| 摘要 |
1295206 Pyrido-pyrimidine derivatives BOEHRINGER MANNHEIM GmbH 28 July 1971 [31 July 1970] 35442/71 Heading C2C Novel compounds of the general Formula I wherein R 1 and R 2 which may be the same or different, are C 1-5 alkyl, alkenyl, cycloalkyl, aralkyl, pyrylalkyl, thenylalkyl or tetrahydrofurylalkyl radicals optionally substituted by hydroxyl, alkoxy or alkylmercapto and wherein one of R 1 and R 2 may be hydrogen; and physiologically compatible acids thereof may be prepared by (a) reaction to compound II wherein X is a reactive group with an amine R 1 R 2 NH ; (b) condensing propargyl aldehyde or a derivative thereof with a compound IV wherein Z is hydroxyl, mercapto or amino, alkoxyl, phenoxy or alkylmercapto and if necessary converting Z simultaneously or subsequently into a hydroxyl group; (c) forming a secondary or tertiary amine from 2-amino-4- hydroxypyrido[2,3-d]pyrimidine; (d) reaction of VI or a cyanide derivative thereof with 2-aminopyridine - 3 - carboxylic acid or a reactive derivative thereof. Pharmaceutical compositions of the compounds I show diuretic and natriuretic activity when administered orally or parenterally with the usual excipients. |
