Work

Synthesis of 2-Aminobenzo[b]thiophenes via an Intramolecular Dehydrogenative C–S Bond Formation Effected by Iodine(III) Reagents

Year: 2024

Type: article

Abstract: A direct synthesis of medicinal chemistry-relevant 2- aminobenzo[b]thiophenes has been achieved from substituted thioamides of 2-arylacetic acids through a fast intramolecular cross-dehydrogenative cyclization, mediated by hydroxy(tosyloxy)iodobenzene (HTIB, Koser’s reagent). This synthetic approach is operationally simple, uses easily accessible substrates, and tolerates a variety of substituents at different sites, providing an opportunity for diversification.

Source: Synthesis

DOI: 10.1055/a-2500-6460

Authors: Dmitry I. Bugaenko, Alexander V. Karchava

Institution: Lomonosov Moscow State University

Language: English

Topic: Sulfur-Based Synthesis Techniques

Subfield: Organic Chemistry

Field: Chemistry

Domain: Physical Sciences

Open Access status: green

Funder: Russian Science Foundation

Award: G227779794