有机化学 ›› 2020, Vol. 40 ›› Issue (6): 1665-1672.DOI: 10.6023/cjoc202001029 上一篇    下一篇

研究论文

含噻唑环结构的新型吡唑酰胺类化合物的合成与杀虫活性研究

梁凯a, 周钱a, 荀校a, 倪亚丹a, 李金峰a, 石玉军a, 周环宇a, 吴新星a, 石健b, 高磊a, 戴红a   

  1. a 南通大学化学化工学院 江苏南通 226019;
    b 南通大学分析测试中心 江苏南通 226019
  • 收稿日期:2020-01-22 修回日期:2020-02-25 发布日期:2020-03-04
  • 通讯作者: 石玉军, 吴新星, 戴红 E-mail:yjshi2015@163.com;wuxinxng@163.com;daihong_2015@aliyun.com
  • 基金资助:
    国家自然科学基金(Nos.21372135)、南通市科技计划(No.MS12019060)和南通大学高层次人才(No.03083031)资助项目.

Synthesis and Insecticidal Activities of Novel Pyrazole Amide Derivatives Containing a Thiazole Unit

Liang Kaia, Zhou Qiana, Xun Xiaoa, Ni Yadana, Li Jinfenga, Shi Yujuna, Zhou Huanyua, Wu Xinxinga, Shi Jianb, Gao Leia, Dai Honga   

  1. a College of Chemistry and Chemical Engineering, Nantong University, Nantong, Jiangshu 226019;
    b Analysis and Testing Center, Nantong University, Nantong, Jiangshu 226019
  • Received:2020-01-22 Revised:2020-02-25 Published:2020-03-04
  • Supported by:
    Project supported by the National Natural Science Foundation of China (No. 21372135), the Science and Technology Project Fund of Nantong City (No. MS12019060) and the Program of High-level Talents of Nantong University (No. 03083031).

为了探索新的吡唑酰胺活性物质,基于吡螨胺的结构,将噻唑环通过酰胺键同吡唑环相连,合成了18个未见文献报道的吡唑酰胺类化合物,通过1H NMR,13C NMR和元素分析等手段确证了其结构.生物活性测试研究显示,所有目标化合物在500 μg/mL时对粘虫都有100%的杀虫活性.7个目标化合物在500 μg/mL时对蚜虫具有70%~100%的防治效果.同时,3个目标化合物在500 μg/mL时对朱砂叶螨显示出40%~50%的防效.

关键词: 噻唑, 吡唑酰胺, 合成, 杀虫活性

In search of novel pyrazole amide compounds possessing good biological activities, a series of pyrazole amides were synthesized by introducing thiazole unit into pyrazole ring via amido bond, based on the lead of tebufenpyrad. The title compounds were structurually confirmed by 1H NMR, 13C NMR and elemental analysis. Preliminary bioassay displayed that all the title compounds exhibited 100% insecticidal activities against Oriental armyworm at 500 μg/mL. At the concentration of 500 μg/mL, seven compounds showed 70%~100% mortality rate against Aphis medicaginis. In addition, three compounds had 40%~50% insecticidal activity against Tetranychus cinnabarinus at 500 μg/mL.

Key words: thiazole, pyrazole amide, synthesis, insecticidal activity