Copper-catalysed addition of α-alkyl azaarenes to ethyl glyoxylate via direct C(sp3)–H activation

A novel protocol for the copper-catalysed direct C(sp3)–H bond functionalisation of 2-alkyl azaarenes to CO double bonds has been developed, which expands the scope of C(sp3)–H bond activation reactions and provides new access to medicinally important azaarene derivatives.