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羟乙膦酸二钠同类物的合成

SYNTHESIS OF DISODIUM ETIDRONATE ANALOGOUS

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【作者】 丁文玉; 刘芳;

【Author】 Ding Wenyu and Liu Fang (Department of Organic Chemistry)

【机构】 中国药科大学有机化学教研室; 中国药科大学有机化学教研室 本校1987届毕业生;

【摘要】 <正> Etidronate disodium学名为1-羟基乙叉二膦酸二钠,系美国孟山都(Monsanto)化学公司研制成功的变形性骨炎治疗药,其结构式如下:

【Abstract】 In order to search for better drugs with less side effects and faster absorp tion rate for the treatment of Paget’s diseases (osteitis deformans) and heterotropic ossification, two compounds of Etidronate disodium, [Disodium dihydrogen (1-hydroxypentylidene-1, 1-diphosphonate)] (Ⅰ)and [Disodium dihydrogen (1-hydroxyhexylidine-1, 1-diphosphonate)] (Ⅱ) were synthesized from n-pentoic acid and n-hexenoic acid respectively by condensation with PCl2, hydrolysis and neutralization with sodium hydroxide to pH 5. The sodium salt of corresponding alkyl diphosphonate (Ⅰ or Ⅱ) was obtained in the total yield of 42% (Ⅰ) and 63% (Ⅱ). (Ⅰ) and (Ⅱ) were characterized by infrared spectrum and elementary analysis, 1H-NMR spectrum, Mass spectrum and Differential thermalanalysis.

  • 【文献出处】 中国药科大学学报 ,Journal of China Pharmaceutical University , 编辑部邮箱 ,1988年01期
  • 【被引频次】1
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