盐酸苯达莫司汀的合成工艺研究  

Study on Synthesis Bendamustine Hydrochloride

作　　者：潘英[1] 倪海华[2] 邹爱峰[2] 刘家健[3] 

机构地区：[1]江苏省肿瘤医院,南京210000 [2]扬子江药业集团,泰州2253213 [3]四川抗菌素工业研究所,成都610052

出　　处：《国外医药（抗生素分册）》2015年第4期167-170,共4页World Notes on Antibiotics

摘　　要：目的盐酸苯达莫司汀的合成。方法以5-硝基-1-甲基-2-苯并咪唑丁酸乙酯(BD-a)为起始原料,经还原、取代、氯代、水解成盐制备得目标产物盐酸苯达莫司汀,共三步反应。结果该工艺对文献报道的合成方法中提供的反应条件及终产物的纯化方法等各方面工艺参数作了相当程度的优化更新,终产物粗品的总收率61.5%。结论本研究获得了一种清洁、操作简单、适于工业化,盐酸苯达莫司汀收率较高和纯度高的合成工艺。Objective To study the synthesis of bendamustine hydrochloride. Methods bendamustine hydrochloride was synthesized by using 5-amino-l-methyl-2H-benzimidazole-butanoic acid ethyl ester as starting materials by reduction, substitution, halogenating and etc to obtain the bendamustine hydrochloride. Results The process for the synthesis method reported in the literature to provide reaction conditions, purification of the final product and other aspects of process parameters have been updated by a considerable optimization with a molar yield of 64.2%. Conclusion This study is suitable for industrialization, and was able to obtain a higher yield of bendamustine hydrochloride.

关 键 词：盐酸苯达莫司汀 合成 慢性淋巴细胞性白血病 

分 类 号：R979.1[医药卫生—药品]