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芬戈莫德的合成

Synthesis of fingolimod

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【作者】 刘剑峰苏鹏韩建奎侯桂华徐文方李月凯

【Author】 LIU Jian-feng;SU Peng;HAN Jian-kui;HOU Gui-hua;XU Wen-fang;LI Yue-kai;Qilu Hospital,Shandong University;School of Medicine,Shandong University;School of Parmaceutical Sciences,Shandong University;

【机构】 山东大学齐鲁医院山东大学医学院山东大学药学院

【摘要】 目的改进免疫抑制剂芬戈莫德的合成工艺。方法以2-苯乙醇和溴化钠为起始原料,经取代、酰化、缩合等反应制得芬戈莫德。结果目标化合物的结构经1H-NMR谱和MS确证。总收率为26.9%,比文献收率提高了6.4%。结论改进后的工艺路线方法操作简便、反应条件温和、收率高、成本低,有利于工业化生产。

【Abstract】 Objective To synthesize fingolimod.Methods Fingolimod was synthesized with 2-phenethyl alcohol and sodium bromide as starting material,and through a series of reactions,such as substitution,acylation,condensation etc.Results The struture of target compound was confirmed by1H-NMR and MS.The overall yield of the process was26.9 %.Compared with the reported method,the overall yield was 6.4% higher.Conclusion This synthetic process was convenient,and had high yield,low cost,and mild reaction condition.It was suitable for industrial production by its operation,low cost and.

  • 【文献出处】 药学研究 ,Journal of Pharmaceutical Research , 编辑部邮箱 ,2014年12期
  • 【分类号】TQ463
  • 【被引频次】2
  • 【下载频次】231
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