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有机化学
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有机化学 ›› 2003, Vol. 23 ›› Issue (9): 967-972. 上一篇    下一篇

研究论文

N-对三氟甲基苯基-α-氨基烷基磷酸酯的合成、晶体结构及生物活性

宋宝安;蒋木庚;吴扬兰;何湘琼;杨松;金林红;刘刚;胡德禹   

  1. 南京农业大学理学院;贵州大学精细化工研究开发中心
  • 发布日期:2003-09-25

Synthesis, Structure and Bioactivity of N-(p-Trifluromethyl)phenyl- α-aminophosphonates

Song Baoan;Jiang Mugeng;Wu Yanglan;He Xiangqiong;Yang Song;Jin Linhong;Liu Gang;Hu Deyu   

  1. College of Sciences, Nanjing Agricultural University;Research and Development Center of Fine Chemicals, Guizhou University
  • Published:2003-09-25

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749

被引次数

14

采用活性基团拼接法将氟原子引入α-氨基烷基膦酸酯中，合成了一系列含氟 芳基α-氨基烷基膦酸酯类新化合物，结构经元素分析，IR，~1H NMR及MS确认。对 所合成的化合物进行了抑制烟草花叶病毒（TMV）田间生物测试，结果表明，该类 化合物具有良好的抑制TMV活性，其中4d化合物在0.0005%浓度下对烟草花叶病毒（ TMV）防效达到了67.03%。就此对4d化合物作了单晶培养，并就晶体结构进行了X衍 射分析。结构表明4d化合物分子属单斜晶系，空间群p2_1/c。晶胞参数a = 1. 1957(5) nm, b = 1.0664(5) nm, c = 1.5943(7) nm, α = 90°,β = 97.623(8) °,γ = 90°,V = 2.0150(15) nm~3, Z = 4. D_c = 1.336 Mg/m~3, μ = 0.189 mm~(-1), F(000) = 840。

关键词: 氨基膦酸 P, 膦酸酯类, 晶体结构, 烟草花叶病毒, 生物活性

A series of N-( p-trifluromethyl) phenyl-α -aminophosphonates were synthesized by the Mannich-type reactions. The structures were established by elemental analysis, ~1H NMR, MS and X-ray diffraction analysis. The crystals of compound 4d are monoclinic, space group P2_1/c, with unit cell dimensions a = 1.1957(5) nm, b = 1.0664(5) nm, c = 1.5943(7) nm, α =90°, β = 97.623(8)°, γ = 90°, V = 2.0150(15) nm~3, Z=A. D_c = 1.336 Mg/m~3, μ = 0.189 mm~(-1), F(000) = 840. The final R = 0.0593, R_w = 0.1690 for 2862 unique reflections. In the tabacoo field test, the new compounds possess a high antiviral activity against TMV. The inhibitivity rate of 4d could reach 67.03 % at the concentration of 0.0005%.

Key words: PHOSPHOAMIDIC ACID P;PHOSPHONIC ACID ESTER;CRYSTAL STRUCTURE, TOBACCO MOSAIC VIRUS;BIOLOGICAL ACTIVITY

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