What question did this study set out to answer?

The aim is to synthesize 2-aminobenzothiophenes effectively using a novel process.

April 8, 2026

Synthesis of 2‐Amino Benzothiophenes Through C–S Bond Formation

Puntos clave

The aim is to synthesize 2-aminobenzothiophenes effectively using a novel process.
Utilized ortho-halo-substituted thioamides as starting materials.
Promoted the reaction using t-BuOK without transition metals.
Conducted density functional theory (DFT) studies to understand the mechanism.
Performed EPR spin trapping experiments for mechanistic investigations.
Achieved high yields in the synthesis of 2-aminobenzothiophenes.
The method showed tolerance for various functional groups.
Elucidated a plausible reaction mechanism through mechanistic studies.

Resumen

ABSTRACT A widely applicable synthesis of medicinal chemistry‐relevant 2‐aminobenzo b thiophenes has been achieved from ortho ‐halo‐substituted thioamides of 2‐arylacetic acids through a t ‐BuOK‐promoted intramolecular C–S bond formation under transition‐metal‐free conditions. The operationally simple, high‐yielding protocol is based on readily accessible substrates and tolerates a variety of functional groups. Density functional theory (DFT) studies, along with mechanistic investigations, including EPR spin trapping experiments, were conducted to elucidate a plausible reaction mechanism.

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Cite This Study

Kopytov et al. (Wed,) studied this question.

synapsesocial.com/papers/69d5f0bb74eaea4b11a7a197 https://doi.org/https://doi.org/10.1002/cctc.202501860

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