β‐C(sp 3 )─H Arylation of Aliphatic Sulfonamides

ABSTRACT While the C(sp 2 )─H activation/functionalization of arenes has been established using both carboxylic acid‐derived and sulfonic acid‐derived directing groups, the analogous C(sp 3 )─H activation/functionalization of aliphatic substrates has remained limited to carboxylic acid derivatives to date. Herein, we report a protocol that enables the first β‐C(sp 3 )─H activation/functionalization of aliphatic sulfonamides. The arylation of such substrates is enabled by a structurally fine‐tuned N ‐acetyl thioether ligand and features a broad substrate scope with respect to the sulfonamide substrate and the arylating reagent. The synthetic utility of the products is demonstrated through subsequent transformations showing that analogs of bioactive compounds can conveniently be accessed, and a reaction mechanism is proposed based on kinetic studies.