NEW BASICALLY SUBSTITUTED 2,4-(1H,3H)-QUINAZOLINDIONE DERIVATIVES AND PROCESSES FOR THE PRODUCTION THEREOF

摘要

1311543 Basically substituted 2,4(1H,3H)- quinazolindiones CASSELLA FARBWERKE MAINKUR AG 3 July 1970 [4 July 1969] 32384/70 Heading C2C Novel compounds of Formula I wherein m is 1, 2 or 3, n is 2 or 3, R 1 is C 1-4 alkoxy attached in the 6 and 7, or 6, 7 and 8 positions of the quinazoline ring, R 2 is C 1-4 alkoxy and R1 is the radical of a secondary C 2-10 aliphatic, cycloaliphatic or araliphatic amine or a 5, 6 or 7 ring membered heterocyclic amine optionally containing an additional N, O or S hetero atom, the radical being attached through the nitrogen atom, R1 being optionally substituted where it represents a secondary aliphatic amine by a piperidino group, or a radical otherwise within the definition of R1 in which a hydroxy group is replaced by a group of formula are prepared either by cyclization of a compound of formula with phosgene or a chloroformate or by esterification of a compound of formula wherein R is as R1 above with the proviso that R may contain OH substituents which will be esterified in the product. 2 - Amino - 3,4,5 - trimethoxy - N[8 - diethylamino - # - (3,4,5 -trimethoxybenzoxy)- propyl]- benzamide is prepared by reduction of the corresponding 2-nitro compound obtained by esterification of 2 - nitro - 3,4,5 - trimethoxy- N - (γ - diethylamino - # - hydroxypropyl) - benzamide prepared by action of 2-nitro-3,4,5-trimethoxybenzoyl chloride on γ-diethylamino-#- hydroxypropylamine. Pharmaceutical compositions in conventional forms and having coronary dilator activity comprise an above novel compound or pharmaceutically acceptable acid addition salt thereof and a conventional pharmaceutically acceptable diluent or carrier.