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.
Enantioselective N-Acylation of Biginelli Dihydropyrimidines by Oxidative NHC Catalysis
Brandolese A.Primo
;Ragno D.Secondo
;Leonardi C.;Di Carmine G.;Bortolini O.;De Risi C.;Massi A.
Ultimo
2020
Abstract
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.File in questo prodotto:
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