发明名称 |
PROCESSES AND INTERMEDIATES FOR MAKING A JAK INHIBITOR |
摘要 |
This invention relates to processes and intermediates for making {1-{1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl}-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl}acetonitrile, useful in the treatment of diseases related to the activity of Janus kinases (JAK) including inflammatory disorders, autoimmune disorders, cancer, and other diseases. |
申请公布号 |
US2016347734(A1) |
申请公布日期 |
2016.12.01 |
申请号 |
US201514976583 |
申请日期 |
2015.12.21 |
申请人 |
Incyte Corporation ;Incyte Holdings Corporation |
发明人 |
Liu Pingli;Wang Dengjin;Wu Yongzhong;Cao Ganfeng;Xia Michael |
分类号 |
C07D401/14;C07F5/02;C07D403/14 |
主分类号 |
C07D401/14 |
代理机构 |
|
代理人 |
|
主权项 |
1. A process, comprising:
reacting a compound of Formula III: with a compound of Formula IV: under Suzuki coupling conditions to form a compound of Formula II: wherein:
Z is H or a protecting group;P1 is a protecting group;X1 is halo; andR1 and R2 are each independently H or C1-6 alkyl; orR1 and R2, together with the two oxygen atoms to which they are attached and the boron atom to which the oxygen atoms are attached, form a 5- to 6-membered heterocycloalkyl ring, which is optionally substituted with 1, 2, 3, or 4 C1-4 alkyl groups. |
地址 |
Wilmington DE US |