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瑞舒伐他汀钙合成新方法

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以([4-(4-氟苯基)-6-异丙基-2-[N-甲基-N-甲磺酰胺基)-5-嘧啶基]三苯基溴化膦为原料,经过缩合、水解、成钙盐等反应,合成瑞舒伐他汀钙。本文对合成过程进行了系统的研究,此方法避免了水解过程中消旋反应的发生,提高了目标产物的纯度和瑞舒伐他汀钙原料药的质量。新开发的合成工艺使瑞舒伐他汀钙盐的总收率达到80%以上,纯度达到99。5%以上,非对映异构体及其他单杂含量小于0。1%。
A new synthesis method for rosuvastatin calcium
Employing({ 4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl} methyl)(triphenyl)phosphonium bromide as raw material,via the reaction of condensation,hydrolysis and calcification,the rosuvastatin calcium salt was.The synthesis process was systematically studied in this paper,avoiding occurring racemization reaction in the hydrolysis path-way,which could increase the purity of the targeted product and the quantity of API of rosuvastatin calcium salt.This new developed protocol resulted in the over 80%total yield and 99.5%purity for rosuvastatin calcium salt,and the percentage of the diastereoiso-mers and other impurities were less than 0.1%.

rosuvastatin calciumpurificationhigh purity

傅收、石艳彩、贾玉香、尹亚军、鞠志宇

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河南豫辰药业股份有限公司,河南 许昌 461000

许昌学院化工与材料学院,河南 许昌 461000

瑞舒伐他汀钙 纯化 高纯度

2025

化学研究与应用
四川省化学化工学会 四川大学

化学研究与应用

北大核心
影响因子:0.555
ISSN:1004-1656
年,卷(期):2025.37(1)