Copper()-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 ortho C(sp 2 )-H amination of arenes/heteroarenes has been developed with the assistance of 8-AIP (8-aminoimidazo[1,2- a ]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. A ubiquitous copper( ii )-catalyzed regioselective ortho C(sp 2 )-H amination of arenes/heteroarenes has been revealed with the assistance of 8-AIP (8-aminoimidazo[1,2- a ]pyridine) as an efficacious 6,5-fused bicyclic removable chelating auxiliary.