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CAI Zhan, JIANG Zhi-hui, ZHAO Ming-zhu, ZHANG Da-zhi, ZANG Cheng-xu, HUANG Jing-hua. Optimization of synthetic process of bendamustin[J]. Journal of Pharmaceutical Practice and Service, 2011, 29(6): 453-454.
Citation: CAI Zhan, JIANG Zhi-hui, ZHAO Ming-zhu, ZHANG Da-zhi, ZANG Cheng-xu, HUANG Jing-hua. Optimization of synthetic process of bendamustin[J]. Journal of Pharmaceutical Practice and Service, 2011, 29(6): 453-454.

Optimization of synthetic process of bendamustin

  • Received Date: 2011-01-05
  • Rev Recd Date: 2011-05-09
  • 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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    [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.
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Optimization of synthetic process of bendamustin

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.

CAI Zhan, JIANG Zhi-hui, ZHAO Ming-zhu, ZHANG Da-zhi, ZANG Cheng-xu, HUANG Jing-hua. Optimization of synthetic process of bendamustin[J]. Journal of Pharmaceutical Practice and Service, 2011, 29(6): 453-454.
Citation: CAI Zhan, JIANG Zhi-hui, ZHAO Ming-zhu, ZHANG Da-zhi, ZANG Cheng-xu, HUANG Jing-hua. Optimization of synthetic process of bendamustin[J]. Journal of Pharmaceutical Practice and Service, 2011, 29(6): 453-454.
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