Emerging Trends in Asymmetric Triazole Synthesis: from Click Chemistry to Biocatalysis

Triazole, also known as Pyrrolidazole, is a fundamental framework in heterocyclic chemistry. This is a five-membered aromatic compound consisting of three nitrogen atoms and two carbon atoms, which exist in two isomeric forms:1,2,3-triazole and 1,2,4-triazole. Both isomers exhibit a diverse range of applications across various domains, including materials science, medicinal chemistry, and catalysis. Despite their well-established advantages, triazole moieties are utilized as significant components in OLEDs, data storage devices, and organic photovoltaics. This review particularly emphasizes the recent advancements from 2020 to 2025, focusing on the asymmetric synthesis of triazole scaffolds and highlighting key methodologies ranging from copper-catalyzed azide-alkyne cycloaddition to biocatalytic strategies. Several studies have been reported about the development of innovative chiral ligands in conjunction with transition metals, including Ni, Rh, and Ir, leading to noble, efficient, and selective catalytic systems. Moreover, the present review article specifically explores the broad substrate scopes, reaction scalability, and detailed mechanistic insights that underscore the synthetic utility and versatility of these protocols. In addition, biocatalytic and chemoenzymatic approaches demonstrate the feasibility of sustainable and stereoselective synthesis of triazole-based antifungal agents. Overall, this mini-review not only guides the young researcher to develop new methodologies by carefully weighing their pros and cons but also equally assists the industrial scientist in designing bioactive heterocyclic compounds.