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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.
Department of Organic Chemistry, School of pharmacy, Second Military Medical University, Shanghai200433, China
2.
Guilin Eight plus one Pharmaceutical Co., Ltd., Gui Lin 541004, China
Received Date: 2011-01-05
Rev Recd Date:
2011-05-09
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.
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.
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.
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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