Transition-Metal-Free Amine Oxidation: A Chemoselective Strategy for the Late-Stage Formation of Lactams

Org Lett. 2017 Feb 17;19(4):870-873. doi: 10.1021/acs.orglett.7b00021. Epub 2017 Feb 8.

Abstract

A metal-free strategy for the formation of lactams via selective oxidation of cyclic secondary and tertiary amines is described. Molecular iodine facilitates both chemoselective and regioselective oxidation of C-H bonds directly adjacent to a cyclic amine. The mild conditions, functional group tolerance, and substrate scope are demonstrated using a suite of diverse small molecule cyclic amines, including clinically approved drug scaffolds.

Publication types

  • Research Support, Non-U.S. Gov't