Process for making dihydropyrimidinones

Details Process for making dihydropyrimidinones Process for making dihydropyrimidinones

C - Chemistry, Metallurgy

07

D

C07D 239/22 (2006.01)

Patent

CA 2238924

The present invention provides a process for forming 5-(alkyl or alkoxy)carbonyl-6-alkyl-4-(aryl or alkyl)-3,4-2(1H)-dihydropyrimidinones by combining a .beta.-keto ester or diketone, an aldehyde and urea in the presence of a boron reagent, a metal salt (e.g., Cu2O) and a catalyst (e.g., acid). The reaction is typically run in one pot in a solvent to afford dihydropyrimidinones in higher yields and with easier work up than previously known methods.

L'invention concerne un procédé relatif à la fabrication de 5-(alkyle ou alcoxy)carbonyl-6-alkyl-4-(aryle ou alkyle)-3,4-2(1H)-dihydropyrimidinones, en associant un .beta.-cétoester ou une dione, un aldéhyde et de l'urée en présence d'un réactif au bore, un sel métallique (par exemple, Cu¿2?O) et un catalyseur (par exemple, un acide). Généralement, la réaction est effectuée dans un seul récipient, en présence d'un solvant, ce qui permet d'augmenter le rendement en dihydropyrimidinones et d'obtenir la formation des produits plus facilement qu'avec les méthodes utilisées précédemment.

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