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有机化学
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有机化学 ›› 2010, Vol. 30 ›› Issue (08): 1255-1258. 上一篇    下一篇

研究简报

4-卤-5-(4-甲基-2H-1-苯并-2-吡喃酮-7-氧基)-2-取代-3(2H)-哒嗪酮衍生物的合成和生物活性研究

拜堃1，姚彩萍2，陈青2，沈忱2，裴文*,1   

  1. (1浙江工业大学化学工程与材料学院 杭州 310014)
    (2浙江工商大学应用化学系 杭州 310012)
  • 收稿日期:2009-11-20 修回日期:2010-03-30 发布日期:2010-04-09
  • 通讯作者: 裴文 E-mail:peiwen58@zjut.edu.cn

Synthesis and Bioactivity of 4-Halogen-5-[(4-methyl-2-oxo-2H-1-ben- zopyran-7-yl)oxy]-2-substituted-3(2H)-pyridazinone Deriva-tives

Bai Kun1 Yao Caiping2 Chen Qing2 Shen Chen2 Pei Wen*,1   

  1. (1 College of Chemical Engineering and Materials, Zhejiang University of Technology, Hangzhou 310014)
    (2 Department of Applied Chemistry, Zhejiang Gongshang Univer-sity, Hangzhou 310012)
  • Received:2009-11-20 Revised:2010-03-30 Published:2010-04-09
  • Contact: pei wen E-mail:peiwen58@zjut.edu.cn

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通过4,5-二氯(溴)-3(2H)-哒嗪酮与7-羟基-4-甲基香豆素在CH3CN/K2CO3体系下的缩合反应, 将具有生物活性的哒嗪酮环引入到苯并吡喃酮结构中, 设计、合成了9个含哒嗪酮环的香豆素类化合物, 其中8个为新化合物. 所有化合物的结构均经 NMR, MS和元素分析确证. 初步生物活性测试结果表明: 化合物4-氯-5-(4-甲基-2H-1-苯并吡喃-2-酮-7-氧基)-2-(4-硝基苯基)-3(2H)-哒嗪酮对黄瓜根部具有一定的抑制作用.

关键词: 香豆素, 哒嗪酮, 合成, 生物活性

Pyridazinone fragments were introduced into coumarin derivatives by the condensation of 4,5-dihalogenpyridazinone with 7-hydroxy-4-methyl coumarin in CH3CN/K2CO3 at reflux. Eight new compounds of pyridazinone derivatives containing coumarin ring were designed and synthesized. The structures of the new compounds were identified by 1H NMR and MS techniques and elemental analysis. The preliminary bio-assay results showed that 4-chloro-5-[(4-methyl-2-oxo-2H-1-benzopyran-7-yl)oxy]-2- (4-nitro-phenyl)-3(2H)-pyridazinone possessed restraining cucumber cotyledon root-formation ac-tivity.

Key words: coumarin, pyridazinone, synthesis, biological activity