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脱氟阿托伐他汀钙的全合成 被引量：3

Total synthesis of desfluoro atorvastatin calcium
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摘要 目的:全合成得到脱氟阿托伐他汀钙,为阿托伐他汀产品质量分析及控制提供重要依据。方法:以异丁酰乙酸乙酯为起始原料,通过胺解,缩合,M ichael-Stetter反应,Paal-Knorr反应,得到关键中间体化合物7,再经酸性条件脱保护及碱性条件酯水解成钠盐,最后与醋酸钙成钙盐得到目标化合物脱氟阿托伐他汀钙。结果:目标化合物结构经1H-NMR、ESI-MS确证。结论:通过该法全合成得到了脱氟阿托伐他汀钙,对阿托伐他汀质量指标的控制具有重要参考价值。 Objective： To totally synthesize desfluoro atorvastatin calcium, and to provide important evi- dence for the quality analysis and control of atorvastatin. Methods ： The compound of desfluoro atorvastatin calcium was synthesized by amination, condensation, Michael-Stetter, Paal-Knorrreaction reaction, deprotection from 4- methyl-3-oxo-pentanoic acid ethyl ester. Results： The structures were confirmed by^1 H-NMR and ESI-MS. Conclusion： The target compounds were obtained by this method, which provides an important reference for establishing the quality control indicators of atorvastatin.
作者 薛雨 罗刚 王瑛瑛 窦瑶 徐寅正 陈宇瑛
机构地区 中国医药集团总公司四川抗菌素工业研究所
出处 《中国新药杂志》 CAS CSCD 北大核心 2011年第15期1459-1462,共4页 Chinese Journal of New Drugs
基金 国家科技支撑计划项目(2008BAI55B01)
关键词 脱氟阿托伐他汀 Michael-Stetter反应 Paal-Knorr反应 合成 desfluoro atorvastatin Michael-Stetter reaction Paal-Knorr reaction synthesis
分类号 R972 [医药卫生—药品]
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参考文献14

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二级参考文献55

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中国新药杂志
2011年 第15期

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