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Enantioselective N ‐Acylation of Biginelli Dihydropyrimidines by Oxidative NHC Catalysis
Author(s) -
Brandolese Arianna,
Ragno Daniele,
Leonardi Costanza,
Di Carmine Graziano,
Bortolini Olga,
De Risi Carmela,
Massi Alessandro
Publication year - 2020
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.202000151
Subject(s) - chemistry , acylation , enantioselective synthesis , catalysis , oxidative phosphorylation , organocatalysis , biginelli reaction , carbene , organic chemistry , combinatorial chemistry , biochemistry
The oxidative N ‐acylation reaction of 3,4‐dihydropyrimidin‐2‐(1 H )‐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.