| 盐酸普拉格雷合成工艺的改进 |
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| 引用本文： | 代黎,姜志辉,蔡瞻,赵明珠,李宴,倪廷峻弘,田淑娟,张大志.盐酸普拉格雷合成工艺的改进[J].药学实践杂志,2013,31(3):195-197. |
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| 作者姓名： | 代黎 姜志辉 蔡瞻 赵明珠 李宴 倪廷峻弘 田淑娟 张大志 |
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| 作者单位： | 第二军医大学药学院有机化学教研室,上海,200433 |
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| 摘 要： | 目的 改进盐酸普拉格雷的合成工艺,以便于放大生产,提高产品纯度.方法 以邻氟苯乙酸和环丙烷甲酸甲酯为原料合成环丙基-2-氟苄基酮,再用NBS溴代得到α-环丙基羰基-2-氟苄基溴,在碱存在下,与2-氧代-2,4,5,6,7,7a-六氢噻吩并3,2-c]吡啶盐酸盐发生亲核取代反应,再经乙酰化和成盐反应制得盐酸普拉格雷.结果 优化后的合成工艺操作简便,成本低廉,可获得高纯度的盐酸普拉格雷.结论 新工艺总产率达到48％,有利于工业生产.
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| 关 键 词： | 盐酸普拉格雷 抗血栓药 药物合成 |
| 收稿时间： | 2012/8/30 0:00:00 |
| 修稿时间： | 2013/4/25 0:00:00 |
Optimization of synthetic process of prasugrel hydrochloride |
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| DAI Li,JIANG Zhi-hui,CAI Zhan,ZHAO Ming-zhu,LI Yan,NI Ting-jun-hong,TIAN Shu-juan and Zhang Da-zhi.Optimization of synthetic process of prasugrel hydrochloride[J].The Journal of Pharmaceutical Practice,2013,31(3):195-197. |
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| Authors: | DAI Li JIANG Zhi-hui CAI Zhan ZHAO Ming-zhu LI Yan NI Ting-jun-hong TIAN Shu-juan and Zhang Da-zhi |
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| Institution: | Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China,Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China,Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China,Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China,Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China,Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China,Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China and Department of Organic Chemistry, School of Pharmacy, Second Military Medical University, Shanghai 200433, China |
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| Abstract: | |
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| Keywords: | Prasugrel hydrochloride antithrombotic drug drug synthesis |
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