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有机化学
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有机化学 ›› 2005, Vol. 25 ›› Issue (04): 445-448. 上一篇    下一篇

研究简报

N-甲氧基-N-[2-(1,6-2H-1-取代-6-羰基-哒嗪-3-氧甲基)苯基]氨基甲酸甲酯的合成及生物活性研究

刘卫东*,1,3，李志伟2，李仲英2，王晓光1，高必达3   

  1. (1 湖南化工研究院国家南方农药创制中心湖南基地 长沙 410007）
    (2 湖南大学化学化工学院 长沙 410082)
    (3 湖南农业大学生物安全科技学院 长沙 410128)
  • 收稿日期:2004-07-12 修回日期:2004-10-28 发布日期:2005-03-30
  • 通讯作者: 刘卫东

Synthesis and Biological Activity of Methyl N-Methoxy-N-[2-(1,6-dihy-

LIU Wei-Dong*,1,3,LI Zhi-Wei2,LI Zhong-Ying2
WANG Xiao-Guang1,GAO Bi-Da3   

  1. (1 Hunan Research Institute of Chemical Industry, National Pesticide Research and Development Southern Center
    Hunan Branch, Changsha 410007)
    (2 College of Chem-istry and Chemical Engineering, Hunan University, Changsha 410082)
    (3 College of Bio-Safety Science and Technology, Hunan Agricultural University, Changsha 410128)
  • Received:2004-07-12 Revised:2004-10-28 Published:2005-03-30
  • Contact: LIU Wei-Dong

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为了寻找高效、低毒的农药, 设计合成了一系列新的N-甲氧基-N-[2-(1,6-2H-1-取代-6-羰基-哒嗪-3-氧甲基)苯基]氨基甲酸甲酯化合物3a～3k, 其结构经IR, 1H NMR, LC/MS和元素分析确认. 生物活性测定表明, 部分化合物在50 mg/L下对小麦赤霉病菌(Gibberella zeae)、稻瘟病菌(Pyricularia oryzae)和黄瓜灰霉病菌(Botrytis cinerea)有较好的抑菌活性.

关键词: 哒嗪酮, N-甲氧基氨基甲酸酯, 合成, 杀菌活性

In an attempt to find novel compounds with high activity and low toxicity, a series of novel methyl N-methoxy-N-[2-(1,6-dihydro-1-substituent-6-oxo-pyridazin-3-yloxymethyl)phenyl]carbamate derivatives 3a～3k were designed and synthesized by bioisoster principle. Their structures were confirmed by 1H NMR, IR, LC/MS spectra and elemental analysis. The preliminary biological activity tests show that some compounds possess fungicidal activities against Pyricularia oryzae, Botrytis cinerea and Erysiphe graminis.

Key words: N-methoxylcarbamate, synthesis, fungicidal activity, pyridazinone