Copper-Catalyzed Oxidative Thioamination of Maleimides with Amines and Bunte Salts

Org Lett. 2020 Mar 6;22(5):1863-1867. doi: 10.1021/acs.orglett.0c00207. Epub 2020 Feb 7.

Abstract

Herein, we describe the first example of copper-catalyzed oxidative thioamination of maleimides with secondary amines and Bunte salts with the achievement of C-N and C-S bonds in a single flask. The protocol showcases a prominently broad substrate scope and is also efficient for the late-stage modification of an array of pharmaceuticals. Preliminary mechanistic investigation indicates copper-catalyzed oxidative amination of maleimides with amines to form reactive enaminone and subsequent intermolecular alkenyl C-H thiolation.

Publication types

  • Research Support, Non-U.S. Gov't