![一种抗肿瘤药物的合成方法](/CN/2015/1/47/images/201510236812.jpg)
基本信息:
- 专利标题: 一种抗肿瘤药物的合成方法
- 专利标题(英):Synthetic method of anti-tumor medicine
- 申请号:CN201510236812.0 申请日:2015-05-11
- 公开(公告)号:CN104817541A 公开(公告)日:2015-08-05
- 发明人: 吉民 , 李元 , 刘海东 , 李锐 , 蔡进 , 胡海燕
- 申请人: 苏州东南药业股份有限公司
- 申请人地址: 江苏省苏州市工业园区仁爱路150号独墅湖高教区第二教学楼C316室
- 专利权人: 苏州东南药业股份有限公司
- 当前专利权人: 苏州东南药业股份有限公司
- 当前专利权人地址: 江苏省苏州市工业园区仁爱路150号独墅湖高教区第二教学楼C316室
- 代理机构: 南京知识律师事务所
- 代理人: 张铂
- 主分类号: C07D403/04
- IPC分类号: C07D403/04 ; C07C271/28 ; C07C269/04 ; C07C269/06 ; C07C233/44 ; C07C231/12 ; A61P35/00
The invention relates to a synthetic method of an anti-tumor medicine, namely N-[2-[[2-(dimethylamino) ethyl] methyl amino]-4-methoxy-5-[[4-(1-methyl-1H-indole-3-yl)-2-pyrimidyl] amino] phenyl]-2-acrylamide (AZD9291) and a key intermediate of the anti-tumor medicine. The synthetic method comprises the following steps: performing Boc acid anhydride protection on 4-fluoro-2-methoxy-5-nitroaniline to obtain 4-fluoro-2-methoxy-5-nitroanilino tert-butyl formate, then reacting with N,N,N'-trimethylethylenediamine to obtain 4-(N,N,N'-trimethylethylenediamino)-2-methoxy-5-nitroanilino tert-butyl formate, then reducing to obtain 2-(N,N,N'-trimethylethylenediamino)-4-methoxy-5-tert-butyl carbamate phenylamine, then completely reacting with acryloyl chloride and directly removing a Boc protecting group to obtain 2-methoxy-4-N,N,N'-trimethylethylenediamino-5-acrylamido phenylamine, and finally reacting with 3-(2-chloropyrimidine-4-yl)-1-methylindole to obtain AZD9291. A process disclosed by the invention is simple in step, relatively high in yield, mild in reaction condition and easy for realization of industrial production.
公开/授权文献:
- CN104817541B 一种抗肿瘤药物的合成方法 公开/授权日:2017-06-16
IPC结构图谱:
C | 化学;冶金 |
--C07 | 有机化学 |
----C07D | 杂环化合物 |
------C07D403/00 | 杂环化合物,含有两个或更多的杂环,以氮原子作为仅有的杂环原子,C07D401/00组不包含的 |
--------C07D403/02 | .含两个杂环 |
----------C07D403/04 | ..被环原子—环原子的键直接连接的 |