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Synthesis and Application of 1,2,3-Triazole Derivatives
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Synthesis and Application of 1,2,3-Triazole Derivatives

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Organic Chemistry".

Deadline for manuscript submissions: 30 September 2026 | Viewed by 1232

Special Issue Editors

Prof. Dr. Yubo Jiang

E-Mail Website
Guest Editor
Faculty of Science, Kunming University of Science and Technology, Kunming 650500, China
Interests: 1,2,3-triazole; heterocycle; cyclization; C-H bond activation; coupling reaction
Dr. Guiping Qin

E-Mail Website
Guest Editor Assistant
Faculty of Science, Kunming University of Science and Technology, Kunming, China
Interests: cascade catalysis; reductive cross-couplings; radical couplings; dicarbofunctionalization of alkenes; construction of all-carbon quaternary centers

Special Issue Information

Dear Colleagues,

1,2,3-triazole derivatives represent a privileged class of nitrogen-containing heterocycles with immense significance across diverse scientific disciplines. Their synthesis has been revolutionized by the advent of click chemistry, particularly the highly efficient, regioselective, and modular copper(I)-catalyzed azide–alkyne cycloaddition (CuAAC) reaction founded by Sharpless and Meldal Groups at the beginning of this century, allowing for rapid generation of extensive libraries of structurally diverse derivatives. The unique structural features of the triazole ring—including stability under physiological conditions, hydrogen bonding capability, dipole moment, and robust aromatic character—contribute to its remarkable versatility. Consequently, 1,2,3-triazole derivatives exhibit a wide spectrum of biological activities, driving extensive exploration in pharmaceutical chemistry as potent antimicrobials, anticancer agents, antivirals, anti-inflammatory agents, and CNS modulators. Beyond medicinal chemistry, these compounds find crucial applications as agrochemicals, corrosion inhibitors for metals, fluorescent sensors and probes, ligands in catalysis, and building blocks for functional polymers and advanced materials. Moreover, 1,2,3-triazole derivatives play remarkable roles in organic synthesis, participating in both ring-retaining and ring-opening processes.

This Special Issue invites original papers and reviews focusing on 1,2,3-triazoles, including their original synthesis, direct modifications, transannulative transformations, and applications in various fields.

Prof. Dr. Yubo Jiang
Guest Editor

Dr. Guiping Qin
Guest Editor Assistant

Manuscript Submission Information

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Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • 1,2,3-triazoles
  • synthesis
  • modification
  • transannulation
  • application

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Published Papers (2 papers)

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Research

11 pages, 1008 KB  
Article
Synthesis, Physical and Ion-Conducting Properties of 1,2,3-Triazolium Ionic Liquids
by Imen Abdelhedi Miladi, Maha Chikhaoui, Malak Alaa Eddine, Anatoli Serghei, Hatem Ben Romdhane and Eric Drockenmuller
Molecules 2026, 31(6), 936; https://doi.org/10.3390/molecules31060936 - 11 Mar 2026
Viewed by 325
Abstract
1,4-Disubstituted 1,2,3-triazoles are readily obtained by copper(I)-catalyzed azide–alkyne 1,3-dipolar cycloaddition (CuAAC)—the most widespread illustration of click chemistry to date. 1,2,3-Triazoles form a vast and easily accessible library of precursors for synthesizing 1,2,3-triazolium ionic liquids (TILs). A series of four 1,3,4-trisubstituted TILs with N [...] Read more.
1,4-Disubstituted 1,2,3-triazoles are readily obtained by copper(I)-catalyzed azide–alkyne 1,3-dipolar cycloaddition (CuAAC)—the most widespread illustration of click chemistry to date. 1,2,3-Triazoles form a vast and easily accessible library of precursors for synthesizing 1,2,3-triazolium ionic liquids (TILs). A series of four 1,3,4-trisubstituted TILs with N-1-n-octyl, N-3-methyl and different C-4 substituents (i.e., aromatic, aliphatic, PEGylated and perfluorinated groups) is synthesized in two steps involving: (i) CuAAC to generate 1,2,3-triazole precursors and (ii) N-alkylation of the 1,2,3-triazole groups with methyl iodide to afford the corresponding 1,2,3-triazolium salts with iodide counter-anions. A thorough investigation of the correlations between structure and properties is carried out using NMR spectroscopy, high-resolution mass spectrometry, differential scanning calorimetry, thermogravimetric analysis and broadband dielectric spectroscopy. The PEGylated TIL has also undergone ion metathesis to produce the TIL analogue with a bis(trifluoromethylsulfonyl)imide counter-anion. Of all the synthesized TILs, this derivative exhibits the lowest glass transition temperature (Tg = −76 °C), the highest thermal stability (Td10 = 345 °C) and the greatest ionic conductivity (σDC = 6.5 × 10−4 S cm−1 at 30 °C under anhydrous conditions). Full article
(This article belongs to the Special Issue Synthesis and Application of 1,2,3-Triazole Derivatives)
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12 pages, 677 KB  
Article
Mechano-Induced Synthesis of Polyethylene Glycols α,ω-DiSubstituted with 4-(PAH)-1H-1,2,3-Triazoles in Presence of In Situ-Generated Bronze Microparticles as Catalyst
by Mohammed S. Mohammed, Igor S. Kovalev, Vadim A. Platonov, Sougata Santra, Zhuo Wang, Grigory V. Zyryanov and Valery N. Charushin
Molecules 2026, 31(2), 270; https://doi.org/10.3390/molecules31020270 - 13 Jan 2026
Viewed by 357
Abstract
A method for the mechanochemical CuAAC click reaction (Cu+-promoted azido–alkyne cycloaddition) in the presence of bronze powder/copper beads without the use of a pre-introduced catalyst and ligands with greener prospect is presented. A new type of tri-, tetra-, and penta-ethylene glycols [...] Read more.
A method for the mechanochemical CuAAC click reaction (Cu+-promoted azido–alkyne cycloaddition) in the presence of bronze powder/copper beads without the use of a pre-introduced catalyst and ligands with greener prospect is presented. A new type of tri-, tetra-, and penta-ethylene glycols (PEGs) α,ω-disubstituted with 4-(PAH)-1H-1,2,3-triazole moieties has been synthesized by means of solvent-free click reaction in the planetary ball-milling in absence of a pre-introduced Cu(I) catalyst. The reaction afforded the above-mentioned compounds at room temperature in as short as 3 h in up to 96% yields and with E-factor values as low as 0.38. For the comparison, some of the key compounds were obtained by the conventional click synthesis in DMF solution. The compounds obtained were synthesized for the first time and can be considered as representative examples of bola-type chemosensors for the detection of electron-deficient species. This work presents a method for catalyzing a click reaction using bronze microparticles that are formed in situ during powder milling. This heterophase catalyst has been shown to be efficient and inexpensive and is suitable for green chemistry methods under solvent-free ball-milling conditions. Full article
(This article belongs to the Special Issue Synthesis and Application of 1,2,3-Triazole Derivatives)
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