PROCESS FOR MAKING HISTAMINE ANTAGONISTS

摘要

2-Aminopyrimidones which are histamine H2-antagonists having the structure in which Het is a nitrogen-containing 5- or 6- membered fully unsaturated heterocyclic group, m is 0 or 1, Y is methylene, oxygen or sulphur, n is 2 or 3, Z is hydrogen or lower alkyl, A is an alkylene group or an alkylene group interrupted by oxygen or sulphur, and B is hydrogen or a methyl, cycloalkyl, heteroaryl, phenyl, naphthyl, benzodioxolyl or dihydrobenzodioxinyl group, are prepared by a process in which an amine Het-(CH2)mY(CH2)nNH2 is reacted with a 2-nitroaminopyrimidone of structure The new 2-nitroaminopyrimidone intermediates are prepared by reacting nitroguanidine with an oxoester RO2CCH(COZ)-A-B where R is lower alkyl.