Hexafluoroisopropanol-Mediated Redox-Neutral α-C(sp³)–H Functionalization of Cyclic Amines via Hydride Transfer

Abstract

Hexafluoroisopropanol has been demonstrated as the versatile promoter for redox-neutral α-C(sp³)-H functionalization of cyclic amines via the cascade [1,5]-hydride transfer/cyclization strategy. A wide range of cyclic amines are functionalized into bioactive tetrahydroquinolines, quinazolines, benzoxazines, and benzotriazepines in moderate to excellent yields. This protocol features additive-free conditions, operational simplicity, and wide substrate scope.