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

J Org Chem. 2020 Feb 21;85(4):1915-1926. doi: 10.1021/acs.joc.9b02606. Epub 2020 Jan 15.

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.

Publication types

  • Research Support, Non-U.S. Gov't