Copper(ii)-catalyzed methoxylation of unactivated (hetero)aryl C–H bonds using a removable bidentate auxiliary

Abstract

A copper(II)-catalyzed methoxylation of unactivated (hetero)aryl C–H bonds directed by our newly developed PIP directing group with methanol has been achieved. This protocol occurs efficiently with a catalytic amount of copper (5 mol%), is a simple and environmentally benign reaction system, has a broad substrate scope and high functional group tolerance.