Direct para-C–H heteroarylation of anilines with quinoxalinones by metal-free cross-dehydrogenative coupling under an aerobic atmosphere

Abstract

Herein, a green and efficient metal-free cross-dehydrogenative coupling (CDC) for the direct para-C–H heteroarylation of anilines with quinoxalinones has been described. This reaction is performed in H₂O/DMSO (v/v = 2 : 1) using air as the sole oxidant. Various anilines (primary, secondary and tertiary amines) and quinoxalinones are well compatible, affording the corresponding products in moderate-to-good yields. Such a methodology provides an environmentally friendly and efficient alternative for the late-stage modification of nitrogen-containing compounds.