Direct C2-alkylation of azoles with alcohols and ethers through dehydrogenative cross-coupling under metal-free conditions.

A metal-free novel, simple, and highly efficient method for the direct C2-alkylation of azoles with alcohols and ethers has been developed on the basis of an oxidative C-H activation process. The dehydrogenative C-C cross-coupling reactions of α-position sp(3) C-H in alcohols and ethers with the 2-position sp(2) C-H in azoles proceeded smoothly in the presence of tert-butyl hydroperoxide (TBHP) under neat reaction conditions, which generated the corresponding products in good yields.