抗肿瘤药物仑伐替尼合成研究进展  

Progress on Synthesis of Anti-tumour Lenvatinib

作　　者：王庆洋 李明[2] 谭绍英 黄军海[2] 马杰[1] WANG Qing-yang;LI Ming;TAN Shao-ying;HUANG Jun-hai;MA Jie(University of Shanghai for Science and Technology,Shanghai 200093,China;Shanghai Pharmaceutical Industry Research Institute,State Key Laboratory of Innovative Drugs and Pharmaceutical Technology,Shanghai 201203,China)

机构地区：[1]上海理工大学,上海200093 [2]上海医药工业研究院,创新药物与制药工艺国家重点实验室,上海201203

出　　处：《广州化学》2020年第3期42-46,共5页Guangzhou Chemistry

基　　金：上海市优秀技术带头人计划(17XD1423000);上海市自然科学基金(17ZR1429300)。

摘　　要：综述了仑伐替尼及其相关主要中间体的合成方法。首先对仑伐替尼逆合成分析,并着重讨论了喹啉环(原料1)以及终产物仑伐替尼的合成。原料1有四种合成方法,对这四种合成方法进行了详细对比与分析,指出第二种合成方法为最佳合成方法。总结了仑伐替尼最常用的两条合成路线并分析优缺点,第一条路线是汇聚式路线,反应时间短、能耗少、成本低、收率高,相比第二条路线更加适合工业化生产。This paper reviewed about the various preparation methods of anticancer drug Lenvatinib and its key intermediates.The retrosynthesis of Lenvatinib was analyzed firstly,and then the synthesis of quinoline ring(start material 1)and the final product lenvastinib was emphatically discussed.Meanwhile,several characteristics and advantages in these synthetic routes of quinoline ring were summarized and the second route is best one.Two synthetic routes commonly used for final product lenvastinib were summarized and their advantages and disadvantages were illustrated.The first route was the convergation-type route,with short time-consuming,low energy consumption,high yield and low cost,which was more suitable for industrial level production than the second route.

关 键 词：抗癌药 仑伐替尼 合成工艺 

分 类 号：A150.2040[哲学宗教—马克思主义哲学]