他米巴罗汀合成路线图解  

Graphical Synthetic Routes of Tamibarotene

作　　者：张宗磊 郭亚芸 段崇刚 张宁 ZHANG Zong-lei;GUO Ya-yun;DUAN Chong-gan;ZHANG Ning(Key Lab for Chemical Drug Research of Shandong Province,Shandong Academy of Pharmaceutical Science,Jinan 250101,China;Shandong Academy of Grape,Jinan 250100,China)

机构地区：[1]山东省药学科学院,山东省化学药物重点实验室,山东济南250101 [2]山东省葡萄研究院,山东济南250100

出　　处：《精细化工中间体》2019年第5期6-9,14,共5页Fine Chemical Intermediates

摘　　要：综述了他米巴罗汀(1)的合成工艺,并针对其不同的合成路线进行了分析和研究,提出了适合工业化生产的路线。以溴苯(7)和2,5-二氯-2,5-二甲基己烷(4)为起始原料,经傅克烷基化、Ullmann-type偶联、与4-氯苯甲酰基苯甲酸甲酯缩合、水解得到目标化合物1。该合成路线反应条件温和,操作简单,收率高,成本低,适合工业化生产。This paper reviewed the existing synthesis methods of Tamibarotene(1),and through research and analysis on different synthetic processes,a route suitable for industrial production was proposed.The target compound 1 was syhthesized by a three-step reaction of Friedel-Crafts,Ullmann-type coupling,with methyl 4-chloroca-rbonylbenzonate and hydrolysis from bromobenzene(7)and 2,5-dichloro-2,5-dimethylhexane(1).This route is simple and easy to operate,has low cost and high yield,and is suitable for industrial production.

关 键 词：他米巴罗汀 急性早幼粒细胞白血病 合成路线图解 

分 类 号：TQ46[化学工程—制药化工]