Neue 1,4-Dihydropyridinderivate

摘要

1317425 1,4-Dihydropyridines BAYER AG 8 Jan 1971 [24 Jan 1970 1 Oct 1970 6 Nov 1970] 1057/71 Heading C2C Novel compounds I in which R is H; linear, branched or cyclic alkyl or alkenyl or linear or branched alkynyl with up to 6 C., which may be substituted by OH or 1-3 C alkoxy; or benzyl or phenethyl in which the benzene ring may be substituted by 1-3 1-3 C alkoxy and/or 1-2 1-3 C alkyl and/or 1-2 F, Cl or Br; R1 is 1-4 C alkyl; R2 is linear, branched or cyclic alkyl or alkenyl of up to 6 C in which the chain may be interrupted by 1 or 2 oxygen atoms and which may be substituted by OH; or alkynyl of up to 6 C; or furfuryl; R3 is aryl which may be substituted by 1-3 NO 2 and/or 1-3 F, Cl or Br, and/or 1-2 OH and/or 1-2 acyloxy and/or 1-3 1-4 C alkoxy and/or a methylenedioxy and/or a 1-4 C alkylthio and/or CF 3 and/or COOH and/or an alkoxycarbonyl and/or a 1-4 C alkylsulphonyl and/or CN; or R3 is benzyl, styryl or pyridyl, pyrimidyl, furyl, thienyl, pyrrolyl which may be substituted by an alkyl radical with 1-2 C or pyrimidyl substituted by 1-2 OCH 3 or OC 2 H 5 groups and R4 is 1-4 C alkyl are prepared (A) by reacting a compound II either (1) with a compound IV and NH 3 or RNH 2 or a salt thereof or (2) with a compound V or (B) by reacting a compound VI either (1) with a compound VII and NH 3 or RNH 2 or (2) with a compound VIII Compounds II are prepared by reaction of aldehydes R3CHO with the appropriate diketones. Compounds VI are prepared by reaction of aldehydes R3CHO with the appropriate #-keto esters. Pharmaceutical compositions for oral or parenteral administration as coronary dilators, anti-fibrillation agents and antihypertensives comprise a compound I together with a suitable excipient.