Chin. J. Org. Chem. ›› 2010, Vol. 30 ›› Issue (9): 1347-1353. Previous Articles     Next Articles

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5-吡唑酰胺类化合物的合成及其杀虫活性研究

刘杰,谢化鹏,宋宝安*,胡德禹,杨松,金林红,薛伟,吴剑,徐维明   

  1. (贵州大学精细化工研究开发中心 绿色农药与农业生物工程教育部重点实验室和国家重点实验室培育基地
    贵阳 550025)
  • 收稿日期:2009-12-27 修回日期:2010-03-24 发布日期:2010-04-22
  • 通讯作者: 宋宝安 E-mail:gzgdjhzx@126.com;songbaoan22@yahoo.com;songbaoan1963@yahoo.com.cn

Synthesis and Insecticidal Activity of 5-Pyrazolecarboxamide Deriva-tives

LIU Jie, XIE Hua-Peng, SONG Bao-An, HU De-Yu, YANG Song, JIN Lin-Hong, XUE Wei, WU Jian, XU Wei-Ming   

  1. (State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricutural Bioengineering, Ministry of Education, Research and Development Center for Fine Chemicals, Guizhou University, Guiyang 550025)
  • Received:2009-12-27 Revised:2010-03-24 Published:2010-04-22

Ten 5-pyrazolecarboxamide derivatives were synthesized by the reaction of amine and intermediate 6 starting from 2,3-dichloropyridine and diethyl maleate. Their structures were identified by elemental analysis, IR, 1H NMR and 13C NMR spectra. The preliminary bioassay showed that compounds 7a7j had moderate insecticidal activities against Nilaparvata lugens (Stal), 7a and 7d possessed good insecticidal ac- tivity with the mortality rate of 57.6% and 64.4% at a concentration of 100 μg/mL, respectively, similarly to the control (buprofezin). Insecticidal mechanism of 7d indicated that it has a good inhibitive activity against Brown planthopper acetylcholinesterase with rate of 75.2% than the commercial control buprofezin (52.2%).

Key words: pyrazolecarboxamide derivative, acetylcholinesterase, synthesis, insecticidal activity