发明专利
CA3024603A1 PROCESS FOR THE PREPARATION OF (S)-N-(5-((R)-2-(2,5-DIFLUOROPHENYL)PYRROLIDIN-1-YL)-PYRAZOLO[1,5-A]PYRIMIDIN-3-YL)-3-HYDROXYPYRROLIDINE-1-CARBOXAMIDE AND SALTS THEREOF
未知
基本信息:
- 专利标题: PROCESS FOR THE PREPARATION OF (S)-N-(5-((R)-2-(2,5-DIFLUOROPHENYL)PYRROLIDIN-1-YL)-PYRAZOLO[1,5-A]PYRIMIDIN-3-YL)-3-HYDROXYPYRROLIDINE-1-CARBOXAMIDE AND SALTS THEREOF
- 申请号:CA3024603 申请日:2017-05-18
- 公开(公告)号:CA3024603A1 公开(公告)日:2017-11-23
- 发明人: EARY CHARLES TODD , REYNOLDS MARK , SPENCER STACEY , JUENGST DERRICK , HACHE BRUNO , JIANG YUTONG , HAAS JULIA , ANDREWS STEVEN W , REYNOLDS MARK , SPENCER STACEY , JUENGST DERRICK , HACHE BRUNO , JIANG YUTONG , HAAS JULIA , ANDREWS STEVEN W
- 申请人: EARY CHARLES TODD , REYNOLDS MARK , SPENCER STACEY , JUENGST DERRICK , HACHE BRUNO , JIANG YUTONG , HAAS JULIA , ANDREWS STEVEN W
- 专利权人: EARY CHARLES TODD,REYNOLDS MARK,SPENCER STACEY,JUENGST DERRICK,HACHE BRUNO,JIANG YUTONG,HAAS JULIA,ANDREWS STEVEN W
- 当前专利权人: EARY CHARLES TODD,REYNOLDS MARK,SPENCER STACEY,JUENGST DERRICK,HACHE BRUNO,JIANG YUTONG,HAAS JULIA,ANDREWS STEVEN W
- 优先权: US201662338359 2016-05-18
- 主分类号: C07D487/04
- IPC分类号: C07D487/04 ; A61K31/5025 ; A61P35/00
摘要:
Process for preparing (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-l- yl)pyrazolo[l,5-a] pyrimidin-3-yl)-3-hydroxypyrrolidine-l-carboxamide (formula I) or a salt thereof by reacting phenyl(5-((R)-2-(2,5- difluorophenyl)pyrrolidin-l-yl)-3,3a-dihydropyrazolo[l,5-a]pyrimidin-3- yl)carbamate or a similar derivative (formula 13) with (S)-pyrrolidin-3- ol (formula 14). Process for preparing phenyl(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-l- yl)-3,3a-dihydropyrazolo[l,5-a]pyrimidin-3-yl)carbamate (formula 13) or a similar derivative by reduction of (R)-5-(2-(2,5-difluorophenyl) pyrrolidin-l-yl)-3-nitropyrazolo[l,5-a]pyrimidine (formula 11) to (R) -5-(2-(2,5-difluorophenyl)pyrrolidin-l-yl)pyrazolo[l,5-a]pyrimidin-3- amine (formula 12). Process for preparing (R)-2-(2,5-difluorophenyl)pyrrolidine(R) -2-hydroxysuccinate (formula 10) by treating (R)-N-((R)-l-(2,5- difluorophenyl)-3-(l,3-dioxan-2-yl)propyl)-2-methylpropane-2- sulfinamide (formula 19) with an acid and a reducing agent. (S)-N-(5-((R)-2-(2,5-difluorophenyl)-pyrrolidin-l-yl)-pyrazolo[l,5- a]pyrimidin-3-yl)-3-hydroxypyrrolidine-l-carboxamide, is a tyrosin kinase (TRK) inhibitor for trearing e.g. cancer.
信息查询:
EspacenetIPC结构图谱:
C | 化学;冶金 |
--C07 | 有机化学 |
----C07D | 杂环化合物 |
------C07D487/00 | 在稠环系中含有氮原子作为仅有的杂环原子的杂环化合物,不包含在C07D451/00至C07D477/00组中 |
--------C07D487/02 | .在稠合系中含有两个杂环 |
----------C07D487/04 | ..邻位稠合系 |