| 盐酸苯达莫司汀合成工艺的改进 |
| |
| 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 |
| |
| 作者姓名： | 蔡瞻 姜志辉 赵明珠 张大志 臧成旭 黄景华 |
| |
| 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 |
| |
| 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。
|
| 关 键 词： | 盐酸苯达莫司汀 抗肿瘤 合成 |
| 收稿时间： | 2011-01-05 |
| 修稿时间： | 2011-05-09 |
Optimization of synthetic process of bendamustin |
| |
| 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 |
| |
| Authors: | CAI Zhan JIANG Zhi-hui ZHAO Ming-zhu ZHANG Da-zhi ZANG Cheng-xu HUANG Jing-hua |
| |
| Affiliation: | 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 |
| |
| 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. |
| |
| Keywords: | bendamustin antitumor synthesis |
| 本文献已被 CNKI 维普 万方数据 等数据库收录！ |
| 点击此处可从《药学实践杂志》浏览原始摘要信息 |
|
点击此处可从《药学实践杂志》下载全文 |
|
