Palladium-Catalyzed C-7 Selective CH Carbonylation of Indolines for Expedient Synthesis of Pyrroloquinazolinediones

A novel palladium-catalyzed C-7 selective CH carbonylation of indolines with carbon monoxide for an expedient synthesis of pyrroloquinazolinediones, a structural motif with great potential in biologically active compounds, has been developed. Oxidation of the pyrroloquinazolinedione with 2,3-dichloro-5,6-dicyano-p-benzoquinone (DDQ) could easily afford the corresponding indole-based derivative in excellent yield.