Rh(III) catalysts have played increasingly important roles in the activation of C-H bonds to build heterocyclic scaffolds. However, there are few reports on the more challenging synthesis of pharmaceutically important 2 H-isoindoles and fused 2 H-isoindoles. The process reported herein is an effective strategy to produce 2 H-isoindole or fused 2 H-isoindole derivatives via a Rh(III)-catalyzed transformation of α-iminonitriles or α-imino esters with acrylates.