Rh-catalyzed sequential oxidative C–H activation/annulation with geminal-substituted vinyl acetates to access isoquinolines

Abstract

The concise synthesis of 3-substituted or non-C3-substituted isoquinolines through Rh-catalyzed sequential oxidative C-H activation/annulation with geminal-substituted vinyl acetates was developed with good functional group tolerance. The protocol was successfully applied to the total synthesis of the natural product papaverine.