盐酸苯达莫司汀的合成  

Synthesis of Bendamustine Hydrochloride

作　　者：殷昕[1] 崔美姬 江淼[1] 谌志华[1] 王庆庆[1] 虞心红[1] 

机构地区：[1]华东理工大学药学院,上海200237

出　　处：《合成化学》2016年第5期457-460,共4页Chinese Journal of Synthetic Chemistry

基　　金：国家自然科学基金资助项目(21476078;20972051);上海市科技支撑计划(12431900900;12431900902)

摘　　要：以2,4-二硝基氯苯为起始原料,依次经甲胺化,选择性还原,N-酰化,环合,催化氢化,N-二羟乙基化,O-甲磺酰化,氯置换,酸化水解和成盐等10步反应合成盐酸苯达莫司汀,其结构经~1H NMR确证,总收率48.4%,纯度99.5%。Bendamustine hydrochloride was synthesized by a ten-step reaction of amination,selective reduction,N-acylation,cyclization,catalytic hydrogenation,hydroxyethylation,O-sulfonylation,chlorination,hydrolysis and salification,using 2,4-dinitrochlorobenzen as starting material. The structure was confirmed by^1 H NMR. The total yield and purity were 48. 4% and 99. 5%,respectively.

关 键 词：2 4-二硝基氯苯 苯达莫司汀 药物合成 工艺改进 

分 类 号：O626.15[理学—有机化学] O625.6[理学—化学]