盐酸苯达莫司汀的合成研究  

The study on synthesis of hydrochloride bendamustine

作　　者：宗在伟[1] 杜有国[1] 陈磊[1] 杨建楠[1] 

机构地区：[1]江苏奥赛康药业有限公司,南京210009

出　　处：《海峡药学》2011年第11期227-229,共3页Strait Pharmaceutical Journal

摘　　要：目的合成盐酸苯达莫司汀。方法以2,4-二硝基氯苯为起始原料,经取代、还原、酰化、环合、还原、取代、氯化、成盐等9步反应合成目标化合物。结果合成的目标化合物,其结构经核磁共振氢谱、核磁共振碳谱、质谱及元素分析确证。结论本方法简化了操作步骤,优化了反应条件,降低了成本,提高了收率,适合工业化生产。OBJECTIVE Aim to synthesize bendamustine.METHODS The target compound was synthesized from 2,4-dinitro-chlorobenzen as a starting material via nine steps including substitution,reduction,cyclization,reduction,substitution,chlorination and saponification.RESULTS The structure of the target compoind was confirmed by 1H-NMR,13C-NMR,MS and elemental analysis.CONCLUSION This optimal synthetic procedure with lower cost and higher yield,the process is suitable for industrial producing.

关 键 词：药物化学 工艺改进 化学合成 抗肿瘤 盐酸苯达莫司汀 

分 类 号：R917[医药卫生—药物分析学]