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米诺膦酸二钠合成工艺的改进
An improved synthesis of disodium minodronate
【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。
【Abstract】 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;
【Key words】 Disodium minodronate; Osteoporosis; Hypercalcemia; Synthesis;
【Key words】 Disodium minodronate; Osteoporosis; Hypercalcemia; Synthesis;
- 【文献出处】 华西药学杂志 ,West China Journal of Pharmaceutical Sciences , 编辑部邮箱 ,2012年06期
- 【分类号】TQ463.6
- 【被引频次】1
- 【下载频次】189