2-(1-取代苄基-1H-[1,2,3]三唑-4-甲硫基)-4,6-二甲基嘧啶类化合物的制备及生物活性评价  

Synthesis and biological activity evaluation of 2-(1-substituted benzyl-1H-[1,2,3]triazol-4-ylmethylsulfanyl)-4,6-dimethylpyrimidine derivatives

作　　者：张刚[1] 杓学蓓 李清寒[1] 杨学军[1] ZHANG Gang;SHAO Xue-bei;Li Qing-han;YANG Xue-jun(School of Chemistry and Environmental Protection Engineering, Southwest Minzu University, Chengdu 610041, P. R. C.)

机构地区：[1]西南民族大学化学与环境保护工程学院,中国成都610041

出　　处：《西南民族大学学报（自然科学版）》2018年第4期367-374,共8页Journal of Southwest Minzu University(Natural Science Edition)

基　　金：四川省科技支撑计划课题(2015NZ0033);西南民族大学"研究生创新型科研项目"(CX2016SZ056)

摘　　要：以2-巯基-4,6-二甲基嘧啶和3-溴丙炔为起始物,通过亲核取代反应制备了中间体2.再在铜盐的催化作用下,化合物2、取代苄溴和叠氮化钠经Click反应合成了12个新的2-(1-取代苄基-1H-\[1,2,3\]三唑-4-甲硫基)-4,6-二甲基嘧啶衍生物3(a^m),所有化合物的结构经IR、MS、~1HNMR及^(13)CNMR所确证.并在体外评价了化合物3(a^m)对细胞周期分裂蛋白25B(CDC25B)增殖的抑制作用.The intermediate 2 was synthesized with 2 - mercapto -4,6 - dimethylpyrimidine and 3 - bromo - propyne as starting material followed by substitution. Then thirteen new 2 - （ 1 - substituted benzyl - 1H - [ 1,2,3 ] triazol - 4 - ylmethylsulfanyl） - 4,6 - dimethylpyrimidine derivatives 3 （ a - m） were synthesized with compound 2, substituted benzyl bromide and sodium azid as starting material followed by click reaction via copper（I） iodide. Their structures were determined by IR, MS and ^1H and ^13C NMR data. The biological activities of compounds 3 （ a - m） were also evaluated concerning their inhibitions on cell divisiton cyclin 25 B functions.

关 键 词：2-巯基-4 6-二甲基嘧啶 1 2 3-三氮唑 铜催化 生物活性 

分 类 号：D621.29[政治法律—政治学] R914[政治法律—中外政治制度]