铜粉催化三氮唑与芳硼酸的交叉偶联反应研究（英文）  

Copper Powder-catalyzed Cross CouplingReaction of 1H-1,2,3-Triazoles with Aryl Boronic Acids

作　　者：张文莹 董涛生 王天昀 杜正银[1] ZHANG Wen-ying;DONG Tao-sheng;WANG Tian-yun;DU Zheng-yin(School of Chemistry and Chemical Engineering,Northwest Normal University,Lanzhou 730070,China)

机构地区：[1]西北师范大学化学化工学院

出　　处：《聊城大学学报（自然科学版）》2019年第6期35-43,共9页Journal of Liaocheng University:Natural Science Edition

基　　金：国家自然科学基金项目(21762039)资助

摘　　要：三氮唑类化合物是一类重要的有机杂环化合物,也是很多农药、医药和有机合成中间体的合成砌块.许多含有1,2,3-三氮唑结构单元的化合物表现出良好的抗菌、消炎、抗癌等生物活性.以市售铜粉作为催化剂,以芳硼酸作为芳基化试剂,研究了1H-1,2,3-三氮唑与芳硼酸的交叉偶联反应.结果表明,1H-1,2,3-三氮唑发生了N-芳基化反应,生成了N1-芳基和N2-芳基三氮唑的异构化产物,总收率最高87%,二者的比例约为(2-5):1.当取代的1H-1,2,3-苯并三氮唑作为反应底物时,N1-芳基化产物又出现了两种不易分离的位置异构体.The cross-coupling reaction between 1 H -1,2,3-triazoles and aryl boronic acids catalyzed by copper powder is studied.N1-aryl and N2-aryl-1,2,3-trizaoles were obtained in the presence of cesium carbonate in acetonitrile under reflux temperature.The total yields were up to 87% with N1-arylation isomers as major products.This method shows good tolerance of various substituents attaching on benzene ring of benzotriazoles and aryl boronic acids.

关 键 词：三氮唑 芳基硼酸 交叉偶联反应 铜粉 N-芳基化反应 

分 类 号：O625[理学—有机化学]