Direct 2-acetoxylation of quinoline N-oxides via copper catalyzed C–H bond activation

An efficient and direct 2-acetoxylation of quinoline N-oxides via copper(I) catalyzed C–H bond activation has been developed. This transformation was achieved using TBHP as an oxidant in the cross-dehydrogenative coupling (CDC) reaction of quinoline N-oxides with aldehydes, and provided a practical pathway to 2-acyloxyl quinolines.