Copper-Catalyzed Remote C–H Functionalizations of Naphthylamides through a Coordinating Activation Strategy and Single-Electron-Transfer (SET) Mechanism

Achieving p-CAr–H site selectivity is one of the major challenges in direct carbon–hydrogen (C–H) functionalization reactions. Herein, the copper-catalyzed and picolinamide-assisted remote p-C–H sulfonylation of 1-naphthylamides was realized. The synthetic utility of this method was further examined by sequential functionalizations and the efficient synthesis of the pharmaceutically useful 5-HT6 serotonin receptor ligand. This approach also...