Aerobic Construction of 2-Acyl Benzoxazole by Tandem C—H Oxygenation and Oxazole Ring Formation

Abstract

The synthesis of useful 2-acyl benzoxazoles has been realized via the tandem methylene C-H oxygenation and oxazole annulation of N-(o-hydroxyphenyl)phenylacetamides via copper catalysis in one-pot fashion. Besides featuring the incomparable step-economy resulting from the multi-step transformation, the tunable synthesis of diverse 2-methylene functionalized benzoxazoles using identical starting materials as well as the expanded synthesis of corresponding benzothiazoles is also attractive advantage of the work.