Process for the production of pyrimidine-5-carboxylates

Pyrimidine-5-carboxylates of formula wherein R is C1-4 alkyl, R is C1_4 alkyl or trifluoromethyl, R is hydrogen or C1 alkyl and X is hydroxy, chlorine or bromine, are prepared from 3-oxoalkanoates of formula with urea and orthoesters of formula R C(OR)3 (III). The intermediate 2-acyl-3-ureidoacrylat...

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1. Verfasser: DUCRY LAURENT,RITTINER BRUNO
Format: Patent
Sprache:eng
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Zusammenfassung:Pyrimidine-5-carboxylates of formula wherein R is C1-4 alkyl, R is C1_4 alkyl or trifluoromethyl, R is hydrogen or C1 alkyl and X is hydroxy, chlorine or bromine, are prepared from 3-oxoalkanoates of formula with urea and orthoesters of formula R C(OR)3 (III). 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).