Enantioselective N-Acylation of Biginelli Dihydropyrimidines by Oxidative NHC Catalysis

The oxidative N-acylation reaction of 3,4-dihydropyrimidin-2-(1H)-ones (DHPMs) with enals and N-heterocyclic carbene (NHC) catalysts is described. The reaction proceeds in the presence of quinone oxidant without additional acyl transfer agents and in the asymmetric variant produces pharmaceutically relevant N3-acylated products with good-to-moderate enantioselectivity.