later, seeds of wheat (Triticum aestivum), wild oats (Avena fatua), cheatgrass (Bromus secalinus) and green foxtail (Setaria lutescens) were planted in the same pots. After an additional 10 days, wheat, barley, corn and sorghum were planted. Immediately after the last planting, the test chemical, dissolved in a non-phytotoxic solvent, was applied to the soil surface and the foliage of the emerged plants. Twenty one days after treatment, all species were rated utilizing the rating system as described for Test A. The response data are summarized in Table E. It will be seen that all species are killed or seriously injured at very low rates of application of compound No. 5, regardless of whether the treatments were applied pre- or post-emergence. Table E Compound 5 Rate g/ha 4 1 Post-Emergence Russian thistle 10C 10C Kochia 10C 2G Cheatgrass 6G 1G Green foxtail 9G,9C 2G Wild Oats 9G 4G Volunteer Wheat 8G,2C 2G Pre-Emergence Wheat 8G,8C 4G Barley 10C 6G Corn 4G 1G Sorghum 10C 5G

Claims: Claims: 1. A compound of the formula: EMI240.1 wherein J is EMI240.2 EMI241.1 EMI242.1 n is 0, 1 or 2; W is O or S; W1 is O or S; R is H or CH3; R1 is X, F, C1, Br, CH3, OCH3, CF3, SCH3 or OCF2H; R2 is H or C1-C4 alkyl; R3 and R4 are independently H, C1-C4 alkyl, Cl or Br; R5 is H or CH3; R6 is H or CH3; R7 is H or CH3; A is EMI243.1 EMI243.2 X is CH3, OCH3, OCH2CH3, C1, F, Br, OCF2H, CH2F or CF3; Y is H, CH3, OCH3, OC2H5, CH2OCH3, NH2, NHCH3, N(CH3)2, C2H5, CF3, SCH3, OCH2CH=CH2, OCH2C=CH, OCH2CF3, CN, N3, OCH2CH2OCH3, CH2SCH3, CR6(QCH3)2, EMI243.3 EMI243.4 CR6(QCH2CH3)2 or QCF2T where Q is O or S and T is H, CHC1F, CHBrF or CHFCF3; z is CH, N, CCH3, CC2H5, CCl or CBr; Y1 is O or CH2; X1 is CH3, OCH3, OC2H5 or OCF2H; X2 is CH3, C2R5 or CH2CF3; ; Y2 is OCH3, OC2H5, SCH3, SC2H5, CH3 or CH2CH3; X3 is CH3 or OCH3; provided that a) when W is S, then R is H, A is EMI244.1 Z is CH or N, and Y is CH3, OCH3, OC2H5, CH2OCH3, C2H5, CF3, SCH3, OCH2CH=CH2, OCH2C=CH, OCH2CF3, OCH2CH2OCH3, CH(OCH3)2 or EMI244.2 b) the total number of carbon atoms in R3 and R4 is less than or equal to 4; c) when X is -Cl, F or Br, then Z is CH and Y is OCH3, OC2H5, NH2, NHCH3, N(CH3)2 or OCF2H; d) when R5 is CH3, then n is 0; e) when J is J24, then P4 and P5 are not both H and $r is not Cl or Br; and their agriculturally suitable salts. 2. Compounds of Claim 1 where W is O, R2 is H or C1-C3 alkyl, R3 and P4 are independently H or C1-C3 alkyl and R1 is bonded to the ortho or meta position of the ring relative to the sulfonylurea moiety. 3. Compounds of Claim 2 where R1 is H, F, Cl, Br, CH3, OCH3, CF3 or SCH3; Y is CH3, OCH3, OC2H5, CH2OCH3, NH2, NHCH3, N(CH3)2, C2H5, CF3, SCH3, OCH2CH=CH2, OCH2C=CH, OCH2CF3, OCH2CH2OCH3, CR6(OCH3)2, EMI244.3 CR6(OCH2CH3)2 or OCF2H; and Z is CH or N. 4. Compounds of Claim 3 where R1 is H, P5 is H, A is EMI245.1 X is CH3, OCH3, Cl, BR, CH2F or-OCF2H; and Y is CH3, OCH3, OC2H5, CH2OCH3, CF3, OCH2CF3, CH(OCH3)2, EMI245.2 CH(OCH2CH3)2 or OCF2H. 5. Compounds of Claim 4 where R is H, Y is CH3 or OCH3 and X is CR3, OCH3, C1 or Br. 6. Compounds of Claim 5 where J is 7. Compounds of Claim 5 where J is J3. 8. Compounds of Claim 5 where J is 9. Compounds of Claim 5 where J is J5. 10. Compounds of Claim 5 where J is J13. 11. Compounds of Claim 5 where J is J16. 12. Compounds of Claim 5 where J is J21. 13. Compounds of any of Claims 6 to 12 where n is O. 14. Compounds of any of claims 6-12 where n is 1. 15. The compound of Claim 1 which is N-I (4,6- dimethoxypyrimidin-2-yl)aminocarbonyll-2,3-dihydro-2methyl-1,2-benzisothiazole-7-sulfonamide, 1,1-dioxide. The compound of Claim 1 which is N-[(4- methoxy-6-methyl-1,3,5-triazin-2-yl)aminocarbonyl]2,3-dihydro-2-methyl-1,2-benzisothiazole-7-sulfonamide, l,l-dioxide. 17. The compound of Claim 1 which is N-[(4 methoxymethyl-6-methylpyrimidin-2-yl)aminocarbOnyll- 2,3-dihydro-2-methyl-1,2-benzisothiazole-7-sulfonamide, l,l-dioxide. 18. The compound of Claim 1 which is N-[(4chloro-6-methoxypyrimidin-2-yl)aminocarbonyl]-2,3dihydro-2-methyl-1,2-benzisothiazole-7-sulfonamide, l,l-dioxide. 19, The compound of Claim 1 which is N-[(4- methoxy-6-methylpyrimidin-2-yl)aminocarbonyll-2,3- dihydro-2-(1-methylethyl)-1,2-benzisothiazole-7sulfonamide, 1,1-dioxide. 20. The compound of Claim 1 which is N-[(4 methoxy-6-methyl-1,3,5-triazin-2-yl)aminocarbonyl] 2,3-dihydro-2-(1-methylethyl)-1,2,-benzisothiazole-7 sulfonamide, l,l-dioxide. 21. 'The compound of Claim 1 which is N-[(4- methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-2,3 dihydro-2-propyl-1,2-benzisothiazole-7-sulfonamide, l,l-dioxide. 22. The compound of Claim 1 which is N-[(4 methoxy-6-methyl-1,3,5-triazin-2-yl)aminocarbonyl] 2,3-dihydro-2-ethyl-1,2-benzisothiazole-7-sulfonamide, 1,1-dioxide. 23-- . The compound of Claim 1 which is N-[(4,6 dimethoxy-1,3 r 5-triazin-2-yl)aminocarbonyll-2,3-di- hydro-2-methyl-2H-1,2-benzisothiazole-8-sulfonamide, 1,1-dioxide. 24. The compound of Claim 1 which is N-[(4,6- dimethoxypyrimidin-2-yl)aminocarbonyll-1,3-dihydro-3- oxoisobenzofuran-4-sulfonamide. 25. I The compound of Claim 1 which is N-1(4 methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-1,3 dihydro-2-methyl-1-oxo-lH-isoindole-7-sulfonamide. 26.. The compound of Claim 1 which is N-1(4- bromo-6-methoxypyrimidin-2-yl)aminocarbonyll-2,3 dihydro-2-methyl-1,2-benzisothiazole-7-sulfonamide, 1,1-dioxide. 27. / A A compound of claim 1 wherein; J is J1, J3, J4, J6, J7, J9, J13, J15, J16 or J18, where n is O or 1; R1 is H, F, C1, Br, CH3, OCH3 or CF3; R2 is C1-C3 alkyl R3 and R4 are independently H or C1-C3 alkyl, except that R4 must be H in J16; W is O or S; R is H or CH3 P5 is H; A is as de.fined in claim 1 but is not triazinylmethyl; X is CH3, OCH3 or C1; Y is CH3, OCH3, OC2H5, CH2OCH3, NH2, NHCH3, N(CH3)2, C2H5, CF3, EMI247.1 CH=CH2, OCH2CECH, OCH2CF3, OCH2CH20CH3, CH(OCH3)2 Z, Y1, \X2 and Y2 are as defined in claim 1; and X1 is CH3, OCH3 or OC2H5. 28. A compound of claim 1 wherein J is selected from J1-J21, with the proviso that R4 in J16 and R3 in J21 are H; W1 is O; n, W, R, R1, R2, R5, R6, R7, A, Y1- X1, X2, Y2 and X3 are as defined in claim 1; R3 and R4 are independently H or C1-C4 alkyl; X is CH3, OCH3, C1, F, Br, OCF2H or CF3; Y is H, CH3, OCH3, OC2H5, CH2OCH3, NH2, NHC3H, N(CH3)2, C2H5, CF3, SCH3, OCH2CH=CH2, OCH2C=CH, OCH2CF3, CN, OCH2CH2OCH3, CH(OCH3)2, EMI247.2 CH(OCH2CH3)2 or QCF2T where Q and T are as defined in claim 1. 29. A composition suitable for controlling the growths of undesired vegetation comprising an effective amount of a herbicidal compound and at least one of the following: surfactant, solid or liquid diluent, characterised in that said herbicidal compound comprises a compound of any of claims 1 to 28. 30. A method for controlling the growth of undesired vegetation by applying to the locus to be protected an effective amount of a herbicidal compound, characterised in that said herbicidal compound comprises a compound of any of claims 1 to 14, 27 or 28. 31. The method of claim '30 wherein a compound of any of claims 15 to 26 is employed. 32. A method for regulating the growth of plants by applying to the locus of such plants an effective but substantially non-phytotoxic amount of a plant growth regulant, characterised in that said plant growth regulant comprises a compound of any of claims 1 to 28. 33. A process for the preparation of a compound of claim 1 which comprises: (a) reacting a sulfonylisocyanate or sulfonyl isothiocyanate of formula J-SO2N=C=W (II) where J is selected from J1-J5, J7-Jl1, J13-J21, 24, J25 Or J26 as defined in claim 1 and W is O or S, with an appropriate heterocyclic amine of formula EMI248.1 wherein" R and A are as defined in claim 1; or (b) reacting a sulfonamide of formula J-SO2NH2 (IV) wherein J is as defined in claim 1, with a heterocyclic isothiocyanate of formula S=C=N-A (V) wherein A is as defined in claim 1, to prepare a compound of claim 1 wherein W is S and R is H; or (c) reacting said sulfonamide of formula (IV), wherein J is selected from J1-J3, J6-J9, J12-J15, J18-J20, J22, J23 or J26 as defined in claim 1, with an appropriate methylcarbamate of formula EMI249.1 wherein R and A are as defined in claim 1, to obtain a compound of claim 1 wherein W is O; or Cd) reacting a sulfonylcarbamate of formula EMI249.2 wherein J is as defined in claim 1, with said heterocyclic amine of formula (III), to obtain a compound of claim 1 wherein W is O. 34. Compounds of formula J-SO 2N=C=W wherein J is selected from J1-J5, J7-J11, J13-J21' J24' J25 or J26 as defined in claim 1 and W is O or S. 35. Compounds of formula J-SO2NH5 wherein J is as defined in claim 1 and T is H or phenoxycarbonyl. Claims= 1. A process for the preparation of a compound of tha formula: EMI250.1 wherein J is EMI250.2 EMI251.1 EMI252.1 n is 0, 1 or 2; W is O or S; W1 is O or S; R is H or CH3; R1 is H, F, Cl, Br, CH3, OCH3, CF3, SCH3 or OCF2H; R2 is H or C1-C4 alkyl; R3 and R4 are independently H, C1-C4 alkyl, Cl or Br; R5 is H or CH3; R6 is H or CH3; R7 is H or CH3; A is EMI253.1 EMI253.2 X is CH3, OCH3, OCH2CH3, Cl, F, BR, OCF2H, CH2F or CF3; Y is H, CH3, OCH3, OC2H5, CH2OCH3, NH2, NHCH3, N(CH3)2, C2H5, CF3, SCH3, OCH2CH=CH2, OCH2C=CH, OCH2CF3, CN, N3, OCH2CH2OCH3, CH2SCH3, CR6(QCH3)2, EMI253.3 EMI253.4 CR6(QCH2CH3)2 or QCF2T where Q is O or S and T is H, CHC1F, CHBrF or CHFCF3; Z is CH, N, CCH3, CC2H5, CCl or CBr; Y1 is O or CH2 X1 is CH3, OCH3, OC2H5 or OCF2H; ; X2 is CH3, C2H5 or CH2CF3; Y2 is OCH3, OC2H5, SCH3, SC2H5, CH3 or CH2CH3; X3 is CH3 or OCH3; provided that a) when W is S, then R is H, A is EMI254.1 Z is CH or N, and Y is CH3, OCH3, OC2H5, CH2OCH3, C2H5, CF3, SCH3, OCH2CH=CH2, OCH2C=CH, OCH2CF3, OCH2CH2OCH3, CH(OCH3)2 or EMI254.2 b) the total number of carbon atoms in R3 and P4 is less than or equal to 4; c) when X is C1, F or Br, then Z is CH and Y is OCH3, OC2H5, NH2, NHCH3, N(CH3)2 or OCF2H; d) when R5 is CH3, then n is 0; e) when J is J241 then P4 and R5 are not both H and R4 is not Cl or Br; or an ag-riculturally suitable salt thereof, which comprises (a) reacting a sulfonylisocyanate or sulfonylisothiocyanate of formula J-SO2N=C=W (II) where J is selected from J1-J5' J7-J11, J13-J21, J24' J25 or J26 as defined above and W is O or S, with an appropriate heterocyclic amine of formula EMI254.3 wherein R and A are as defined above; or (b) reacting a sulfonamide of formula J-SO2NH2 (IV) wherein J is as defined above, with a heterocyclic isothiocyanate of formula S=C=N-A CV) wherein A is as defined above to prepare a compound formula I wherein W is S and R is H; or (c) reacting said sulfonamide of formula CIV), wherein J is selected from J1-J3, J6-J9, J12-J15, J18-J20, J22, J23 or J26 as defined above, with an appropriate methylcarbamate of formula EMI255.1 wherein R and A are as defined above, to obtain a compound of formula I wherein W is o; or (d) reacting a sulfonylcarbamate of formula EMI255.2 wherein J is selected from J1-J26, with said heterocyclic amine of formula (III), to obtain a compound of formula I wherein W is O. 2. A process of Claim 1 wherein; J is J1, J3, J4, J6, J7, J9, J13, J15, J16 or J18, where n is O or 1; - R1 is -'H,- F, C1, Br, CR3, OCH3 or CF3; R2 is C1-C3 alkyl R3 and R4 are independently H or C1-C3 alkyl, except that R4 must be H in J16; W is O or S; R is H or CH3 R5 is H; A is as defined in claim 1 but is not triazinylmethyl; X is CH3, OCH3 or C1; Y is CH3, OCH3, OC2H5, CH2OCH3, NH2, NHCH3, N(CH3)2, C2H5, CF3, EMI255.3 CH=CH2, OCH2C=CH, OCH2CF3, OCH2CH2OCH3, CH(OCH3)2 Z, Y1, X2 and Y2 are as defined in claim 1; and X1 is CH3, OCH3 or OC2H5. 3. A process of claim 1 wherein J is selected from J1-J21 with the proviso that R4 in J16 and R3 in J21 are H; W1 is O; n, W, R, R1, R2, R5, R6, R7, A, Y1, X1, X2, Y2 and X3 are as defined in claim 1; R3 and R4 are independently H or C1-C4 alkyl; X is CH3, OCH3, Cl, F, Br, OCF2H or CF3; Y is H, CH3, OCH3, OC2H5, CH2OCH3, NH2, NHCH3, N(CH3)2, C2H5, CF3, SCH3, OCH2CH=CH2, OCH2C=CH, OCH2CF3, CN, OCH2CH2OCH3, CH(OCH3)2, EMI256.1 CH(OCH2CH3)2 or QCF2T where Q and T are as defined in claim 1. 4. A process of Claim 1 or 2 where W is 0, R2 is B or C1-C3 alkyl, R3 and R4 are independently H or C1-C3 alkyl and R1 is bonded to the ortho or meta position of the ring relative to the sulfonylurea moiety. 5. A process of Claim 4 where R1 is H, F, Cl, Br, CH3, OCH3, CF3 or SCH3; Y is CH3, OCH3, OC2H5, CH2OCH3, NH2, NHCH3, N(CH3)2, C2H5, CF3, SCH3, OCH2CH=CH2, OCH2C=CH, OCH2CF3, OCH2CH2OCH3, CR6(OCH3)2, EMI256.2 CR6(OCH2CH3)2 or OCF2H; and Z is CR or N. 6. A process of Claim 5 where R1 is H, R5 is H, A is EMI256.3 X is CH3, OCH3, Cl, Br, CH2F or OCF2H; and Y is CH3, OCH3, OC2H5, CH2OCH3, CF3, OCH2CF3, CH(OCH3)2, EMI257.1 CH(OCH2CH3)2 or OCF2H. 7. A process of Claim 6 where R is H, Y is CH3 or OCH3 and X is CH3, OCH3, C1 or Br. 8. A process of Claim 7 where J is selected from 3 J4' J5' J13' J16 or J21. 9. A process of Claim 1 wherein the product is a compound selected from N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-2,3-dihydro-2methyl-1,2-benzisothiazole-7-sulfonamide, 1,1-dioxide; N-[(4-methoxy-6-methyl-1,3,5-triazin-2-yl)aminocarbonyl] 2,3-dihydro-2-methyl-1,2-benzisothiazole-7-sulfonamide, 1,1-dioxide; N-1(4-methoxymethyl-6-methylpyrimidin-2-yl)aminocarbonyl3- 2,3-dihydro-2-methyl-1,2-benzisothiazole-7-sulfonamide, l,l-dioxide; N-1(4-chloro-6-methoxypyrimidin-2-yl)aminocarbonyl]-2,3- dihydro-2-methyl-1,2-benzisothiazole-7-sulfonamide, 1,1-dioxide; N-[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-2,3 dihydro-2-tl-methylethyl}-1,2-benzisothiazole-7-sulfonamide, l,l-dioxide; ; N-[(4-methoxy-6-methyl-1,3,5-triazin-2-yl)aminocarbonyl] 2,3-dihydro-2- C1-methylethyl)-l, -l ,2-benzisothiazole-7-sulfbnamide, l,l-dioxide; N-[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-2,3 dihydro-2-propyl-1,2-benzisothiazole-7-sulfonamide, l,l-dioxide; N-t(4tmethoxy-6-methyl-1,3,5-triazin-2-yl)aminocarbonyl]- 2,3-dihydro-2-ethyl-1,2-benzisothiazole-7-sulfonamide, 1,l-dioxide; N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-2,3-di hydro-2-methyl-2H,1,2-benzisothiazole-8-sulfonamide, 1,1-dioxide; or N-[(4-bromo-6-methoxypyrimidin-2-yl)aminocarbonyl]-2,3dihydro-2-methyl-1,2-benzisothiazole-7-sulfonamide, l,l-dioxide. 10. A process of Claim 1 wherein the product is N-1(4,6-dimethOxypyrDmidin-2-ylXaminocarbonyl]-1,3-dihydro-3- oxoissobenzofuran-4-sulfonamide or N-[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-1,3dihydro-2-methyl-1-oxo-1H-isoindole-7-sulfonamide. 11. A method for controlling the growth of undesired Vegetation by applyiTi,g to the locus to be protected an effective amount of a herbicidal compound, characterised in that said herbicidal compound comprises a compound of formula I as defined in any of claims 1 to 10. 12. A method for regulating the growth of plants by applying to the locus of such plants an effective but substantially non,-phytotoxic amount of a plant growth regulant, characterised in that said plant growth regulant comprises a compound of formula I as defined in any of claims 1 to 10.

Inventors: PASTERIS, ROBERT JAMES
Applicants: E.I. DU PONT DE NEMOURS AND COMPANY
Application year: 1983
Main classification: A01N47
IPC codes: C07D275, A01N47, A01P13, C07D491, C07D521, C07D417