| 盐酸沙格雷酯合成工艺改进 |
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| 引用本文： | 范石虎. 盐酸沙格雷酯合成工艺改进[J]. 中国药物化学杂志, 2013, 23(4): 295-296 |
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| 作者姓名： | 范石虎 |
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| 作者单位： | （安徽科创药物研究所有限责任公司 化学合成部，安徽合肥230088） |
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| 摘 要： | 目的改进盐酸沙格雷酯的合成工艺。方法以2-[2-(3-甲氧基苯基)乙基]苯酚为起始原料,经成醚反应、胺解反应、酯化成盐得盐酸沙格雷酯。结果目标产物的结构经元素分析、IR、1H-NMR谱数据确证,且质量符合日本药典标准。结论改进后的工艺操作简便、产品质量稳定、收率高、成本低,更适合工业化生产。
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| 关 键 词： | 盐酸沙格雷酯 相转移催化 工艺改进 |
| 收稿时间： | 2012-02-29 |
| 修稿时间： | 2013-06-20 |
Improved synthetic technology of sarpogrelate hydrochloride |
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| FAN Shi-hu. Improved synthetic technology of sarpogrelate hydrochloride[J]. Chinese Journal of Medicinal Chemistry, 2013, 23(4): 295-296 |
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| Authors: | FAN Shi-hu |
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| Affiliation: | （Anhui Kechuang Institute For Drugs Co.,Ltd Department of Chemical Synthesis，Hefei 230088,China） |
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| Abstract: | To improve the synthetic technology of sarpogrelate hydrochloride, sarpogrelate hydrochloride was synthesized from a main material 2-[2-(3-methoxyphenyl)ethyl]phenol, which was subjected to alkylation, amination, esterification and salt formation. The structure of final product was confirmed by elemental analysis, IR, 1H-NMR and the qualities of final product measure up JP16. The improved process has high yield, low cost and is easy to operate, while the quality of products is much more stable and suitable for industrial production. |
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| Keywords: | sarpogrelate hydrochloride；phase transfer；process improvement |
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