发明授权
US07705148B2 Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile
有权
制备4 - [[4 - [[4-(2-氰基乙烯基)-2,6-二甲基苯基]氨基] -2-嘧啶基]氨基]苄腈的方法
- 专利标题: Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile
- 专利标题(中): 制备4 - [[4 - [[4-(2-氰基乙烯基)-2,6-二甲基苯基]氨基] -2-嘧啶基]氨基]苄腈的方法
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申请号: US12031011申请日: 2008-02-14
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公开(公告)号: US07705148B2公开(公告)日: 2010-04-27
- 发明人: Didier Philippe Robert Schils , Joannes Josephus Maria Willems , Bart Petrus Anna Maria Jozef Medaer , Elisabeth Therese Jeanne Pasquier , Paul Adriaan Jan Janssen , Jan Heeres , Ruben Gerardus George Leenders , Jérôme Emile Georges Guillemont
- 申请人: Didier Philippe Robert Schils , Joannes Josephus Maria Willems , Bart Petrus Anna Maria Jozef Medaer , Elisabeth Therese Jeanne Pasquier , Paul Adriaan Jan Janssen , Jan Heeres , Ruben Gerardus George Leenders , Jérôme Emile Georges Guillemont
- 申请人地址: BE
- 专利权人: Janssen Pharmaceutica N.V.
- 当前专利权人: Janssen Pharmaceutica N.V.
- 当前专利权人地址: BE
- 主分类号: C07D239/48
- IPC分类号: C07D239/48 ; C07C255/42 ; C07C253/30 ; C07C253/20 ; A61K31/505 ; A61P31/18
摘要:
Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).
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