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有机化学 ›› 2005, Vol. 25 ›› Issue (03): 304-307. 上一篇    下一篇

研究论文

多卤代苯甲酰基脲类几丁质抑制剂的合成及杀虫活性多卤代苯甲酰基脲类几丁质抑制剂的合成及杀虫活性

林军*,1,2，严胜骄1,2，杨丽娟1,2，李俊峰1，刘复初1   

  1. (1云南大学应用化学系 云南大学生物制药创新人才培养基地 昆明 650091)
    (2南开大学元素有机化学研究所 元素有机化学国家重点实验室 天津 300071)
  • 收稿日期:2004-03-12 修回日期:2004-09-23 发布日期:2005-02-28
  • 通讯作者: 林军

Synthesis and Insecticidal Activities of Novel Polyhalo Benzoyl-phenylurea Derivatives

LIN Jun*,1,2,YAN Sheng-Jiao1,2,YANG Li-Juan1,2,LI Jun-Feng1,LIU Fu-Chu1   

  1. (1 Department of Applied Chemistry, Center for Advanced Studies of Medicinal and Organic Chemis-try,
    Yunnan University, Kunming 650091)
    (2 State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071)
  • Received:2004-03-12 Revised:2004-09-23 Published:2005-02-28
  • Contact: LIN Jun

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从易得原料百菌清1出发, 经过氟交换、氨解、水解、脱羧和酰化反应, 合成得到10个新的多卤代苯甲酰基脲类几丁质抑制剂衍生物, 总收率为30%～50%. 所有化合物经1H NMR, HREIMS, IR光谱证实. 对化合物进行了生物活性筛选, 结果表明该类化合物对粘虫和蚊幼虫均有一定的杀虫活性.

关键词: 百菌清, 苯甲酰基脲, 杀虫活性, 几丁质抑制剂

Ten novel polyhalo benzoylphenylurea chitin inhibitor derivatives have been synthesized in over 30%～50% yields from readily available starting material chlorothalonil 1 via fluorine exchange, aminolysis, decarboxylation and acylation reactions. All products were characterized by 1H NMR, HREIMS and IR spectra. Preliminary bioactive research showed that some of the synthesized compounds have the potential insecticidal activities against Mythimna separata and Culex pipiens pallens.

Key words: chitin inhibitor, insecticidal activity, benzoylphenylurea, chlorothalonil