Copper-Catalyzed Cross-Dehydrogenative C–N Bond Formation of Azines with Azoles: Overcoming the Limitation of Oxidizing N–O Activation Strategy

Here, we report the copper-catalyzed C2 selective cross-dehydrogenative C–N bond formation of azines with azoles. This straightforward method enables us to address the key limitation of prior N–O activation strategy in C2 amination of azines. The wide substrate scope, high functional group tolerance, and ease of operation of the present method are expected to promote its potential application in synthetic chemistry.