Copper-Catalyzed Direct Oxidative C–H Amination of Benzoxazoles with Formamides or Secondary Amines under Mild Conditions

Abstract

A facile, efficient, and practical method for copper-catalyzed direct C-H amination of benzoxazoles with formamides or secondary amines has been developed. The system can be performed in the absence of external base and only requires O(2) or even air as oxidant. A variety of substituted benzoxazol-2-amines were synthesized with moderate to excellent yield.