| 摘要 |
1,242,970. Benzo[b]thiophene derivatives. PARK DAVIS & CO. 14 Aug., 1969 [15 Aug., 1968; 25 June, 1969], No. 40723/69. Heading C2C. The invention comprises compounds of formula RR<SP>1</SP>CHCO 2 H and their pharmaceutically acceptable salts, wherein R is H or C 1-4 alkyl, and R<SP>1</SP> is one of the following radicals in which each Ph may be halogen- or methylsubstituted, R<SP>11</SP> is Ph or cyclohexyl and X is the benzo[b]thiophene nucleus: 4-Ph-2-X, 7-R<SP>11</SP>- 3-X, 7-R<SP>11</SP>-4-X, 2-Me-7-Ph-4-X, 2-Ph-6-X and 3- or 4-Ph-7-X. These compounds are prepared by hydrolysing compounds of formula RR<SP>1</SP>CHY, in which Y is a group hydrolysable to CO 2 H. Starting materials.-Details are given for the preparation of the following: 2-benoylthiophenes, ethyl 3 - phenyl - 3 - (2-thienyl) acrylates and -propionates, 3-phenyl (or methyl or cyclohexyl - 3 - (2 - thieny]) propan - 1 - ols, 3 - phenyl (or methyl or cyclohexyl) - 3 - (2 - thienyl)propyl bromides and cyanides, 4- phenyl (or methyl or cyclohexyl) - 4 - (2 - thienyl)butyric acids, 7 - phenyl (or methyl or cyclohexyl) - 6,7 - dihydrobenzo[b]thiophen- 4(5H) - ones, ethyl 7 - phenyl - 6,7 - dihydrobenzo[6]thiophene - 4 - acetates, ethyl 7- phenyl) or cyclohexyl)benzo[b]thiophene- 3 and 4 - acetates, 2 - phenacylthiotoluenes, 3 (or -4) phenyl - 7 - methylbenzo[b]thiophenes and their 7 - bromomethyl and 7 - cyanomethyl analogues, 7 - (alpha - cyanoalkyl) - 3 (or 4)- phenylbenzo[b]thiophenes, 3 - (alpha - cyanoalkyl) - 7 - phenylbenzo[b]thiophene, 3 - methyl- 7 - phenyl - and 2 - methyl - 4 - phenyl - benzo [b]thiophenes and their bromomethyl and cyanomethyl analogues, 6 - bromo (and cyano) methyl - 2 - phenylbenzo[b]thiophenes, (2 - biphenylylthio)acetone, ethyl 3 - oxo - 4 - [(2- phenyl or 2-cyclohexyl)phenylthio]butyrate, 2- (3 - carboxypropionyl) - 5 - methylthiophene and its methyl ester, 2-(3-carboxypropyl)- 5- methylthiophene. |
