Synthesis of Functionalized Pyrrolidinone Scaffolds via Smiles-Truce Cascade

Org Lett. 2023 Sep 15;25(36):6736-6740. doi: 10.1021/acs.orglett.3c02559. Epub 2023 Sep 5.

Abstract

Arylsulfonamides have been found to react with cyclopropane diesters under simple base treatment to give α-arylated pyrrolidinones. This one-pot process comprises three steps: nucleophilic ring-opening of the cyclopropane, reaction of the resulting enolate in a Smiles-Truce aryl transfer, and lactam formation. The reaction represents a new, operationally simple approach to biologically active pyrrolidinones and expands Smiles-Truce arylation methods to encompass sp3 electrophilic centers in cascade processes.