Copper-catalyzed direct secondary and tertiary C-H alkylation of azoles through a heteroarene-amine-aldehyde/ketone coupling reaction.

Coupling the strangers: A copper-catalyzed three-component heteroarene-amine-aldehyde/ketone coupling affords a novel approach to the hitherto difficult direct secondary/tertiary C-H alkylation of azoles. This simple method allows the facile installation of diversely substituted, branched and nitrogen-containing alkyl or alkaloid side chains on the azole moiety by using readily available starting materials.