Copper-Catalyzed Remote para-C−H Functionalization of Anilines with Sodium and Lithium Sulfinates



A copper-catalyzed, cross-dehydrogenative coupling of anilines with sodium and lithium sulfinates was developed. By using a cooperative reaction system with Mn(OAc)3 as stoichiometric co-oxidant a highly selective para-functionalization of anilines was accomplished. Various functional groups were tolerated and the desired products were obtained in high yields. This method not only provides a novel approach for the synthesis of arylsulfones but might also offer new opportunities for the development of copper-catalyzed para-selective C−H functionalizations.