米诺膦酸二钠合成工艺的改进  

An improved synthesis of disodium minodronate

作　　者：程进波[1] 赵世明[2] 罗振福[2] 孙有光[1] 

机构地区：[1]天津理工大学化学化工学院,天津300384 [2]天津药物研究院化学制药部,天津300193

出　　处：《华西药学杂志》2012年第6期615-617,共3页West China Journal of Pharmaceutical Sciences

摘　　要：目的改进米诺膦酸的制备方法。方法以(S)-3-羟基-1,4-丁内酯为原料,经过水解开环、氧化、缩合、水解、与三氯化磷和水反应后再成盐,制备米诺膦酸二钠。结果和结论反应总收率为22.6%,反应条件温和,操作易控,分离纯化简单,产品收率高,可用于工业放大生产。OBJECTIVE To improve the synthetic method of disodium minodro-nate.METHODS Disodium minodronateis was synthesized from（S）-3-hydroxyl 1,4-butyrrolactone by ring-opening,oxidation,condensation,hydrolysis and then reacting with PCl3 followed by salification.RESULTS and CONCLUSION The total yield was 22.6%.The method has the advantages of mild condition,easily controlled operation,simple isolation and fine yield rate,which can be applied to the future scale-up production.

关 键 词：米诺膦酸二钠 骨质疏松 高钙血症 合成 

分 类 号：R914[医药卫生—药物化学]