发明申请
US20120178926A1 METHODS FOR PREPARING PYRIMIDINE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS
失效
用于制备作为蛋白激酶抑制剂有用的吡啶衍生物的方法
- 专利标题: METHODS FOR PREPARING PYRIMIDINE DERIVATIVES USEFUL AS PROTEIN KINASE INHIBITORS
- 专利标题(中): 用于制备作为蛋白激酶抑制剂有用的吡啶衍生物的方法
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申请号: US13424736申请日: 2012-03-20
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公开(公告)号: US20120178926A1公开(公告)日: 2012-07-12
- 发明人: Jean-Damien Charrier , Steven Durrant , David Kay
- 申请人: Jean-Damien Charrier , Steven Durrant , David Kay
- 申请人地址: US MA Cambridge
- 专利权人: VERTEX PHARMACEUTICALS INCORPORATED
- 当前专利权人: VERTEX PHARMACEUTICALS INCORPORATED
- 当前专利权人地址: US MA Cambridge
- 优先权: USPCT/US2010/050132 20100924
- 主分类号: C07D487/14
- IPC分类号: C07D487/14
摘要:
A method of preparing a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and claims, comprises the step of: a) cyclizing a compound represented by Structural Formula A: under suitable reductive cyclisation conditions to form a compound represented by Structural Formula B: wherein R10 is LG1 or —X1R1, and -LG1 is a suitable leaving group; and b) optionally, when R10 of Structural Formula (B) is LG1, further comprising the step of replacing the -LG1 of Structural Formula (B) with —X1R1 to form the compound represented by Structural Formula (I).
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