The Biginelli reaction, involving a three-component reaction of an aromatic aldehyde, urea and ethyl acetoacetate, has emerged as an extremely useful synthetic tool to organic chemists for the synthesis of 3,4-dihydropyrimidine-2-(1H)-ones and related heterocyclic compounds. In the past decades, the asymmetric variants of this reaction have been at the forefront of investigations in several research groups. In 2013, we highlighted the developments occurred in the asymmetric version of the Biginelli reaction. This review article focuses on the recent developments of asymmetric Biginelli reaction covers the literature going back to 2012.
Keywords: 3-4-Dihydropyrimidine-2-(1H)-ones; Asymmetric reaction; Biginelli reaction; Catalysis; Enantioselective reaction; Enantioselectivity; Heterocyclic compounds; MCRs; Pyrimidines; Stereoselectivity.