Enantioselective Syntheses of 4<i>H</i>-3,1-Benzoxazines via Catalytic Asymmetric Chlorocyclization of <i>o</i>-Vinylanilides

Abstract

The catalytic asymmetric halocyclization of alkene is a powerful and straightforward strategy for the synthesis of chiral heterocyclic compounds. Herein, an effective approach to chiral benzoxazine derivatives through organocatalyzed chlorocyclization of o-vinylanilides was reported. This method provides facile access to a series of chiral benzoxazines in good to excellent yields (up to 99% yield) and with high-level enantiocontrol (up to 92% ee).