Copper-catalyzed and Y(OTf)3-promoted deoxyaminative alkylation of imidazo[1,2-a] pyridines with benzyl alcohols and amines.

A straightforward and efficient Cu(OAc)2/TEMPO-catalyzed and then Y(OTf)3-promoted protocol for deoxyaminative alkylation of imidazo[1,2-a]pyridines with benzyl alcohols and amines has been developed. This protocol enables the direct use of readily available alcohols as alkylating agents for constructing valuable functionalized imidazo[1,2-a]pyridine derivatives under mild aerobic conditions, featuring atomic economy, a broad substrate scope, and excellent functional group tolerance. Moreover, this transformation can be readily scaled up to the gram scale and allows for further modification, highlighting its practical potential in organic synthesis and pharmaceutical development.