PROCESS FOR PRODUCTION OF 2,5-DIAMINO-4,6-DICHLOROPYRIMIDINE AND ITS FORMAMIDE, N-(2-AMINO-4,6-DICHLOROPYRIMIDINE-5-YL)FORMAMIDE AND 4,6-DICHLOROPYRIMIDINES

摘要

The process for the preparation of N- (2-amino-4,6-dichloropyrimidin-5-yl) formamide and 2,5-diamino-4,6-dichloropyrimidine of formula (VIII) is characterized in that the aminomalonic acid ester of general formula (I) is cyclized in the first step. of formula (II) or a salt thereof with guanidine or a salt thereof in the presence of a base to the 2,5-diamino-4,6-dihydroxypyrimidine of formula (III) or a salt thereof, which is then chlorinated in a second step with a chlorinating agent in the presence of an amide IV) to the 4,6-dichloropyrimidine of formula (V), which is then converted in the third step with the carboxylic acid of formula (VI) to give the final product of formula (VIII). Disclosed is a novel pyrimidine derivative, N- (2-amino-4,6-dichloropyrimidin-5-yl) formamide, which can well be converted to nucleotide derivatives.