Invention Grant
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
- Patent Title: Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile
- Patent Title (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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Application No.: US12031011Application Date: 2008-02-14
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Publication No.: US07705148B2Publication Date: 2010-04-27
- Inventor: 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
- Applicant: 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
- Applicant Address: BE
- Assignee: Janssen Pharmaceutica N.V.
- Current Assignee: Janssen Pharmaceutica N.V.
- Current Assignee Address: BE
- Main IPC: C07D239/48
- IPC: C07D239/48 ; C07C255/42 ; C07C253/30 ; C07C253/20 ; A61K31/505 ; A61P31/18
![Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile](/abs-image/US/2010/04/27/US07705148B2/abs.jpg.150x150.jpg)
Abstract:
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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