琥珀酸 S-美托洛尔的合成工艺及其杂质控制研究 |
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引用本文: | 狄潘潘,李家明,徐自奥,刘海亮,李晓祥.琥珀酸 S-美托洛尔的合成工艺及其杂质控制研究[J].安徽医药,2015(3):427-430. |
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作者姓名: | 狄潘潘 李家明 徐自奥 刘海亮 李晓祥 |
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作者单位: | 1. 安徽中医药大学药学院,安徽 合肥,230038;2. 安徽省新星药物开发有限责任公司,安徽 合肥,230088 |
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基金项目: | 安徽中医药大学千人计划培养资助 |
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摘 要: | 目的:通过工艺优化,合成高光学纯度(≥99.7%)的琥珀酸 S-美托洛尔及其关键杂质。方法以对甲氧基乙基苯酚, R-表氯醇和异丙胺为起始原料,通过反应条件的摸索与优化,并经纯化、拆分后,制备出纯度大于99.5%的 S-美托洛尔,同时合成其中2个关键杂质。结果所制备的高光学纯度的琥珀酸 S-美托洛尔及相关杂质,经核磁共振氢谱(NMR),质谱(MS),高效液相色谱(HPLC)确证。结论优化后的工艺收率高,易操作,适合工业化生产。
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关 键 词: | S-美托洛尔 合成 杂质 工艺优化 |
Synthesis technique and control of impurities of (S)-Succinate Metoprolol |
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Institution: | DI Pan-pan;LI Jia-ming;XU Zi-ao;Anhui University of Traditional Chinese Medicine;Anhui New Star Pharmaceutial Development Co. ,Ltd; |
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Abstract: | Objective To optimize the synthetic method for synthesizing high optical purity (≥99.7%)S-succinate metoprolol and two key impurities.Methods With p-(2-methoxyethyl)phenol,R-epichlorohydrin and isopropylamine as starting materials,the prepa-ration of high purity (>99.5%)of S-metoprolol was made after purification and separation.Results S-metoprolol and the related im-purties were confirmed by proton magnetic resonance spectroscopy(NMR),mass spectrum (MS)and high performance liquid chroma-tography (HPLC).Conclusions The yield of optimized process is high,which is easy to operate and suitable for industrial production. |
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Keywords: | S-metoprolol synthesis impurity process optimization |
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