有机化学 ›› 2017, Vol. 37 ›› Issue (11): 3006-3012.DOI: 10.6023/cjoc201707022 上一篇    下一篇

研究简报

新型含七氟异丙基结构的吡唑酰胺类化合物的合成与杀虫活性研究

洪宇a, 戴红a, 叶林玉a, 仲苏林b, 曹雄飞a, 石玉军c, 李春建c, 石健a   

  1. a 南通大学化学化工学院 南通 226019;
    b 联合国南通农药剂型开发中心 南通 226006;
    c 南通大学分析测试中心 南通 226019
  • 收稿日期:2017-07-20 修回日期:2017-08-15 发布日期:2017-08-18
  • 通讯作者: 戴红, 石玉军 E-mail:yjshi2015@163.com;ntgao2016@163.com
  • 基金资助:

    国家自然科学基金(No.21372135)、江苏省“六大人才高峰”(No.2013-SWYY-013)、南通市科技计划(No.MS22015020)、江苏省大学生创新训练计划(No.201610304047Z)和南通大学研究生科研创新计划(No.YKC16086)资助项目.

Synthesis and Insecticidal Activities of Novel Pyrazole Amides Containing Heptafluoroisopropyl Moiety

Hong Yua, Dai Honga, Ye Linyua, Zhong Sulinb, Cao Xiongfeia, Shi Yujunc, Li Chunjianc, Shi Jiana   

  1. a College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019;
    b United Nations Nantong Pesticide Forulation Development Centre, Nantong 226006;
    c Analysis and Testing Center, Nantong University, Nantong 226019
  • Received:2017-07-20 Revised:2017-08-15 Published:2017-08-18
  • Contact: 10.6023/cjoc201707022 E-mail:yjshi2015@163.com;ntgao2016@163.com
  • Supported by:

    Project supported by the National Natural Science Foundation of China (No. 21372135), the Research Foundation of the Six People Peak of Jiangsu Province (No. 2013-SWYY-013), the Science and Technology Project Fund of Nantong City (No. MS22015020), the Science and Technology Innovation Foundation for the College Students of Jiangsu Province (No. 201610304047Z) and the Science and Technology Innovation Foundation for the Graduate Students of Nantong University (No. YKC16086).

为了寻找具有较好生物活性的吡唑类化合物,通过活性亚结构拼接的方法,设计并合成了一系列未见文献报道的新型含七氟异丙基结构的吡唑酰胺类衍生物.利用1H NMR、13C NMR和元素分析等手段确证了目标化合物的结构.初步的生物活性测试结果显示,部分目标化合物表现出较好的杀虫活性.在测试浓度为500 μg/mL时,有11个化合物对粘虫的杀灭活性可达60%~100%.当测试浓度降为100 μg/mL时,3个化合物对粘虫的杀死率可达60%~70%,优于对照药剂唑虫酰胺的药效.

关键词: 七氟异丙基, 吡唑, 合成, 杀虫活性

In order to find new pyrazole derivatives with potent biological activities, a series of novel pyrazole amides containing heptafluoroisopropyl moiety were prepared according to the method of active substructure combination. Their structures were characterized by 1H NMR, 13C NMR and elemental analysis. Preliminary bioassay data showed that some target compounds displayed good insecticidal activities. At the concentration of 500 μg/mL, eleven compounds had insecticidal activity against Oriental armyworm of 60%~100%. When the concentration was reduced to 100 μg/mL, three compounds showed insecticidal activity against Oriental armyworm of 60%~70%, better than that of the control tolfenpyrad.

Key words: heptafluoroisopropyl, pyrazole, synthesis, insecticidal activity