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有机化学
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有机化学 ›› 2005, Vol. 25 ›› Issue (11): 1477-1481. 上一篇    下一篇

研究简报

含噁二唑杂环取代的新型三唑并嘧啶衍生物的合成及其生物活性

陈悟1，陈琼2，吴琼友2，杨光富*,2   

  1. (1华中科技大学生命科学与技术学院 武汉 430074)
    (2华中师范大学化学学院 农药与化学生物学教育部重点实验室 武汉 430079)
  • 收稿日期:2005-04-02 修回日期:2005-05-23 发布日期:2005-10-30
  • 通讯作者: 杨光富

Synthesis and Fungicidal Evaluation of Novel 1,2,4-Triazolo[1,5-a]- pyrimidine Containing Oxadiazolyl De-rivatives

CHEN Wu1,CHEN Qiong2,WU Qiong-You2,YANG Guang-Fu*,2   

  1. (1 College of Life Science and Technology, Huazhong University of Science and Technology, Wuhan 430074)
    (2 Key Laboratory of Pesticide & Chemical Biology, Ministry of Educa-tion, College of Chemistry, Central China Normal
    University, Wuhan 430079)
  • Received:2005-04-02 Revised:2005-05-23 Published:2005-10-30
  • Contact: YANG Guang-Fu

被引次数

82

2-肼羰基亚甲硫基-5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶与二硫化碳在乙醇溶液中回流制得化合物2-(5-巯基-1,3,4-噁二唑-2-亚甲硫基)-5,7-二甲基-1,2,4-三唑并[1,5-a]嘧啶, 后者在碱性环境中与卤化苄反应得到17种新型双杂环化合物. 对所得化合物结构均经元素分析, 1H NMR和MS确认. 初步生物活性测试表明这些化合物具有一定的杀菌活性.

关键词: 三唑并嘧啶, 1,3,4-噁二唑, 生物活性

Reaction of 2-hydrazinocarbonylmethenethio-5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidine with carbon disulfide in refluxing ethanol afforded 2-(5-mercapto-1,3,4-oxadiazol-2-ylmethylthio)-5,7-di-methyl-1,2,4-triazolo[1,5-a]pyrimidine, which was then treated with various benzyl halide in basic condition to yield 17 novel biheterocyclic derivatives. The structures of all compounds obtained were con-firmed by elemental analyses, 1H NMR and MS. Preliminary bioassay indicates that some compounds display antibacterial activity to certain extent.

Key words: 1,3,4-oxadiazole, bioactivity, 1,2,4-triazolo[1,5-a]pyrimidine