Copper(II)-Mediated, Site-Selective C(sp²)–H Sulfonamidation of 1‑Naphthylamines

An operationally simple and efficient protocol for copper(II)-mediated, picolinamido-directed C8–H sulfonamidation of 1-naphthylamine derivatives with various sulfonamides has been developed. Remarkably, this cross-dehydrogenative C–H/H–N coupling reaction exhibits a broad substrate scope with excellent functional group tolerance, is scalable, and enables an expeditious route to a library of unsymmetrical N-arylated sulfonamides in good to excellent yields with exclusive site selectivity.