4.1 Article

PREPARATION OF PYRIMIDINE DERIVATIVES THROUGH THREE-COMPONENT REACTIONS OF DIALKYL (2-OXO-3,3,3-TRIFLUOROPROPYL)PHOSPHONATES

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CHEMISTRY OF HETEROCYCLIC COMPOUNDS
卷 47, 期 8, 页码 977-982

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SPRINGER
DOI: 10.1007/s10593-011-0863-4

关键词

hexahydropyrimidinone; dihydropyrimidinone; orthoformate; oxophosphonate; tetrahydropyrimidinone; trifluoromethyl group; Biginelli reaction; multicomponent reaction

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Methods are proposed for the preparation of fluorophosphorus-containing pyrimidines through three-component reactions of dialkyl (3,3,3-trifluoro-2-oxopropyl)phosphonates. Cyclocondensation of these phosphonates with urea and aryl aldehydes gave 6-aryl-4-hydroxy-2-oxo-4-trifluoromethylhexahydropyrimidin-5-ylphosphonates and reaction with urea and trialkyl orthoformates led to 4-alkoxy-2-oxo-4-trifluoromethyl-1,2,3,4-tetrahydropyrimidin-5-ylphosphonates.

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