Photocatalyzed defluoro-α-aminoalkylation of trifluoromethylarenes with tertiary amines

Abstract We report the defluoro-α-aminoalkylation of trifluoromethylarenes with N-methyl-substituted tertiary amines using Ir(ppy)3 catalyst under visible-light irradiation. The resulting products were successfully converted into the corresponding unprotected primary amines via an oxidation/dealkylation sequence. This sequential transformation provides a practical route to bioactive compounds. Moreover, site-selective C−F bond transformation of perfluoroalkylarenes was achieved.