Abstract
An efficient method for the synthesis of halo-carbolines has been developed via Pd-catalysed formation of C-N bonds through C-sp(2)-H/N-H activation of 4-methyl-N-[2-(pyridine-3-yl)phenyl] benzene-sulfonamide derivatives. Pd(OAc)(2) in the presence of Cu(OAc)(2) as oxidant afforded halo-carbolines in good to excellent yields with tolerance to a variety of substituents.