3-甲基-5-芳基吡唑[3,4-e]并-1,2,3,4-四嗪衍生物的合成  

Synthesizing of 5-Aryl-3-Methylpyrazole[3,4-E][1,2,3,4]Tetrazines

作　　者：成学丽[1] 吴冬梅[1] 杨巧荷[1] 鲁源[1] 

机构地区：[1]内蒙古医学院药学院,内蒙古呼和浩特010059

出　　处：《疾病监测与控制》2010年第9期513-514,共2页Journal of Diseases Monitor and Control

摘　　要：目的为了寻找干扰核酸代谢的抗肿瘤新药,设计和合成嘌呤生物碱的类似物—吡唑[3,4-e]并-1,2,3,4-四嗪衍生物是有意义的。方法以3-甲基-5-氨基-1H-吡唑为原料,经过重氮化、偶合和分子内关环合成目标化合物3-甲基-5-芳基吡唑[3,4-e]并-1,2,3,4-四嗪衍生物。结果合成了八个新的嘌呤类似物。结论所得化合物,通过IR、1H-NMR、元素分析和质谱分析证实为目标化合物。Objective In order to search the new anti-cancer drugs that disturb nucleic acid metabolizing,we designed and synthesized purine base analogues—pyrazole[3,4-e][1,2,3,4]tetrazines which is significative.Methods The objective compounds—5-aryl-3-methylpyrazole[3,4-e][1,2,3,4]tetrazines were synthesized via diazotization,coupling and intramolecular cyclization,using 5-amino-3-methyl-1-H-pyrazoles as materials.Result Eight new purine analogues were synthesized.Conclusion The resulting compounds were all identical to the objective compounds by IR,~1H-NMR,MS and element analysis.

关 键 词：吡唑[3 4-e]并[1 2 3 4]四嗪 合成 抗肿瘤药 

分 类 号：R914.1[医药卫生—药物化学]