| 摘要 |
1278348 Thiophen ethers FARBWERKE HOECHST AG 13 July 1970 [12 July 1969] 33832/70 Heading C2C Novel thiophen ethers of the general Formula I wherein R 1 represents a thiophen ring optionally substituted by one or more C 1-6 alkyl, hydroxymethyl, carboxyl (optionally esterified) groups or chlorine or bromine or a combination thereof; R 2 is a phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl group optionally substituted by one or more C 1-6 alkyl or alkoxy or chlorine or bromine and A is a C 2 -C 6 straight or branched alkylene radical or a CH 2 CHOH-CH 2 group may be prepared by one of six known condensation reactions, or reduction of a keto group in a corresponding compound to Formula I having an R 1 -O-B-CO- side chain, wherein B is a C 1 -C 5 straight or branched alkylene radical with a metal hydride to produce A, followed optionally by saponification, decarboxylation reducing carboxylic acid ester groups and/or converting the bases into salts or salts into free bases. The intermediate VI may be prepared by condensation of a hydroxy thiophen with chlorohydrin in the presence of base. Pharmaceutical compositions of the compounds I or their pharmaceutically acceptable salts show α-sympathicolytic activity and have sedative, blood pressure lowering and vasodilatatory effects when administered parenterally or orally. |
