Advances in Metal‐Catalyzed Buchwald–Hartwig Coupling for Bioactive Molecule Synthesis: A Review

ABSTRACT Metal‐catalyzed cross‐coupling reactions that form C–N bonds have become valuable methods for constructing various heterocyclic systems. The Buchwald–Hartwig amination reaction of aryl halides has attracted considerable attention in recent years for the synthesis of (hetero)arylamines, which are fundamental structures in natural products, medicines, and other physiologically active compounds. Our purpose here is to provide readers with information about recent advances in this strategy for C‐N bond formation, particularly in the construction of various heterocyclic systems. This review examines developments in Buchwald–Hartwig coupling for the synthesis of bioactive molecules from 2014 to the present.

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Journal
ChemistrySelect
Published
2026-03-01
DOI
https://doi.org/10.1002/slct.202507465
Primary Topic
Catalytic Cross-Coupling Reactions
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article
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Advances in Metal‐Catalyzed Buchwald–Hartwig Coupling for Bioactive Molecule Synthesis: A Review

Muhammad Imran, Aqsa Kanwal, Sadia Nazir, Uzma Afzal et al.
ChemistrySelect
Catalytic Cross-Coupling Reactions
article

Advances in Metal‐Catalyzed Buchwald–Hartwig Coupling for Bioactive Molecule Synthesis: A Review

Muhammad Imran, Aqsa Kanwal, Sadia Nazir, Uzma Afzal, Hasan A. Abbas, M. Waqas, Mahwish Arshad, Nasir Rasool
article en

Abstract

ABSTRACT Metal‐catalyzed cross‐coupling reactions that form C–N bonds have become valuable methods for constructing various heterocyclic systems. The Buchwald–Hartwig amination reaction of aryl halides has attracted considerable attention in recent years for the synthesis of (hetero)arylamines, which are fundamental structures in natural products, medicines, and other physiologically active compounds. Our purpose here is to provide readers with information about recent advances in this strategy for C‐N bond formation, particularly in the construction of various heterocyclic systems. This review examines developments in Buchwald–Hartwig coupling for the synthesis of bioactive molecules from 2014 to the present.

ChemistrySelectVol. 11(12)
University of Verona (IT), Government College University, Faisalabad (PK), Dalian University of Technology (CN), Dalian University (CN), Government College Women University Faisalabad (PK), University of Pennsylvania (US), King Khalid University (SA)
Openalex Percentile: Top 9%
Catalytic Cross-Coupling Reactions
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Advances in Metal‐Catalyzed Buchwald–Hartwig Coupling for Bioactive Molecule Synthesis: A Review — Muhammad Imran, Aqsa Kanwal, et al. · ChemistrySelect (2026) | TGRS Research Map | TGRS