Synthesis methods of 1,2,3-/1,2,4-triazoles: A review

Abstract

Triazole, comprising three nitrogen atoms and two carbon atoms, is divided into two isomers 1,2,3-triazole and 1,2,4-triazole. Compounds containing a triazole are one of the significant heterocycles that exhibit broad biological activities, such as antimicrobial, analgesic, anti-inflammatory, anticonvulsant, antineoplastic, antimalarial, antiviral, antiproliferative, and anticancer activities. A great quantity of drugs with a triazole structure has been developed and proved, for example, ketoconazole and fluconazole. Given the importance of the triazole scaffold, its synthesis has attracted much attention. This review summarizes the synthetic methods of triazole compounds from various nitrogen sources in the past 20 years.

Recent Advancements in Triazole-based Click Chemistry in Cancer Drug Discovery and Development

“…There are many methods for the synthesis of triazole rings but click chemistry is a rapid, selective, and reliable method for triazole synthesis. 14,15 Since its introduction by Meldal and Sharpless 14,16 click chemistry has been used in polymers, 17,18 materials science, [19][20][21][22][23][24] drug discovery, [25][26][27] bioconjugation, [28][29][30][31][32] and organic chemistry. [33][34][35][36][37][38] The most common reaction in click chemistry is the copper(I)-catalyzed 1,3-dipolar cycloaddition of alkynes and azides to form 1,2,3-triazoles.…”

“…Figure15 Structures of 6-(4-((substituted-1H-1,2,3-triazol-4-yl)methyl)piperazin-1-yl)phenanthridine compound 7g and 7h81 …”

An overview of the privileged synthetic heterocycles as urease enzyme inhibitors: Structure–activity relationship

“…[ 60 ] This molecule facilitates the creation of a diversity of noncovalent bonds with receptors and enzymes persuading a wide range of biological activities such as anticancer, antituberculosis, antibacterial, and anti‐HIV. [ 61 ] Triazole has identified two isomers including 1,2,4‐triazole and 1,2,3‐triazole. Their derivatives have been extensively used in many medicinal scaffolds.…”

Regioselective Access to 1,2,4-Triazole-Fused N-Heterocycle, Pyrrolo[1,2-a][1,2,4]triazolo[5,1-c]pyrazine, via Double Dehydrative Cyclizations

“…1,2,4-Triazole has been widely employed as a key structure of numerous bioactive small molecules (Figure ). Indeed, it is a substructure of many therapeutic agents being developed as well as clinically used medicines such as triazolam, trapidil, and sitagliptin. Despite its prevalence in functional chemicals, 1,2,4-triazole-fused ring systems have been relatively less explored .…”