Catalytic Asymmetric Reactions of α-Isocyanoacetates and <i>meso</i>-Aziridines Mediated by an in-Situ-Generated Magnesium Catalytic Method

Abstract

A catalytic asymmetric ring-opening reaction between α-isocyanoacetates and meso-aziridines has been realized by developing an in-situ-generated magnesium catalytic method. Chiral oxazoline-OH ligands were employed in the magnesium catalyst and diphenylphosphinamide was improved as a powerful achiral additive in this reaction. The ring-opening products of the desired reaction were obtained in good chemical yields and enantioselectivities. Moreover, these enantio-enriched adducts can be smoothly transformed into tetrahydropyrimidines mediated by a silver salt under mild conditions.