Direct Construction of Diverse Polyheterocycles Bearing Pyrrolidinediones via Rh(III)‐Catalyzed Cascade C−H Activation/Spirocyclization

Abstract Rh(III)‐catalyzed cascade oxidative annulation of 2‐arylquinazolinones with various maleimides to afford spiroisoindoloquinazolinones bearing pyrrolidinediones is described. Sequential ortho C−H functionalization and spirocyclization via aza‐Michael addition result in the formation of both C−C and C−N bonds in a single operation. This atom‐ and step‐economic strategy provides an efficient and novel approach for the syntheses of diverse polyheterocycles bearing pyrrolidinediones, starting from 2‐heteroarylquinazolinones and 5‐arylpyrazolopyrimidinones, in good to excellent yields. magnified image