Rh(III)‐Catalyzed C−H Cyclization of 2‐Arylbenzimidazoles with CF₃‐Imidoyl Sulfoxonium Ylides and Further Sc(III)‐Catalyzed Deaminative Hydroxylation

Abstract An efficient Rh(III)‐catalyzed C−H bond activation/cyclization of 2‐arylbenzimidazoles with CF 3 ‐imidoyl sulfoxonium ylides has been achieved, yielding diverse CF 3 − and amino‐disubstituted 5,6‐dihydrobenzoimidazo[2,1‐ a ]isoquinolines, which could undergo a deaminative hydroxylation to access CF 3 − and hydroxy‐disubstituted 5,6‐dihydrobenzoimidazo[2,1‐ a ]isoquinolines catalyzed by Sc(OTf) 3 . This developed strategy features easily available starting materials, broad substrate scope, good scalability and high efficiency. Moreover, the antitumor activities of selected products against some human cancer cell lines were also investigated, and the results indicated that several products show antiproliferative activities.