| 盐酸苯达莫司汀合成工艺的改进 |
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| 引用本文： | 蔡瞻,姜志辉,赵明珠,张大志,臧成旭,黄景华.盐酸苯达莫司汀合成工艺的改进[J].药学实践杂志,2011,29(6):453-454. |
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| 作者姓名： | 蔡瞻 姜志辉 赵明珠 张大志 臧成旭 黄景华 |
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| 作者单位： | 1. 第二军医大学药学院有机教研室,上海,200433
2. 桂林八加一药物研究股份有限公司,广西桂林,541004 |
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| 摘 要： | 目的改进盐酸苯达莫司汀的合成工艺,以提高产品纯度。方法以1-甲基-2-(4’-丁酸乙酯基)-5-硝基]-1H-苯并咪唑为起始原料,经氢化还原、取代、水解和成盐等反应制得盐酸苯达莫司汀。结果优化后的制备工艺成本低,操作简便,可获得高纯度的盐酸苯达莫司汀。结论新工艺产率达到62%,适合工业生产。
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| 关 键 词： | 盐酸苯达莫司汀 抗肿瘤 合成 |
| 收稿时间： | 1/5/2011 12:00:00 AM |
| 修稿时间： | 5/9/2011 12:00:00 AM |
Optimization of synthetic process of bendamustin |
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| CAI Zhan,JIANG Zhi-hui,ZHAO Ming-zhu,ZHANG Da-zhi,ZANG Cheng-xu and HUANG Jing-hua.Optimization of synthetic process of bendamustin[J].The Journal of Pharmaceutical Practice,2011,29(6):453-454. |
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| Authors: | CAI Zhan JIANG Zhi-hui ZHAO Ming-zhu ZHANG Da-zhi ZANG Cheng-xu and HUANG Jing-hua |
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| Institution: | Department of Organic Chemistry, School of pharmacy, Second Military Medical University, Shanghai200433, China;Department of Organic Chemistry, School of pharmacy, Second Military Medical University, Shanghai200433, China;Department of Organic Chemistry, School of pharmacy, Second Military Medical University, Shanghai200433, China;Department of Organic Chemistry, School of pharmacy, Second Military Medical University, Shanghai200433, China;Guilin Eight plus one Pharmaceutical Co., Ltd., Gui Lin 541004, China;Guilin Eight plus one Pharmaceutical Co., Ltd., Gui Lin 541004, China |
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| Abstract: | Objective To optimize the synthetic process of bendamustin for high purity. Methods Bendamustin was prepared from 1-Methyl-5-amino-1H-benzimidazole-2-butanoic acid ethyl ester by reduction,substitution,hydrolization and salification,successively. Results A good process for preparation of bendamustin was successfully achieved with low cost, easy operation and high purity. Conclusion The overall yield of the new process was 62%, which was more suitable for industrial production. |
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| Keywords: | bendamustin antitumor synthesis |
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