This review highlights innovative synthetic methodologies for 1,2,3‐triazoles, emphasizing their role in drug discovery.
ABSTRACT 1,2,3‐Triazoles have emerged as essential scaffolds in medicinal chemistry due to their versatile biological activities and bio‐isosteric properties. Several triazole‐containing drugs have received FDA approval, with many others undergoing clinical evaluation, highlighting their significance in drug discovery. In recent years, substantial progress has been made in developing efficient and sustainable synthetic methodologies for 1,2,3‐triazoles. This review provides a comprehensive overview of these advances, covering strategies such as transition metal‐catalyzed, organocatalyzed, heterogeneous, ionic liquid‐mediated, and metal‐free approaches from early 2018 to the present. The discussion emphasizes innovative modifications to established protocols and the exploration of novel reaction pathways that enable structural diversification. This compilation serves as a valuable resource for researchers aiming to expand the synthetic utility of triazole derivatives for pharmaceutical and material science applications.
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Alagarasan et al. (2025) studied this question.