Synthesis of Substituted Benzo[ b]thiophenes via Base-Promoted Domino Condensation-Intramolecular C-S Bond Formation

Org Lett. 2021 Mar 5;23(5):1698-1702. doi: 10.1021/acs.orglett.1c00085. Epub 2021 Feb 12.

Abstract

A novel synthesis of 2,3-substituted benzothiophenes is reported, involving a tandem base-mediated condensation of o-iodoarylacetonitriles/acetates/ketones with (hetero)aryldithioesters and an intramolecular C-S bond formation. The reaction affords diversely substituted benzothiophenes and heterofused thiophenes in excellent yields.