Cu(I)‐Catalyzed Site Selective Acyloxylation of Indoline Using O2 as the Sole Oxidant

Abstract

AbstractA Cu(I)‐catalyzed regioselective cross‐dehydrogenative coupling of indoline with a variety aryl and alkyl carboxylic acids is described. The divergent process for the oxygenation was achieved in satisfactory yields under additive free conditions, which provides an efficient strategy for the regioselective C7 functionalization of indolines using inexpensive copper catalyst. Oxygen as the sole oxidant is required in this protocol. The method is tolerated by a wide range of functional groups. Preliminary mechanistic study provided support for a reversible C−H bond metallation step.magnified image