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有机化学
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有机化学 ›› 2010, Vol. 30 ›› Issue (08): 1207-1211. 上一篇    下一篇

研究论文

新型3-(α-羟基吲哚亚甲基)吡咯烷-2,4-二酮衍生物的合成与除草活性研究

朱有全*，朱然，袁燕伟，张金，王文虎，邹小毛*，胡方中，刘向明，杨华铮   

  1. (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:2009-10-23 修回日期:2010-03-04 发布日期:2010-03-30
  • 通讯作者: 朱有全 E-mail:zyq8165@nankai.edu.cn
  • 基金资助:

    国家级.国家自然科学基金

Synthesis and Bioactivities of Novel 3-[α-Hydroxy(indol-3-yl)- methylene]-pyrrolidine-2,4-dione Derivatives

ZHU You-Quan, ZHU Ran, YUAN Yan-Wei, ZHANG Jin, WANG Wen-Hu, ZOU Xiao-Mao, HU Fang-Zhong, LIU Xiang-Ming, YANG Hua-Zheng   

  1. (State Key Laboratory and Institute of Elemento-Organic Chemistry, Nankai University, Tianjin 300071)
  • Received:2009-10-23 Revised:2010-03-04 Published:2010-03-30

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为了进一步研究3-羟亚甲基吡咯烷-2,4-二酮类化合物构效关系, 以期发现高活性化合物, 利用生物等排原理引入具有芳香性的吲哚环, 合成了22个未见文献报道的新型3-羟亚甲基吡咯烷-2,4-二酮衍生物, 其结构均经过1H NMR和元素分析确证. 初步生物活性测试结果表明, 这些化合物均具有一定的除草活性. 初步的构效关系研究表明, 该类吡咯烷-2,4-二酮类化合物的除草活性与平面A和B的相对构型有关.

关键词: 吲哚, 吡咯烷-2,4-二酮, 合成, 除草活性, 构效关系

In order to further study the structure-activity relationships of the title compounds and find new kinds of herbicides, the aromatic indole ring was introduced and 22 new compounds were prepared by reaction of ketoacid esters with amio-acid esters. All of them have been confirmed by 1H NMR spectra and elemental analysis. The preliminary bioassay results indicated that all of them possessed some extent herbicidal activities. Preliminary quantitative structure-activity relationship (QSAR) analysis indicated that the herbicidal activity for pyrrolidine-2,4-dione derivatives was strongly related with the configuration for planes A and B.

Key words: indole, pyrrolidine-2,4-dione, synthesis, herbicidal activity, quantitative structure-activity relationship