有机化学 ›› 2015, Vol. 35 ›› Issue (11): 2399-2404.DOI: 10.6023/cjoc201506004 上一篇    下一篇

研究简报

新型含取代吡啶环的取代吡唑甲醛肟的合成及生物活性测定

戴红a, 庄辉阳b, 施磊a, 李刚a, 张海军a, 方源a, 戴宝江b,c   

  1. a 南通大学化学化工学院 南通 226019;
    b 南通南沈植保科技开发有限公司 南通 226017;
    c 南通职业大学化学与生物工程学院 南通 226007
  • 收稿日期:2015-06-03 修回日期:2015-06-30 发布日期:2015-07-10
  • 通讯作者: 张海军, 戴宝江 E-mail:zhanghj2801@163.com;daibj2001@163.com
  • 基金资助:

    国家自然科学基金(Nos. 21202089, 21372135)和南通市科技计划(No. AS2013002)资助项目.

Synthesis and Biological Activities of Novel Substituted Pyrazole Oximes Containing Substituted Pyridine Group

Dai Honga, Zhuang Huiyangb, Shi Leia, Li Ganga, Zhang Haijuna, Fang Yuana, Dai Baojiangb,c   

  1. a College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019;
    b Nantong Nanshen Plant Protection Science and Technology Development Co. Ltd, Nantong 226017;
    c School of Chemical and Biological Engineering, Nantong Vocational University, Nantong 226007
  • Received:2015-06-03 Revised:2015-06-30 Published:2015-07-10
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 21202089, 21372135), and the Science and Technology Project Fund of Nantong City (No. AS2013002).

为了从吡唑肟类化合物中寻找新的活性物质, 利用活性亚结构拼接原理, 将取代吡啶骨架引入到吡唑肟分子结构中, 制备了一系列未见文献报道的新型含取代吡啶环结构的取代吡唑甲醛肟化合物. 通过核磁氢谱、碳谱和元素分析确证了新化合物的结构. 初步的生物活性测试结果显示, 某些标题化合物表现出一定的杀虫与杀螨活性. 其中化合物5i在浓度为400 μg/mL时对蚕豆蚜的杀死率达到90%.

关键词: 取代吡啶, 吡唑肟, 合成, 生物活性

In order to explore novel potent pesticide from pyrazole oxime derivatives, a series of new pyrazole oxime ester compounds bearing substituted pyridine moiety were synthesized by the introduction of pyridyl backbone into the molecules of pyrazole oxime. Their structures were confirmed by 1H NMR, 13C NMR and elemental analysis. Preliminary bioassay results showed that some of the title compounds displayed certain insecticidal and acaricidal activities. For example, compound 5i exhibited insecticidal activity against Aphis craccivora with 90% mortality at the concentration of 400 μg/mL.

Key words: substituted pyridine, pyrazole oxime, synthesis, bioactivity