Enantioselective Synthesis of Quinazoline‐Based Heterocycles through Phosphine‐Catalyzed Asymmetric [3+3] Annulation of Morita−Baylis−Hillman Carbonates with Azomethine Imines

Abstract

Abstract Enantioselective synthesis of chiral quinazoline‐based heterocycles is achieved through a chiral phosphine‐catalyzed [3+3] annulation reaction of quinazoline‐based 1,3‐dipoles with Morita−Baylis−Hillman carbonates. The reaction proceeds smoothly under mild conditions to give various chiral heterocyclic compounds in high yields with excellent diastereoselectivities and enantioselectivities. Further diverse elaborations of the annulation products work well to produce novel tetrahydroquinazoline derivatives. magnified image