Abstract : This article reports an efficient CH activation process for regioselective halogenation of 1,4-benzodiazepinones. Direct halogenation with NXS (X = Br, I) affords halogenated benzodiazepinones on the central aromatic ring whereas catalyst (Pd(OAc) 2) controlled CH activation furnishes regioselectively ortho halogenated benzodiazepinones on the phenyl side chain.
