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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

Synthesis and Biological Activity of Methyl N-Methoxy-N-[2-(1,6-dihy- dro-1-substituent-6-oxo-pyridazin-3-yloxymethyl)phenl]carbamates

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【作者】 刘卫东; 李志伟; 李仲英; 王晓光; 高必达;

【Author】 LIU, Wei-Dong*,a,c LI, Zhi-Weib LI, Zhong-Yingb WANG, Xiao-Guanga GAO, Bi-Dac (a Hunan Research Institute of Chemical Industry, National Pesticide Research and Development Southern Center Hunan Branch, Changsha 410007) (b College of Chemistry and Chemical Engineering, Hunan University, Changsha 410082) (c College of Bio-Safety Science and Technology, Hunan Agricultural University, Changsha 410128)

【机构】 湖南化工研究院国家南方农药创制中心湖南基地; 湖南大学化学化工学院; 湖南农业大学生物安全科技学院 长沙410007湖南农业大学生物安全科技学院长沙410128; 长沙410082; 长沙410007; 长沙410128;

【摘要】 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,1HNMR,LC/MS和元素分析确认.生物活性测定表明,部分化合物在50mg/L下对小麦赤霉病菌(Gibberellazeae)、稻瘟病菌(Pyriculariaoryzae)和黄瓜灰霉病菌(Botrytiscinerea)有较好的抑菌活性.

【Abstract】 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 de-rivatives 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.

【基金】 国家十五科技攻关(No.2004BA308A22);湖南省杰出青年科学基金(No.04JJ1009)资助项目.
  • 【文献出处】 有机化学 ,Chinese Journal of Organic Chemistry , 编辑部邮箱 ,2005年04期
  • 【分类号】TQ450.1
  • 【被引频次】17
  • 【下载频次】190
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