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有机化学
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有机化学 ›› 2010, Vol. 30 ›› Issue (12): 1876-1883. 上一篇    下一篇

研究论文

6-甲基-4-(3-三氟甲基苯基)-3(2H)-哒嗪酮的合成与生物活性研究

许寒，胡绪红，刘斌，朱有全，邹小毛，胡方中，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:2010-01-26 修回日期:2010-06-03 发布日期:2010-07-22
  • 通讯作者: 许寒 E-mail:xuhan@mail.nankai.edu.cn

Synthesis and Herbicidal Activity of Novel 6-Methyl-4-(3-trifluoro- methylphenyl)pyridazin-3(2H)-one

XU Han, HU Xu-Hong, LIU Bin, ZHU You-Quan, ZOU Xiao-Mao, HU Fang-Zhong, YANG Hua-Zheng   

  1. (Institute of Elemento-Organic Chemistry, State Key Laboratory of Elemento-Organic Chemistry, Nankai University, Tianjin 300071)
  • Received:2010-01-26 Revised:2010-06-03 Published:2010-07-22

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在对3-三氟甲基-1,1 -联苯类衍生物类化合物进行CoMFA计算的基础上, 设计合成了化合物6-甲基-4-(3-三氟甲基苯基)-3(2H)-哒嗪酮(T-1), 分别采用小杯法、浮萍法和盆栽法对其除草活性进行了较详细的研究, 发现化合物T-1具有很好的白化活性和除草效果. 研究了T-1的合成路线, 实施了三条完全不同的路线进行合成, 比较了三条路线的优缺点.

关键词: 八氢番茄红素脱氢酶, 合成, 6-甲基-4-(3-三氟甲基苯基)-3(2H)-哒嗪酮, 白化活性, 除草活性

6-Methyl-4-(3-trifluoromethylphenyl)pyridazin-3(2H)-one (T-1) was designed and synthesized based on the comparative molecular field analysis (CoMFA) of three series herbicidal 3-trifluoromethyl- 1,1 -biphenyl derivatives inhibiting phytoene desaturase. Herbicidal activities of T-1 were evaluated through barnyardgrass, rape cup tests, Spirodela polyrrhiza (L.) and greenhouse test. T-1 exhibited good herbicidal and bleaching activites. Three methods for the preparation of T-1 were reported.

Key words: phytoene desaturase, synthesis, 6-methyl-4-(3-fluorotrimethylphenyl)pyridazin-3(2H)-one, bleaching activity, herbicidal activity