芬戈莫德的合成  

Synthesis of fingolimod

作　　者：刘剑峰[1] 苏鹏[1] 韩建奎[1] 侯桂华[2] 徐文方[3] 李月凯[1] 

机构地区：[1]山东大学齐鲁医院,山东济南250012 [2]山东大学医学院,山东济南250012 [3]山东大学药学院,山东济南250012

出　　处：《药学研究》2014年第12期739-741,共3页Journal of Pharmaceutical Research

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。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 by 1 H-NMR and MS. The overall yield of the process was 26. 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 opera-tion,low cost and.

关 键 词：2-苯乙醇 溴化钠 芬戈莫德 免疫抑制剂 

分 类 号：TQ460.31[化学工程—制药化工]