| 发明名称 |
Methods for the preparation of 5-[2-[7 (trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo [1,5-A]pyrimidin-3-yl[ethynyl]-2-pyridinamine |
| 摘要 |
The present invention provides methods for preparing 5-[2-[7-(trifluoromethyl)-5-[4-(trifluoromethyl)phenyl]pyrazolo[1,5-a]pyrimidin-3-yl]ethynyl]-2-pyridinamine (compound A), which is useful for the treatment of depression and other CNS disorders. The present methods are useful for preparing compound A on large scale in manufacturing facilities.; |
| 申请公布号 |
US9447099(B2) |
申请公布日期 |
2016.09.20 |
| 申请号 |
US201213628069 |
申请日期 |
2012.09.27 |
| 申请人 |
Hoffmann-La Roche Inc. |
发明人 |
Bachmann Stephan;Bailey Daniel;Brice Jodie;Cedilote Miall;Dong Zhiming;Hildbrand Stefan;Miller Doreen;Spurr Paul;Srivastava Amit;Wichmann Juergen;Woltering Thomas;Yang Jason;Zhang Pingsheng |
| 分类号 |
C07D213/73;C07D487/04 |
主分类号 |
C07D213/73 |
| 代理机构 |
|
代理人 |
Kale Tamara A. |
| 主权项 |
1. A method for preparing compound 9 having the formula:which comprises:
(a) reacting compound 8; with 2-methyl-3-butyn-2-ol via a Sonogashira coupling reaction in an inert solvent to provide compound 13; and b) deprotecting compound 13 with a base in an inert solvent to provide compound 9. |
| 地址 |
Little Falls NJ US |
