Immediately after the invention of ‘Click Chemistry’ in 2002, the regioselective 1,2,3-triazole scaffolds resulted from respective organic azides and terminal alkynes under Cu(I) cataly-sis have been well recognized as the functional heterocyclic core at the centre of modern organic chemistry, medicinal chemistry, and material sciences. This CuAAC reaction has several notable features including excellent regioselectivity, high-to-excellent yields, easy to execute, short reac-tion time, modular in nature, mild condition, readily available starting materials, etc. Moreover, the resulting regioselective triazoles can serve as amide bond isosteres, a privileged functional group in drug discovery and development. More than hundreds of reviews had been devoted to the ‘Click Chemistry’ in special reference to 1,4-disubstituted triazoles, while only little efforts were made for an opposite regioisomer i.e., 1,5-disubstituted triazole. Herein, we have presented vari-ous classical approaches for an expeditious synthesis of a wide range of biologically relevant 1,5-disubstituted 1,2,3-triazole analogues. The syntheses of such a class of diversly functionalized tri-azoles have emerged as a crucial investigation in the domain of chemistry and biology. This tuto-rial review covers the literature assessment on the development of various synthetic protocols for the functionalized 1,5-disubstituted triazoles reported during the last 12 years.

中文翻译：

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功能化1,5-二取代三唑的合成最新进展

2002年“点击化学”发明后不久，在Cu(I)催化下由各自的有机叠氮化物和末端炔烃产生的区域选择性1,2,3-三唑支架已被公认为中心的功能性杂环核现代有机化学、药物化学和材料科学。该CuAAC反应具有优异的区域选择性、高产率、易于执行、反应时间短、模块化、条件温和、起始原料易得等显着特点。此外，所得的区域选择性三唑可用于作为酰胺键等排体，是药物发现和开发中的特殊官能团。超过数百篇评论专门针对“点击化学”，特别涉及 1,4-二取代三唑，而对相反的区域异构体（即 1,5-二取代三唑）的研究却很少。在此，我们提出了各种经典方法，用于快速合成各种生物学相关的 1,5-二取代 1,2,3-三唑类似物。此类多官能化三唑的合成已成为化学和生物学领域的一项重要研究。本教程综述涵盖了过去 12 年报道的功能化 1,5-二取代三唑的各种合成方案开发的文献评估。