VERFAHREN ZUR HERSTELLUNG VON PYRIMIDIN-5- CARBOXYLATEN

VERFAHREN ZUR HERSTELLUNG VON PYRIMIDIN-5- CARBOXYLATEN

Pyrimidine-5-carboxylates of formula: wherein R is C1-4 alkyl, R1 is C1-4 alkyl, trifluoromethyl, R2 is hydrogen or C1-4 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...

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Bibliographische Detailangaben
Hauptverfasser: RITTINER, BRUNO, DUCRY, LAURENT
Format: Patent
Sprache:ger
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Zusammenfassung:Pyrimidine-5-carboxylates of formula: wherein R is C1-4 alkyl, R1 is C1-4 alkyl, trifluoromethyl, R2 is hydrogen or C1-4 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).