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DOI: 10.1055/a-2564-4826
Regioselective Synthesis of 1,4-Disubstituted 1,2,3-Triazoles: Advances in Click Chemistry and Multicomponent Reaction Engineering
D.S. and K.D. are thankful to Council of Scientific and Industrial Research (CSIR), New Delhi, India for the research grant [Grant No. 02(0399)/21/EMR-II]. P.G. thanks CSIR, New Delhi for research fellowship. We sincerely thank DST for financial support under Department of Science and Technology PURSE (DST-PURSE) project (SR/PURSE/2022/143 (C)) and Department of Science and Technology FIST (DST-FIST) project (SR/FST/CS-I/2020/152).

Abstract
The regioselective synthesis of 1,2,3-triazoles has emerged as a cornerstone of modern synthetic chemistry, offering immense potential in pharmaceuticals, materials science, and functional applications. This account focuses on advancing the click reaction with an emphasis on the innovations stemming from the contributions from our group. Highlights include the development of novel catalytic systems, both homogeneous and heterogeneous, and the exploration of copper-free and photocatalytic methodologies. This account bridges traditional and modern approaches, offering mechanistic insights and engineering strategies to improve regioselectivity and efficiency. This work envisions a transformative feature for azide–alkyne cycloaddition, advancing from copper-based or copper-free catalysis to light-driven innovations.
1 Introduction
2 Fundamentals and Mechanistic Insights of the CuAAC
3 Homogeneous Catalysts for Regioselective AAC
3.1 Copper-Catalyzed Homogeneous Catalytic Systems
3.2 Copper-Free Homogeneous Catalytic Systems
4 AAC Reactions Using Heterogeneous Catalysts
4.1 Copper-Based Catalysts on Solid Supports
4.2 Copper-Free Heterogeneous Catalytic Systems
5 AAC Using Non-conventional Sources of Energy
5.1 Microwave-Assisted Synthesis
5.2 Ultrasound-Assisted Synthesis
5.3 Photocatalytic AAC (PcAAC) Reactions
6 Some Applications of 1,2,3-Triazoles
7 Concluding Remarks and Future Scope
Key words
click reaction - regioselectivity - azide–alkyne cycloaddition - multicomponent reaction - triazoles - light-mediatedPublication History
Received: 31 January 2025
Accepted after revision: 21 March 2025
Accepted Manuscript online:
21 March 2025
Article published online:
21 May 2025
© 2025. Thieme. All rights reserved
Georg Thieme Verlag KG
Oswald-Hesse-Straße 50, 70469 Stuttgart, Germany
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