盐酸苯达莫司汀的合成工艺研究  

Study on synthetic process of bendamustine hydrochloride

作　　者：高文磊[1] 马帅[1] 李少华[1] 叶家林[1] 曹胜华[1] 丁小东[2] 

机构地区：[1]四川抗菌素工业研究所,四川成都610052 [2]四川大学分析测试中心,四川成都610064

出　　处：《化学研究与应用》2014年第10期1679-1682,共4页Chemical Research and Application

摘　　要：盐酸苯达莫司汀是用于治疗慢性淋巴细胞性白血病(CLL)及乳腺癌的药物,市场前景广阔[1]。目前的合成方法中存在反应条件苛刻、产率低等缺点。本文以2,4-二硝基氯苯为原料,通过取代、还原、酰化、环合、催化还原、烃基化、成盐等七步反应成功合成盐酸苯达莫司汀,终产率为40.99%。反应条件温和、步骤少,降低了生产成本以及设备要求,有良好的工业化应用前景。Bendamustine hydrochloride,a derivant of nitrogen mustard,is a bioalkylating agengt,essentially used for the treatment of chronic lymphocytic leukemia and lymphomas. The process for its preparation generally suffers from the drawback of a high require of reaction condition. The synthetic process of bendamustine hydrochloride through seven main reactions,such as substitution,reduc-tion,acylation,cyclization,reduction,alkylation,salification reaction etc was reported in this paper. A short synthesis route with mild reaction conditions,less steps,reducing the production cost and equipment requirements,a good prospect of industrialization,was provided.

关 键 词：2  4-二硝基氯苯 盐酸苯达莫司汀 工艺优化 

分 类 号：O626.23[理学—有机化学]