Neue Pyrimidinderivate und Verfahren zu ihrer Herstellung

摘要

1,272,075. 2 - Amino - 4,5,6,7 - tetrahydrothieno[2,3-c]pyridines. CIBA-GEIGY A.G. 31 July, 1969 [2 Aug., 1968; 20 June, 1969], No. 3576/71. Divided out of 1,272,074. Heading C2C. Novel 2 - amino - 4,5,6,7 - tetrahydrothieno- [2,3-c]pyridines of the general formula wherein R 2 , R1 2 , R 3 and R1 3 are each a hydrogen atom or an optionally substituted hydrocarbon radical and/or R 2 and R1 2 and/or R 3 and R1 3 together form a bivalent hydrocarbon radical, each of R n and R 4 is a hydrogen atom or an optionally substituted hydrocarbon radical and Y11 is a free or esterified carboxyl group, a carbamoyl group or a cyano group, N2-acyl derivatives thereof and salts thereof are prepared (a) by reaction of a 4-piperidone of the general formula with a nitrile of the general formula Y11-CH 2 - CN and simultaneously or subsequently with sulphur; (b) when Y11 is a free carboxyl group, by hydrolysis of the corresonding compound of the first general formula above, wherein Y11 is an esterified carboxyl group or an N2-acyl derivative thereof, and (c) when the desired compound is an N2-acyl derivative, by acylation of the corresponding compound of the first general formula above; followed optionally by salification of the product. 4-Piperidones of the second general formula above are prepared by reaction of ammonia or an amine with acetone or a derivative thereof and an aldehyde. Pharmaceutical compositions having antihypertensive and anti-exudative activity comprise, as active ingredient, a 2-amino-4,5,6,7- tetrahydrothieno[2,3-c]pyridine of the first general formula above, an N2-acyl derivative thereof or a physiologically tolerable salt thereof, together with a pharmaceutical carrier, and may be administered enterally or parenterally.