Synthesis of Indolesthrough C2–C3 Bond FormationUsing Lawesson’s Reagent

Amidophenylglyoxylic esters react with Lawesson’s reagent at elevated temperatures, leading to the formation of a diverse array of indole derivatives. This methodology demonstrates broad substrate tolerance and utilizes readily available starting materials. Moreover, this synthetic route is metal-free and environmentally compatible. The scalability of this approach is evidenced by successful gram-scale reactions, highlighting its potential industrial applicability. Furthermore, the resulting products are amenable to further modifications, thereby expanding the potential applications of this synthetic strategy.

Publication Details

Journal
Figshare
Published
2025-02-20
DOI
https://doi.org/10.1021/acs.joc.4c02922.s001
Primary Topic
Synthesis and Reactivity of Sulfur-Containing Compounds
Type
article
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Synthesis of Indolesthrough C2–C3 Bond FormationUsing Lawesson’s Reagent

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Synthesis and Reactivity of Sulfur-Containing Compounds
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Synthesis of Indolesthrough C2–C3 Bond FormationUsing Lawesson’s Reagent

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Abstract

Amidophenylglyoxylic esters react with Lawesson’s reagent at elevated temperatures, leading to the formation of a diverse array of indole derivatives. This methodology demonstrates broad substrate tolerance and utilizes readily available starting materials. Moreover, this synthetic route is metal-free and environmentally compatible. The scalability of this approach is evidenced by successful gram-scale reactions, highlighting its potential industrial applicability. Furthermore, the resulting products are amenable to further modifications, thereby expanding the potential applications of this synthetic strategy.

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Synthesis and Reactivity of Sulfur-Containing Compounds
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Synthesis of Indolesthrough C2–C3 Bond FormationUsing Lawesson’s Reagent · Figshare (2025) | TGRS Research Map | TGRS