title: Primary Amine-Catalyzed Biginelli Reaction for the Enantioselective Synthesis of 3,4-Dihydropyrimidin-2(1H)-ones.
abstract: Several chiral primary amines, mainly those derived from the cinchona alkaloids, were evaluated as the organocatalysts for the asymmetric Biginelli reaction. With the quinine-derived amine catalyst 1 and after extensive optimization of the reaction conditions, 3,4-dihydropyrimidin-2(1H)-ones were obtained in moderate to good yields and 51-78% ee from a three-component reaction of aryl and aliphatic aldehydes, urea, and acetoacetate.
authors.affiliation: Department of Chemistry, University of Texas at San Antonio, Texas, 78249-0698.
authors.forename: Derong
authors.initials: D
authors.lastname: Ding
authors.forename: Cong-Gui
authors.initials: CG
authors.lastname: Zhao