Abstract
An efficient copper(II)-catalyzed regioselective ortho C(sp2)-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.
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