苯丁酸氮芥的合成以及工艺研究  

Study on synthetic process of chlorambucil

作　　者：董宏波[1] 杜伟宏[1] 高文磊[1] 曹胜华[1] 丁小东[2] 

机构地区：[1]成都大学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》2016年第2期267-270,共4页Chemical Research and Application

摘　　要：苯丁酸氮芥(Chlorambucil)是目前临床上最重要的一种一线抗肿瘤药物。近年来以此药物为母核,对其进行结构改造,以期找到活性更好,副作用更小的抗肿瘤药物成为国际上研究的一个热点。但是,通过文献调研我们发现,目前只有少量文献报道此药物的全合成,且已报道的路线存在原料昂贵,工艺复杂,不绿色环保等问题。针对这些问题,本文报道了一条更加简便,环保,适合工业生产的路线,通过五步反应,以总收率19.9%得到了苯丁酸氮芥,对进一步研究此药物的应用提供了帮助。Chlorambucil is the most important antitumor drug in clinic.Nowadays more and more researchers focus their attention onmodifying the structure of Chlorambucilto enhance its antitumor activity and reduce sideeffects. Through our literature researches,however,it found that there were only a few reports about the synthesis of chlorambucil,and the complex interaction,high-cost,andcontinual pollution were the drawbacks of these routes. So a new method which was more convenient,environmentally friendly,and suitable for industrial production by five steps in total yield of 19. 9% wa reporeed.This would be helpful for further research on this drug.

关 键 词：苯丁酸氮芥 合成 工艺 

分 类 号：O623.61[理学—有机化学]