Synthesis and Reactivity of Indole Derivatives: A Comprehensive Review

Indole derivatives, a versatile class of N,O-heterocyclic compounds, due to their biochemical processes, demonstrate a variety of pharmacological characteristics. The indole structure is fundamental in both natural and synthetic chemistry, which contributes enormous opportunities to develop novel synthetic drug molecules. Furthermore, indole derivatives are essential in different applications, as flavoring ingredients, fragrances, and pharmaceutical formulations. From a synthetic perspective, several methods have been developed for indole production. In this review, we report the classical strategies to prepare indole derivatives via Fischer indole synthesis and Skraup synthesis, both of which remain widely employed in the design of complex indole-based heterocyclic compounds. Some green methods and efficient protocols have been discussed to increase yield, selectivity, and sustainability.

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Publication Details

Journal
Current Organic Synthesis
Published
2026-04-15
DOI
https://doi.org/10.2174/0115701794440031260108103017
Primary Topic
Synthesis of Indole Derivatives
Type
article
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article

Synthesis and Reactivity of Indole Derivatives: A Comprehensive Review

Souad Zerbib, Mustapha Dib, Oumaima Kassi, Mostafa Khouili et al.
Current Organic Synthesis
Synthesis of Indole Derivatives
article

Synthesis and Reactivity of Indole Derivatives: A Comprehensive Review

Souad Zerbib, Mustapha Dib, Oumaima Kassi, Mostafa Khouili, Abderrafia Hafid
article en

Abstract

Indole derivatives, a versatile class of N,O-heterocyclic compounds, due to their biochemical processes, demonstrate a variety of pharmacological characteristics. The indole structure is fundamental in both natural and synthetic chemistry, which contributes enormous opportunities to develop novel synthetic drug molecules. Furthermore, indole derivatives are essential in different applications, as flavoring ingredients, fragrances, and pharmaceutical formulations. From a synthetic perspective, several methods have been developed for indole production. In this review, we report the classical strategies to prepare indole derivatives via Fischer indole synthesis and Skraup synthesis, both of which remain widely employed in the design of complex indole-based heterocyclic compounds. Some green methods and efficient protocols have been discussed to increase yield, selectivity, and sustainability.

Current Organic SynthesisVol. 23
Université Sultan Moulay Slimane (MA), Premier University (BD)
Responsible consumption and production
Openalex Percentile: Top 9%
Synthesis of Indole Derivatives
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Synthesis and Reactivity of Indole Derivatives: A Comprehensive Review — Souad Zerbib, Mustapha Dib, et al. · Current Organic Synthesis (2026) | TGRS Research Map | TGRS