Ligand-Controlled Chemoselective One-Pot Synthesis Of Dibenzo-Thiazepinones And Dibenzoxazepinones Via Twice Copper-Catalyzed Cross-Coupling

A highly efficient and generally applicable protocol, starting from 2-bromobenzamides and 2-bromo(thio) phenols via twice copper-catalyzed couplings to afford dibenzothiazepines and dibenzoxazepinones has been developed. High levels of yield and chemoselectivity are achieved in a single-pot reaction by using an appropriate ligand. Moreover, this facile methodology allows rapid access to a variety of bioactive compounds and known psychotropic drug, which should broaden its application in organic synthesis.