Copper(II)-catalyzed, site-selective C(sp)-H amination using 8-aminoimidazo[1,2-]pyridine (8-AIP) as a directing group.

An efficient copper(II)-catalyzed regioselective C(sp)-H amination of arenes/heteroarenes has been developed with the assistance of 8-AIP (8-aminoimidazo[1,2-]pyridine) as an efficacious 6,5-fused bicyclic removable chelating auxiliary. This operationally simple approach is scalable, has a broad substrate scope, and is highly compatible with functional groups. Furthermore, post-diversification of the synthesized derivatives demonstrates the methodology's synthetic adaptability.