A regioselective C7 bromination and C7 palladium-catalyzed Suzuki-Miyaura cross-coupling arylation of 4-substituted NH-free indazoles.

A direct and efficient regioselective C7-bromination of 4-substituted 1 H -indazole has been achieved. Subsequently, a successful palladium-mediated Suzuki-Miyaura reaction of C7-bromo-4-substituted-1 H -indazoles with boronic acids has been performed under optimized reaction conditions. A series of new C7 arylated 4-substituted 1 H -indazoles was obtained in moderate to good yields.