BPO-promoted [4 + 2] cyclization of enaminones and o-phenylenediamines to 2-acyl quinoxalines via a cascade transamination and C–H amination

Abstract

Rapid assembly of quinoxalines in a single step from readily available precursors has been recognized as an ideal platform in terms of efficiency and operation. Herein, we report a BPO-promoted metal-free approach to 2-acyl quinoxalines from enaminones and o-phenylenediamines via cascade transamination and C–H amination. This methodology demonstrates excellent compatibility with various substrates, including o-hydroxy enaminones, drug derivatives and natural products under mild reaction conditions.