Chin. J. Org. Chem. ›› 2017, Vol. 37 ›› Issue (4): 1020-1026.DOI: 10.6023/cjoc201611042 Previous Articles     Next Articles



戴红a, 叶林玉a, 李阳b, 方源b, 石玉军a,b, 梁志鹏c, 石健c   

  1. a. 南通大学化学化工学院 南通 226019;
    b. 江苏科技大学环境与化学工程学院 镇江 212003;
    c. 南通大学分析测试中心 南通 226019
  • 收稿日期:2016-11-30 修回日期:2017-01-04 发布日期:2017-01-17
  • 通讯作者: 石玉军, 石健;
  • 基金资助:


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

Dai Honga, Ye Linyua, Li Yangb, Fang Yuanb, Shi Yujuna,b, Liang Zhipengc, Shi Jianc   

  1. a. College of Chemistry and Chemical Engineering, Nantong University, Nantong 226019;
    b. School of Environmental and Chemical Engineering, Jiangsu University of Science and Technology, Zhenjiang 212003;
    c. Analysis and Testing Center, Nantong University, Nantong 226019
  • Received:2016-11-30 Revised:2017-01-04 Published:2017-01-17
  • Contact: 10.6023/cjoc201611042;
  • 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), and the Science and Technology Innovation Foundation for the Graduate Students of Nantong University (No. YKC16086).

In order to explore novel potent pesticide from pyrazole oxime derivatives, a series of new pyrazole oxime compounds carrying substituted pyrimidine moiety were synthesized by the method of active substructure combination. The structures of the title compounds were characterized by 1H NMR, 13C NMR, MS and elemental analysis. Preliminary bioassay data displayed that some target compounds showed certain insecticidal activities. At the concentration of 500 μg/mL, compounds 6b and 6c exhibited 60% and 70% insecticidal activity against Aphis craccivora, compounds 6a, 6b, 6c, and 6d had 100%, 100%, 100% and 90% insecticidal activity against Nilaparvata lugens. When the concentration was reduced to 100 μg/mL, compounds 6a, 6b and 6d were still active against Nilaparvata lugens with inhibitory values of 60%, 60% and 50%, respectively. In addition, insecticidal activities against Oriental armyworm of compounds 6f, 6g and 6m were 80%, 70% and 90%, respectively, at 500 μg/mL.

Key words: pyrimidine, pyrazole oxime, synthesis, bioactivity