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有机化学
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有机化学 ›› 2010, Vol. 30 ›› Issue (12): 1870-1875. 上一篇    下一篇

研究论文

瑞香酮类似物的合成与生物活性研究

杨绍祥1，康铁牛1，杨新玲1，孙玉凤1，芮昌辉2，凌云*,1   

  1. (1中国农业大学理学院应用化学系 农业部农药化学与应用重点开放实验室 北京 100193)
    (2中国农业科学院植物保护研究所 北京 100193)
  • 收稿日期:2010-05-05 修回日期:2010-07-20 发布日期:2010-07-20
  • 通讯作者: 凌云 E-mail:lyun@cau.edu.cn
  • 基金资助:

    国家“863”计划和国家重点基础研究发展计划（973计划)资助项目

Synthesis and Biological Activities of Daphneolone Analogues

Yang Shaoxiang1 Kang Tieniu1 Yang Xinling1 Sun Yufeng1 Rui Changhui2 Ling Yun*,1   

  1. (1 Key Laboratory of Pesticide Chemistry and Application, Ministry of Agriculture, Department of Applied Chemistry, College of Science, China Agricultural University, Beijing 100193)
    (2 Institute of Plant Protection, Chinese Academy of Agricultural Sciences, Beijing 100193)
  • Received:2010-05-05 Revised:2010-07-20 Published:2010-07-20

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1337

被引次数

12 | 1

以瑞香狼毒(Stellera chamaejasme L.)中分离得到的天然产物(E)-1,5-二苯基-2-烯-1-戊酮(I)为先导, 用不同的含氮杂环取代1-苯基, 设计合成了8个未见报道的化合物, 其结构均经过1H NMR, IR和元素分析确证. 初步生物活性测试表明, 目标化合物在600 μg/mL浓度下表现出一定的杀蚜活性, 其中化合物6a对棉蚜的校正死亡率为92.9%, 活性优于先导I.

关键词: 瑞香狼毒, (E)-1,5-二苯基-2-戊烯-1-酮, 类似物, 合成, 杀蚜活性

The botanical aphicide (E)-1,5-diphenyl-1-penten -1-one (I) from Stellera chamaejasme L. as the lead compound, 8 new compounds were designed and synthesized in which 1-phenyl was replaced by different nitrogen heterocycles. Their structures were confirmed by 1H NMR, IR spectra and elemental analysis. The results of biological tests indicated that these compounds showed insecticidal activity against Aphis gossypii at 600 mg/mL, especially compound 6a (corrected mortality is 92.9%) showed higher activity than I.

Key words: Stellera chamaejasme L., (E)-1,5-diphenyl-1-penten-1-one, analogues, synthesis, aphicidal activity