Process for the production of 2,5-diamino-4,6-dichloropyrimidine

摘要

Production of 2,5-diamino-4,6-dichloropyrimidine of formula (I) comprises: a) cyclising a dialkyl aminomalonate of formula R1OC(=O)CH(NH2)C(=O)OR1 (II) with guanidine; b) chlorinating the resulting 2,5-diamino-4,6-dihydroxypyrimidine or formula (III) in the presence of an amide of formula HC(=O)R2 (IV); and c) reacting the 2-amino-4,6-dichloro-5-(substituted methyleneamino)-pyrimidine of formula (V) obtained with a carboxylic acid of formula R6COOH (VI) in an aqueous alcohol. R1 = 1-6C alkyl; R2 = 5- or 6-membered N-heterocycloalkyl (optionally N-substituted) or NR3R4; R3, R4 = 1-6C alkyl or benzyl; R5 = NH2; R6 = 1-6C alkyl or 3-6C cycloalkyl.