| 卡托普利合成工艺改进及有关物质合成 |
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| 引用本文： | 孙忠华,叶欣,王吉,胡小丽,陈益林,宦玉亮,朱怡君.卡托普利合成工艺改进及有关物质合成[J].合成化学,2020,28(4):314-318. |
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| 作者姓名： | 孙忠华 叶欣 王吉 胡小丽 陈益林 宦玉亮 朱怡君 |
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| 作者单位： | 上药集团 常州制药厂有限公司，江苏 常州 213018 |
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| 基金项目： | 江苏省博士后基金资助项目;2018年度江苏省"双创人才"计划 |
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| 摘 要： | 以(2S)-1-(3-巯基-2-甲基-1-氧代丙基)-L-脯氨酸为起始物料,经水解、盐析、精制合成了卡托普利,总收率85%,纯度99.72%,单杂小于0.1%。基于该工艺合成了卡托普利的5种杂质,纯度均大于95.0%,结构经1H NMR,13C NMR和HR-MS(ESI)确证。
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| 关 键 词： | 卡托普利 水解 工艺改进 杂质合成 脯氨酸 |
| 收稿时间： | 2019-10-23 |
Process Improvement of Captopril and Synthesis of Its Impurities |
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| SUN Zhong-hua,YE Xin,WANG Ji,HU Xiao-li,CHEN Yi-lin,HUAN Yu-liang,ZHU Yi-jun.Process Improvement of Captopril and Synthesis of Its Impurities[J].Chinese Journal of Synthetic Chemistry,2020,28(4):314-318. |
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| Authors: | SUN Zhong-hua YE Xin WANG Ji HU Xiao-li CHEN Yi-lin HUAN Yu-liang ZHU Yi-jun |
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| Institution: | Changzhou Pharmaceutical Factory Co., Ltd., Shanghai Pharma, Changzhou 213000, China |
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| Abstract: | Captopril was synthesized by hydrolysis of(2S)-1-(3-acetylthio-2-methyl-1-oxopropyl)-L-proline with diluted hydrochloric acid,the yield was 85%,and the purity of Captopril was 99.62%,while all the impurities were below 0.1%.Five related impurities were synthesized based on this process,and the structures were confirmed by 1H NMR,13C NMR and HR-MS(ESI). |
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| Keywords: | Captopril acid hydrolysis process improvement impurity synthesis proline |
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