盐酸苯达莫司汀合成工艺的改进
Optimization of synthetic process of bendamustin
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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。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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Key words:
- bendamustin /
- antitumor /
- synthesis
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