
基本信息:
- 专利标题: 一种制备奈妥吡坦关键中间体N-甲基-4-(2-甲基苯基)-6-(4-甲基-1-哌嗪基)-3-吡啶胺的新方法
- 专利标题(英):New method for preparation of netupitant key intermediate N-methyl-4-(2-methyl phenyl)-6-(4-methyl-1-piperazinyl)-3-pyridylamine
- 申请号:CN201510478969.4 申请日:2015-08-03
- 公开(公告)号:CN105061303A 公开(公告)日:2015-11-18
- 发明人: 张善军 , 关文捷 , 程泷 , 高红
- 申请人: 成都欣捷高新技术开发有限公司
- 申请人地址: 四川省成都市高新区冯家湾工业园科园南路88号B7栋5楼
- 专利权人: 成都欣捷高新技术开发有限公司
- 当前专利权人: 成都欣捷高新技术开发有限公司
- 当前专利权人地址: 四川省成都市高新区冯家湾工业园科园南路88号B7栋5楼
- 代理机构: 成都九鼎天元知识产权代理有限公司
- 代理人: 徐宏; 吴彦峰
- 主分类号: C07D213/74
- IPC分类号: C07D213/74
Belonging to the field of drug synthesis, the invention relates to a new method for preparation of the netupitant key intermediate N-methyl-4-(2-methyl phenyl)-6-(4-methyl-1-piperazinyl)-3-pyridylamine. The method comprises the steps of: 1) in certain solvent, subjecting 6-(4-methyl-1-piperazinyl)-4-(2-methyl phenyl)nicotinamide (formula I compound) and ROX (X=H or Na) to Hoffman degradation reaction under the condition of iodobenzene diacetate or substituted Iodobenzene diacetate, thus obtaining a formula II compound; and 2) carrying out reduction reaction on the formula II compound to obtain N-methyl-4-(2-methyl phenyl)-6-(4-methyl-1-piperazinyl)-3-pyridylamine (formula III compound). The new method for preparation of the netupitant key intermediate N-methyl-4-(2-methyl phenyl)-6-(4-methyl-1-piperazinyl)-3-pyridylamine has the advantages of easily available production raw materials, mild reaction conditions and simple operation, avoids application of strong base and controlled reagents, and provides an environment-friendly generation process.
IPC结构图谱:
C | 化学;冶金 |
--C07 | 有机化学 |
----C07D | 杂环化合物 |
------C07D213/00 | 杂环化合物,含六元环、不与其他环稠合、有1个氮原子作为仅有的杂环原子、环原子间或环原子与非环原子间有3个或更多个双键 |
--------C07D213/02 | .环原子间或环原子与非环原子间有3个双键 |
----------C07D213/04 | ..在环氮原子与非环原子间没有键或只有氢或碳原子直接连在环氮原子上 |
------------C07D213/06 | ...除了环氮原子外,只含氢和碳原子 |
--------------C07D213/62 | ....氧或硫原子 |
----------------C07D213/74 | .....被烃基或取代烃基所取代的胺基或亚胺基 |