Efficient accessibility of indole and pyrrole nuclei via late-stage aryl C–H activation of drug molecules promoted by thianthrenium salts

Abstract

An efficient redox-neutral palladium-catalyzed system has been developed to introduce indole and pyrrole units to a wide range of bioactive molecules via late-stage aryl C–H activation, providing a robust tool for medicinal chemists to explore structure–activity relationships (SARs). Furthermore, the successful gram-scale reaction and subsequent synthetic investigations demonstrate the potential application of this established method in organic synthesis, materials science, and biochemistry.