Recent Advances in Copper-Catalyzed C-H Arylation of Heteroarenes and Arenes

Transition metal-catalyzed C-H arylation has become an important area of research due to the significant applications of biaryl scaffolds in medicinal and synthetic organic chemistry, including ligand and analytical tool design. Among various transition metal catalysts, copper catalysts have gained considerable attention because of their wide availability and inexpensive and non-toxic nature. Because of these advantages, several copper-catalyzed C-H arylation protocols for aryl and heteroaryl substrates have been developed over the past few years. In these methods, various arylating precursors such as aryl halides, boronic acids, aryldiazonium salts, and diaryliodonium salts have been successfully employed to construct biaryl scaffolds. Some of these methods provide an efficient and straightforward route for constructing complex molecular frameworks, including natural products and pharmaceuticals. This review article provides a comprehensive overview of the latest developments in copper-catalyzed C-H arylation methods, highlighting current trends in the advancement of catalytic systems toward sustainability, various synthetic applications, and detailed mechanistic insights.

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Journal
Current Organic Chemistry
Published
2026-03-11
DOI
https://doi.org/10.2174/0113852728415347251208175245
Primary Topic
Catalytic C–H Functionalization Methods
Type
article
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article

Recent Advances in Copper-Catalyzed C-H Arylation of Heteroarenes and Arenes

Samir Mandal, Manash Kumar Manna, Sudip Sahana
Current Organic Chemistry
Catalytic C–H Functionalization Methods
article

Recent Advances in Copper-Catalyzed C-H Arylation of Heteroarenes and Arenes

Samir Mandal, Manash Kumar Manna, Sudip Sahana
article en

Abstract

Transition metal-catalyzed C-H arylation has become an important area of research due to the significant applications of biaryl scaffolds in medicinal and synthetic organic chemistry, including ligand and analytical tool design. Among various transition metal catalysts, copper catalysts have gained considerable attention because of their wide availability and inexpensive and non-toxic nature. Because of these advantages, several copper-catalyzed C-H arylation protocols for aryl and heteroaryl substrates have been developed over the past few years. In these methods, various arylating precursors such as aryl halides, boronic acids, aryldiazonium salts, and diaryliodonium salts have been successfully employed to construct biaryl scaffolds. Some of these methods provide an efficient and straightforward route for constructing complex molecular frameworks, including natural products and pharmaceuticals. This review article provides a comprehensive overview of the latest developments in copper-catalyzed C-H arylation methods, highlighting current trends in the advancement of catalytic systems toward sustainability, various synthetic applications, and detailed mechanistic insights.

Current Organic ChemistryVol. 30
Bankura University (IN)
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Openalex Percentile: Top 24%
Catalytic C–H Functionalization Methods
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