Metal catalyzed C(sp3)-H bond amination of 2-alkyl azaarenes with diethyl azodicarboxylate.

Metal-catalyzed direct C(sp3)–H bond amination of 2-alkyl azaarenes with NN double bonds has been developed, which expands the scope of C(sp3)–H bond activation reactions and provides a new access to medicinally important azaarene derivatives.