无溶剂高效合成1,4-二取代-1,2,3-三唑类衍生物  

Efficient synthesis of 1,4-disubstituted-1,2,3-triazole derivatives without solvent

作　　者：万乐 卢俊瑞[1] 谢志强 刘金彪[1] WAN Le;LU Jun-rui;XIE Zhi-qiang;LIU Jin-biao(School of Chemistry and Chemical Engineering,Tianjin University of Technology,Tianjin 300384,China;Tianjin Ruiling Chemical Co.,Ltd.,Tianjin 300384,China)

机构地区：[1]天津理工大学化学化工学院,天津300384 [2]天津瑞岭化工有限公司,天津300384

出　　处：《天津理工大学学报》2020年第5期39-43,共5页Journal of Tianjin University of Technology

基　　金：国家自然科学基金(21476174,21176194).

摘　　要：1,2,3-三唑类化合物药动学和安全性良好,是新药发展的主流方向.本文在无溶剂条件下,以取代炔烃和叠氮化物为原料,研究探讨了不同铜离子催化剂对产率的影响,确定了最佳反应条件,在此基础上,经Click反应,成功合成出了一系列不同基团取代的1,4-二取代-1,2,3-三唑类衍生物.目标化合物的结构经1H NMR、13C NMR和高分辨质谱(HRMS)确证.该方法所得目标化合物收率良好且官能团容忍性强,具有简单、高效、绿色经济的特点,符合绿色化学和原子经济性的理念要求.1,2,3-triazole compounds have good pharmacokinetics and safety,and are the main direction of new drug development.In this paper,taking the substituent alkynes and azides as the reaction substrates,the effects of different copper ion catalysts on yields were studied.With the optimum conditions determined,a series of 1,4-disubstituted-1,2,3-triazole derivatives were successfully synthesized by Click reaction.The structure of the target compounds was confirmed by 1H NMR,13C NMR and HRMS.This method that avoids the environmental pollution caused by the solvent in the traditional method,and has strong functional group tolerance and good yields of the target compounds,which is simple,efficient and green-economic,and meets the concept requirements of green chemistry and atomic economy.

关 键 词：1 4-二取代-1 2 3-三唑 无溶剂 CLICK反应 绿色高效 

分 类 号：O626.26[理学—有机化学]