Process for the production of pyrimidine-5-carboxylates

摘要

Pyrimidine-5-carboxylates of formula: wherein R is C_1-4 alkyl, R¹ is C_1-4 alkyl, trifluoromethyl, R² is hydrogen or C_1-4 alkyl and X is hydroxy, chlorine or bromine, are prepared from certain 3-oxoalkanoates of formula (II): with urea and orthoesters of formula (III) R²C(OR). The intermediate 2-acyl-3-ureidoacrylate, without being isolated, is reacted to give a 2-hydroxypyrimidine-5-carboxylate[(I), X-OH] or a hydrate thereof, which is optionally converted into the corresponding chloro or bromo compound (I, X-Cl, Br).