Highly Enantioselective Biginelli Reaction Catalyzed by Double Axially Chiral Bisphosphorylimides

Abstract

Abstract Double axially chiral bisphosphorylimides have been used as catalysts in enantioselective Biginelli reactions. The three‐component reaction of aromatic aldehydes, thiourea, and ethyl acetoacetate took place by using 5 mol‐% catalyst in ethyl acetate at 50 °C. A series of chiral dihydropyrimidinethiones (DHPMs) were obtained in high yields (up to 97 %) with good to high enantioselectivities (up to 96 % ee ) in only 12 hours.