Regioselective Thiolation of Indole to Construct 3-Arylthioindoles

Abstract

A practical and novel approach for the regioselective synthesis of 3-arylthioindole derivatives has been accomplished using a combination of indole substrates with p-toluene sulfonyl hydrazide. This methodology employs NIS as the oxidant and PPh<inf>3</inf> as the reductant to give the desired 3-arylthioindoles in good to excellent yields. This method offers several advantages, including simplicity, operational ease, and broad substrate scope. © 2025 Bentham Science Publishers.