含1,3,4-噻二唑环吡唑并[3,4-d]嘧啶类化合物的合成及生物活性有机化学.pdfVIP

DOI: 10.6023/cjoc1110081 研究简报 有机化学 Chinese Journal of Organic Chemistry NOTE 含1,3,4-噻二唑环吡唑并[3,4-d]嘧啶类化合物的合成及生物活性 宋新建*,a,b 邵 宇b 段正超b 李世荣a a ( 湖北民族学院生物资源保护与利用湖北省重点实验室 恩施 445000) (b 湖北民族学院化学与环境工程学院 恩施 445000) 摘要 通过 5-氨基-4-氰基-1-苯基吡唑与甲酸发生环合、再经氯化和芳香族亲核取代反应, 合成了 12 种新的含 1,3,4- 噻二唑环吡唑并[3,4-d]嘧啶类化合物. 目标化合物的结构经红外光谱、核磁共振氢谱、质谱和元素分析方法予以确认. 初步的生物活性测定试验表明, 在 50 mg/L 浓度下, 大部分目标化合物对小麦纹枯病菌(Rhizoctonia cerealis)表现出较 好的杀菌活性, 其中化合物 5b, 5d 和 5j 的抑菌率超过90%. 关键词 吡唑并[3,4-d]嘧啶; 1,3,4-噻二唑; 合成; 杀菌活性 Synthesis and Biological Activity of Pyrazolo[3,4-d]pyrimidine Derivatives Containing 1,3,4-Thiadiazole Song, Xinjian*,a,b Shao, Yub Duan, Zhengcaob Li, Shironga a ( Key Laboratory of Biological Resources Protection and Utilization of Hubei Province, Hubei University for Nationalities, Enshi 445000) b ( School of Chemical and Environmental Engineering, Hubei University for Nationalities, Enshi 445000) Abstract Twelve novel pyrazolo[3,4-d]pyrimidine derivatives containing a 1,3,4-thiadiazole group were synthesized through cyclization of 5-amino-4-cyano-1-phenylpyrazole with formic acid, followed by chloridization and S Ar reaction. The struc- N tures of all these title compounds were confirmed by IR, 1H NMR, MS techniques and elemental analysis. The preliminary bioassay showed th