左磷右胺盐制备磷霉素钠工艺的优化研究  

Optimization on Synthesis Technology of Fosfomycin Sodium by Phosphonomycin(R)-1-phenethylamine Salt

作　　者：黄晨[1] 丁一刚[1] 杜治平[1] 黄丽明[1] 王超[1] 沈琼璐[1] 孟庆岭[1] 

机构地区：[1]武汉工程大学绿色化工过程省部共建教育部重点实验室湖北省新型反应器与绿色化学工艺重点实验室,湖北武汉430073

出　　处：《化学与生物工程》2013年第1期32-35,共4页Chemistry & Bioengineering

基　　金：国家自然科学基金重点资助项目(20936003);湖北省自然科学基金重点资助项目(2008CDA009);湖北省教育厅科学技术研究项目(Q20101511);武汉工程大学研究生创新基金项目(CX201108)

摘　　要：以左旋磷霉素右旋苯乙胺盐为原料与氢氧化钠反应制备磷霉素钠(FS),考察了反应温度、投料时间、保温时间、氢氧化钠浓度、原料配比等因素对磷霉素钠收率的影响,并优化了磷霉素钠的析晶条件。确定适宜的合成工艺条件为:反应温度37～38℃、投料时间20min、保温时间60min、氢氧化钠浓度5mol.L-1、左磷右胺盐与氢氧化钠摩尔比1∶1.7,在此条件下,磷霉素钠的收率达85.4%。用无水乙醇在60℃、磷霉素钠投料量与乙醇用量比为1∶4(mol∶L)的条件下可析出晶型良好的磷霉素钠结晶粉末。With phosphonomycin （R）-1-phenethylamine salt as raw material, fosfomycin sodium （FS） was prepared by reaction witl-r sodium hydroxide. The effects of various factors such as reaction temperature, feeding time,warm-keeping time, concentration of sodium hydroxide and reactant ratio on FS yield were investigated and the crystallization conditions for FS were optimized. The FS yield reached 85.4% under the optimum syn- thetic conditions as follows=the reaction temperature of 37-38℃ ,the feeding time of 20 min,the warm-keep- ing time of 60 min,the concentration of sodium hydroxide of 5 mol · L^-1 ,the molar ratio of phosphonomycin （R）-l-phenethylamine salt to sodium hydroxide was 1 ： 1.7. Moreover,the FS crystal powder with good crystal type could be obtained by crystallation using anhydrous ethanol at 60 ℃ with the amount ratio of FS to ethanol of 1 ： 4（mol· L）.

关 键 词：磷霉素钠 合成 工艺优化 

分 类 号：TQ463[化学工程—制药化工]