| 摘要 |
A process for the production of 2,5-diamino-4,6--dichloropyrimidine of the formula: (see formula I) wherein, in a first step, an aminomalonic ester of the general formula: (see formula II) in which R1 denotes a C1-C6 alkyl group, or a salt thereof is cyclised with guanidine or a salt thereof in the presence of a base to yield a 2,5-diamino-4,6-dihydroxypyrimidine of the formula: (see formula III) or a salt thereof, chlorinating the latter in a second step with a chlorinating agent in the presence of an amide of the general formula: (see formula (IV) in which R2 is a 5- or 6-membered N-heterocycloalkyl residue, which is optionally substituted on the nitrogen atom, or -NR3R4, in which R3 and R4 are identical or different and represent a C1-C6 alkyl group or a benzyl group, to yield a 4,6--dichloropyrimidine of the general formula: (see formula V) in which R2 is defined as above and R5 denotes -NH21-NH-CH=O or -N=CH-R2, in which R2 is defined as above, and reacting the compound V in a third step with a carboxylic acid of the general formula: (see formula VI) in which R6 denotes a C1-C6 alkyl group, branched or unbranched, or a C3-C6 cycloalkyl group, in an aqueous alcoholic solution to yield the final product of formula (I).
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