Recent Developments in the Transition-metal-free Approaches for C- and N-Arylation/Heteroarylation of Indoles

Indole is a privileged heterocyclic scaffold widely prevalent in bioactive compounds, agrochemicals, and advanced materials. Introduction of aryl and heteroaryl groups offers enhanced structural and functional diversity, intriguing a significant interest in the synthesis of aryl-and heteroaryl substituted indoles. However, the emerging cost- and environment-related challenges associated with the popular transition-metal mediated arylations have propelled a surge in the development of sustainable metal-free approaches. This review discusses the recent progress in the transition-metal-free C- and N- arylations of indoles. Various arylation methods using diazonium salts, diaryliodonium salts, aryl halides and other arylating reagents are discussed. The review assesses the capabilities of current metal-free arylation strategies to inspire the discovery of environmentally benign and sustainable C- and N- functionalization strategies.

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Publication Details

Journal
Synthesis
Published
2026-07-28
DOI
https://doi.org/10.1055/a-2925-0367
Primary Topic
Catalytic C–H Functionalization Methods
Type
article
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article

Recent Developments in the Transition-metal-free Approaches for C- and N-Arylation/Heteroarylation of Indoles

Anee Mohanty, Rakesh Kumar, Shreya Rana
Synthesis
Catalytic C–H Functionalization Methods
article

Recent Developments in the Transition-metal-free Approaches for C- and N-Arylation/Heteroarylation of Indoles

Anee Mohanty, Rakesh Kumar, Shreya Rana
article en

Abstract

Indole is a privileged heterocyclic scaffold widely prevalent in bioactive compounds, agrochemicals, and advanced materials. Introduction of aryl and heteroaryl groups offers enhanced structural and functional diversity, intriguing a significant interest in the synthesis of aryl-and heteroaryl substituted indoles. However, the emerging cost- and environment-related challenges associated with the popular transition-metal mediated arylations have propelled a surge in the development of sustainable metal-free approaches. This review discusses the recent progress in the transition-metal-free C- and N- arylations of indoles. Various arylation methods using diazonium salts, diaryliodonium salts, aryl halides and other arylating reagents are discussed. The review assesses the capabilities of current metal-free arylation strategies to inspire the discovery of environmentally benign and sustainable C- and N- functionalization strategies.

Synthesis
Dr. B. R. Ambedkar National Institute of Technology Jalandhar (IN)
Life in Land
Openalex Percentile: Top 16%
Catalytic C–H Functionalization Methods
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