Abstract

Synthetically versatile anthranils as a bifunctional amino source have been employed for the first time to enable direct amination on unactivated C(sp3)-H bonds of thioamides under Cp*CoIII catalysis. The excellent site-selectivity on primary C(sp3)-H bonds is observed for a diverse array of thioamides with high functional group tolerance. Further applicability of the products is also highlighted through a series of interesting synthetic elaborations.

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