| 脱氟阿托伐他汀钙的全合成 |
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| 引用本文： | 薛雨,罗刚,王瑛瑛,窦瑶,徐寅正,陈宇瑛. 脱氟阿托伐他汀钙的全合成[J]. 中国新药杂志, 2011, 0(15) |
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| 作者姓名： | 薛雨 罗刚 王瑛瑛 窦瑶 徐寅正 陈宇瑛 |
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| 作者单位： | 中国医药集团总公司四川抗菌素工业研究所; |
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| 基金项目： | 国家科技支撑计划项目(2008BAI55B01) |
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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。
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| 关 键 词： | 脱氟阿托伐他汀 Michael-Stetter反应 Paal-Knorr反应 合成 |
Total synthesis of desfluoro atorvastatin calcium |
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| XUE Yu,LUO Gang,WANG Ying-ying,DOU Yao,XU Yin-zheng,CHEN Yu-ying. Total synthesis of desfluoro atorvastatin calcium[J]. Chinese Journal of New Drugs, 2011, 0(15) |
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| Authors: | XUE Yu LUO Gang WANG Ying-ying DOU Yao XU Yin-zheng CHEN Yu-ying |
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| Affiliation: | XUE Yu,LUO Gang,WANG Ying-ying,DOU Yao,XU Yin-zheng,CHEN Yu-ying(Sinopharm Sichuan Industrial Institute of Antibiotics,Chengdu 610052,China) |
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| Abstract: | Objective: To totally synthesize desfluoro atorvastatin calcium,and to provide important evidence 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 1H-NMR and ESI-MS.Conclusion: The target compounds were obtained by this method,which provides an important reference... |
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| Keywords: | desfluoro atorvastatin Michael-Stetter reaction Paal-Knorr reaction synthesis |
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