盐酸苯达莫司汀合成工艺的改进
Optimization of synthetic process of bendamustin
-
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.
-
Key words:
- bendamustin /
- antitumor /
- synthesis
-
[1] 陈 栋,宫 平.盐酸苯达莫司汀[J].中国药物化学杂志,2009,19(2):159. [2] Bremer K,Roth W.Bendamustine,a low toxic nitrogen mustard derivative with high efficiency in malignant lymphomas[J].Tumordiagn Ther,1996,17(1):1. [3] 高丽梅,汪燕翔,宋丹青.盐酸苯达莫司汀的合成[J].中国新药杂志,2007,16(23):1960. [4] 戴延凤,张胜菊,付 敏,等.盐酸苯达莫司汀的合成[J].化学试剂.2010,32(8):753. [5] Von WO,Krebs D.ω-,[Bis-(β-chlorathyl)-amino-benzimidazolyl-(2)]-propion-bzw.-buttersiiuren als potentielle Cytosatatika[J].J Fur Praktische Che-mic,1963,20(4):178. [6] Teichert J,Sohr R,Baumann F.Synthesis and charac-terization of some new phase II metabolites of the al-kylator bendamustine and their identification in human bile,urine,and plasma from patients with cholagio-carcinoma[J].Drug Metab Dispos,2005,33(7):984. -
点击查看大图
计量
- 文章访问数: 3329
- HTML全文浏览量: 165
- PDF下载量: 320
- 被引次数: 0
下载:
