Transition-metal-free arylation of benzoxazoles with aryl nitriles

Abstract

Transition-metal-free arylation of benzoxazoles with aryl nitriles has been developed to afford important 2-aryl benzoxazoles under simple reaction conditions. A variety of functional groups were tolerated and heteroaryl nitriles were also suitable substrates. Preliminary mechanistic studies indicated a ring-opening mechanism. The methylation of azoles with acetonitrile was also achieved in a similar manner. This protocol provides a novel strategy for the efficient synthesis of complex 2-aryl benzoxazole derivatives.