BF₃·Etherate-Mediated Friedel–Crafts Arylation of 2-Hydroxy-1,4-benzoxazines: Synthesis of 2-Aryl-1,4-benzoxazine Derivatives

Abstract

BF3·etherate-mediated carbon-carbon bond formation by the Friedel-Crafts arylation of 2-hydroxybenzoxazine derivatives with various electron-rich arenes is reported. The current protocol provides an easy access for the synthesis of a series of densely substituted 2-aryl-1,4-benzoxazine derivatives under mild conditions.