发明申请
US20110040090A1 PROCESS FOR THE PREPARATION OF 5-(2-AMINO-PYRIMIDIN-4-YL)-2-ARYL-1H-PYRROLE-3-CARBOXAMIDES
有权
制备5-(2-氨基 - 嘧啶-4-基)-2-芳基-1H-吡咯-3-羧酸的方法
- 专利标题: PROCESS FOR THE PREPARATION OF 5-(2-AMINO-PYRIMIDIN-4-YL)-2-ARYL-1H-PYRROLE-3-CARBOXAMIDES
- 专利标题(中): 制备5-(2-氨基 - 嘧啶-4-基)-2-芳基-1H-吡咯-3-羧酸的方法
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申请号: US12989518申请日: 2009-04-30
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公开(公告)号: US20110040090A1公开(公告)日: 2011-02-17
- 发明人: Matteo D'Anello , Carlo Battistini , Maria Gioia Fornaretto , Ermes Vanotti
- 申请人: Matteo D'Anello , Carlo Battistini , Maria Gioia Fornaretto , Ermes Vanotti
- 申请人地址: IT Nerviano (MI)
- 专利权人: Nerviano Medical Sciences S.r.l.
- 当前专利权人: Nerviano Medical Sciences S.r.l.
- 当前专利权人地址: IT Nerviano (MI)
- 优先权: EP08155501.3 20080430
- 国际申请: PCT/EP2009/055262 WO 20090430
- 主分类号: C07D403/04
- IPC分类号: C07D403/04 ; C07D207/416
摘要:
The present invention relates to a process for the preparation of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides and to the useful intermediate compounds of such process. 5-(2-Amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carboxamides are described and claimed in W02007110344, which also discloses processes for their preparation. These compounds can be advantageously prepared through a process which allows to obtain the desired products in high yields and purity and with a limited number of steps. The synthesis is starting from a cyano pyrrole derivative, and is characterized from the final hydrolysis of 5-(2-amino-pyrimidin-4-yl)-2-aryl-1H-pyrrole-3-carbonitrile. The compounds prepared according to the process of the present invention are endowed with protein kinase inhibiting activity and, more particularly, Cdc7 or Cdc7/Cdks inhibiting activity. The compounds are therefore useful in the treatment of a variety of cancers, cell proliferative disorders and diseases associated with protein kinases.
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