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Chin. J. Org. Chem. ›› 2010, Vol. 30 ›› Issue (08): 1207-1211. Previous Articles     Next Articles

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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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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