Copper-Catalyzed Aerobic Cross-Dehydrogenation Coupling of Indoles for Synthesis of 2,3'-Bisindoles

Abstract

2,3'-Bisindoles with C-C linkages have attracted interest in medicinal chemistry, yet their synthesis is intricate with many steps. Notably, direct C-H/C-H cross-coupling of non-directed heteroaromatics remains challenging, often requiring precious metals and oxidants to enhance coupling efficiency. Herein, we present a copper-catalyzed C-H/C-H cross-coupling method for N-substituted indoles without directing groups, facilitated by molecular oxygen under gentle conditions. It showed reasonable functional group compatibility and provided one-pot access to a variety of 2,3'-bisindoles derivatives in moderate to good yields.

Keywords: 2,3′-bisindoles; Copper-catalyzed; Cross-dehydrogenation coupling.