有机化学 ›› 2015, Vol. 35 ›› Issue (2): 422-427.DOI: 10.6023/cjoc201406017 上一篇    下一篇

研究论文

含二氟甲基取代的吡唑酰胺类化合物的合成及杀菌活性

刘婷婷a, 倪芸a, 钟良坤a, 黄红英b, 胡伟群b, 许天明b, 谭成侠a   

  1. a 浙江工业大学化学工程学院 杭州 310014;
    b 中化蓝天集团有限公司 浙江省化工研究院有限公司 杭州 310023
  • 收稿日期:2014-06-13 修回日期:2014-09-22 出版日期:2015-02-25 发布日期:2014-10-22
  • 通讯作者: 谭成侠 E-mail:tanchengxia@zjut.edu.cn
  • 基金资助:

    “十二五”国家科技支撑计划(No. 2011BAE06B03-01)、浙江省重点科技创新团队(No. 2010R50018)资助项目.

Synthesis and Fungicidal Activity of Difluoromethy Substituted Carboxamide Derivatives

Liu Tingtinga, Ni Yuna, Zhong Liangkuna, Huang Hongyingb, Hu Weiqunb, Xu Tianmingb, Tan Chengxiaa   

  1. a College of Chemical Engineering, Zhejiang University of Technology, Hangzhou 310014;
    b Sinochem Lantian Zhejiang Research Institute of Chemical Industry Co. Ltd, Hangzhou 310023
  • Received:2014-06-13 Revised:2014-09-22 Online:2015-02-25 Published:2014-10-22
  • Supported by:

    Supported by the Key Innovation Team of Science and Technology in Zhejiang Province (No. 2010R50018), and the Project supported by the National Key Technologies R&D Program (No. 2011BAE06B03-01).

为了寻找高效安全的杀菌剂新品种和具有生物活性的新型先导化合物, 根据活性亚结构拼接原理, 将异噁唑和含氟基团引入到吡唑酰胺结构中, 设计了13个未见文献报道的含异噁唑的二氟甲基吡唑酰胺类化合物, 通过1H NMR, MS和HRMS对其结构进行了表征, 并对目标产物进行了初步的生物活性测定. 结果表明, 在剂量为200 mg/L时, 大部分化合物均表现出较高的杀菌活性.

关键词: 异噁唑, 吡唑酰胺, 合成, 杀菌活性

In the course of discovering novel fungicidal lead compounds with high activity and safety, 13 new difluoromethyl substituted carboxamide derivatives were designed and synthesized according to the principle of bioactive substructure combination. Their structures were confirmed by 1H NMR, MS and HRMS. The fungicidal activities of these compounds were evaluated. Preliminary bioassay showed that most of the title compounds showed good fungicidal activity at 200 mg/L.

Key words: isoxazole, pyrazole amides, synthesis, fungicidal activity