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有机化学
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有机化学 ›› 2006, Vol. 26 ›› Issue (03): 337-340. 上一篇    下一篇

研究论文

2-氰基-3-(2-氟吡啶-5-基)甲氨基-3-甲硫基氰基丙烯酸酯类化合物的合成及除草活性

邹小毛，郁丽敏，高颍，施欢乐，裴江，刘斌
李慧芬，胡方中，杨华铮*   

  1. (南开大学元素有机化学国家重点实验室 元素有机化学研究所 天津 300071)
  • 收稿日期:2005-01-30 修回日期:2005-09-28 发布日期:2006-02-28
  • 通讯作者: 杨华铮

Synthesis and Herbicidal Activity of 2-Cyano-3-(2-fluoropyrid-5-yl)- methylamino-3-methylthioacrylates

ZOU Xiao-Mao,YU Li-Min,GAO Yin,SHI Huan-Le,PEI Jiang,LIU Bin
LI Hui-Fen,HU Fang-Zhong,YANG Hua-Zheng*   

  1. (State Key Laboratory of Elemento-Organic Chemistry, Institute of Elemento-organic Chemistry,
    Nankai University, Tianjin 300071)
  • Received:2005-01-30 Revised:2005-09-28 Published:2006-02-28
  • Contact: YANG Hua-Zheng

PDF

2251

被引次数

31

设计合成了系列光系统II (PS-II)电子传递抑制剂2-氰基-3-(2-氟吡啶-5-基)甲氨基-3-甲硫基氰基丙烯酸酯类化合物. 其结构经1H NMR、元素分析确证. 生物活性测定表明: 部分化合物显示出很好的除草活性. 其中活性最好的化合物在150 g/ha, 对阔叶杂草的防效在90%以上. 构效关系研究表明: 氰基丙烯酸酯的3位取代基对它们的活性影响较大. 3位由(2-氟吡啶-5-基)甲氨基取代的氰基丙烯酸酯和相应的氯取代的氰基丙烯酸酯的除草活性相当或稍高.

关键词: 2-氰基-3-(2-氟吡啶-5-基)甲氨基-3-甲硫基氰基丙烯酸酯, 除草活性, 构效关系, 光系统II (PS-II)电子传递抑制剂

A series of 2-cyano-3-(2-fluoropyrid-5-yl)methylamino-3-methylthioacrylates were synthesized as herbicidal inhibitors of photosynthesis II electron transport and some of these compounds exhibited good herbicidal activities. A suitable group at the 3-position of acrylate is essential for high herbicidal activity. 2-Cyanoacrylates containing a 2-fluoro-5-pyridyl group may be provided higher herbicidal activities than relevant chloride derivatives.

Key words: herbicidal activity, SAR, 2-cyano-3-(2-fluoropyrid-5-yl)methylamino-3- methylthioacrylate, inhibitor of photosynthesis II electron transport