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芬戈莫德的合成
Synthesis of fingolimod
【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.
【Key words】 2-phenethyl alcohol; Sodium bromide; Fingolimod; Immunosuppressant;
- 【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