Rh(III)‐Catalyzed [4+2]‐Annulation of Indoles: Access to Functionalized Pyrimidoindolones Containing α‐Amino Acid Framework

Abstract

Abstract An efficient method for the selective preparation of new CF 3 ‐substituted α‐amino acid derivatives decorated with pharmacophore pyrimido[1,6‐ a ]indolone core has been developed via Rh(III)‐catalyzed C−H activation/[4+2]‐annulation of N ‐(pivaloyloxy)‐indole‐1‐carboxamides with propargyl‐containing α‐amino carboxylates and α‐amino phosphonates.