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N-对三氟甲基苯基-α-氨基烷基膦酸酯的合成、晶体结构及生物活性
Synthesis, Structure and Bioactivity of N-(p-Trifluromethyl)phenyl-α-aminophosphonates
【摘要】 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 ,1HNMR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 0 0 0 5 %浓度下对烟草花叶病毒 (TMV)防效达到了 6 7.0 3%.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 =1.195 7(5 )nm ,b =1.0 6 6 4(5 )nm ,c =1.5 943(7)nm ,α =90° ,β =97.6 2 3(8)° ,γ =90° ,V =2 .0 15 0 (15 )nm3 ,Z =4.Dc=1.336Mg/m3 ,μ =0 .189mm-1,F(0 0 0 ) =840 .
【Abstract】 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=4. 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%.
- 【文献出处】 有机化学 ,Chinese Journal of Organic Chemistry , 编辑部邮箱 ,2003年09期
- 【分类号】O627.51
- 【被引频次】42
- 【下载频次】290