盐酸苯达莫司汀的合成  

Synthesis of bendamustine

作　　者：高丽梅[1] 汪燕翔[1] 宋丹青[1] 

机构地区：[1]中国医学科学院中国协和医科大学医药生物技术研究所,北京100050

出　　处：《中国新药杂志》2007年第23期1960-1961,1970,共3页Chinese Journal of New Drugs

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、水解、成盐等9步反应制得目标化合物。结果:目标化合物的质谱、核磁共振氢谱、红外光谱均与文献报道相吻合,总收率为33.5%。结论:本路线操作简单,成本较低,适合工业化生产。Objective： To synthesize bendamustine. Methods： The target compound was synthesized from 2,4-dinitro-chlorobenzen as a starting material via nine steps including substitution, reduction, acylation, cyclization, reduction, substitution, hydrolization and salification. Results： The structure of the target compound was confirmed by MS, ^1H-NMR, 33.5%. Conclusion ： This cost-saving and simplified IR analysis. The total yield of bendamustine was method can be used in the industrial manufacture.

关 键 词：盐酸苯达莫司汀 抗肿瘤 药物合成 

分 类 号：R979.1[医药卫生—药品] R73[医药卫生—药学]