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有机化学
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有机化学 ›› 2006, Vol. 26 ›› Issue (10): 1398-1402. 上一篇    下一篇

研究论文

2-氧代-2-[(2-氯-5-吡啶甲氨基)(芳基)甲基]-4-芳基-5,5-二甲基-1,3,2-二氧膦杂环己烷的合成及其生物活性研究

孙凤梅，石德清*   

  1. (华中师范大学化学学院 农药与化学生物学教育部重点实验室 武汉 430079)
  • 收稿日期:2005-12-20 修回日期:2006-03-20 发布日期:2006-09-19
  • 通讯作者: 石德清

Studies on the Synthesis and Biological Activities of 2-[(2-Chloro- 5-pyridylmethylamino)(aryl)methyl]-4-aryl-5,5-dimethyl-1,3,2-dioxaphosphinane 2-Oxides

SUN Feng-Mei,SHI De-Qing*   

  1. (Key Laboratory of Pesticide and Chemical Biology of Ministry of Education, College of Chemis-try,
    Central China Normal University, Wuhan 430079)
  • Received:2005-12-20 Revised:2006-03-20 Published:2006-09-19
  • Contact: SHI De-Qing

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通过类Mannich 反应“一锅法”合成了10个未见文献报道的含吡啶基的环状α-氨基膦酸酯, 其结构经1H NMR, 31P NMR, IR, MS和元素分析确证. 测定了该系列化合物的杀虫、杀菌和除草活性, 结果表明, 所测化合物的杀虫活性不太好, 但所有化合物在药液浓度为1.0×10－4 g/mL 时都具有较好的除草活性, 部分化合物在5.0×10－5 g/mL时显示出良好的杀菌活性.

关键词: 2-氯-5-吡啶甲胺, 合成, 生物活性, α-氨基膦酸酯

Ten novel cyclic α-aminophosphonates containing pyridine moiety were synthesized by “one pot” Mannich-type reaction. Their structures were confirmed by 1H NMR, 31P NMR, IR, MS spectra and elemental analysis. The preliminary biological activity tests show that all of the compounds have weak insecticidal activity but they have very good herbicidal activity at the concentration of 1.0×10－4 g/mL, and some of the target compounds possess good fungicidal activity at the concentration of 5.0×10－5 g/mL .

Key words: 2-chloro-5-pyridylmethylamine, synthesis, biological activity, α-amino phosphonate