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

An efficient method for the selective preparation of new CF3-substituted alpha-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 alpha-amino carboxylates and alpha-amino phosphonates.

Automated summary

An efficient method for the selective synthesis of new CF3-substituted alpha-amino acid derivatives 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 alpha-amino carboxylates and alpha-amino phosphonates.