发明申请
WO2004016581A1 PROCESSES FOR THE PREPARATION OF 4-[[4-[[4-(2-CYANOETHENYL)-2,6-DIMETHYLPHENYL]AMINO]-2-PYRIMIDINYL]AMINO]BENZONITRILE
审中-公开
制备4 - [[4 - [[4-（2-氰基乙基）-2,6-二甲基苯基]氨基] -2-吡啶基]氨基]苯并噻唑的方法
- 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-氰基乙基）-2,6-二甲基苯基]氨基] -2-吡啶基]氨基]苯并噻唑的方法
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申请号： PCT/EP2003/050366申请日： 2003-08-07
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公开(公告)号： WO2004016581A1公开(公告)日： 2004-02-26
- 发明人: SCHILS, Didier, Philippe, Robert , WILLEMS, Joannes, Josephus, Maria , MEDAER, Bart, Petrus, Anna, Maria, Jozef , PASQUIER, Elisabeth, Therese, Jeanne , JANSSEN, Paul, Adriaan, Jan , HEERES, Jan , LEENDERS, Ruben, Gerardus, George
- 申请人： JANSSEN PHARMACEUTICA N.V. , GUILLEMONT, Jérôme, Emile, Georges , SCHILS, Didier, Philippe, Robert , WILLEMS, Joannes, Josephus, Maria , MEDAER, Bart, Petrus, Anna, Maria, Jozef , PASQUIER, Elisabeth, Therese, Jeanne , JANSSEN, Paul, Adriaan, Jan , HEERES, Jan , LEENDERS, Ruben, Gerardus, George
- 申请人地址： Turnhoutseweg 30, B-2340 Beerse BE
- 专利权人： JANSSEN PHARMACEUTICA N.V.,GUILLEMONT, Jérôme, Emile, Georges,SCHILS, Didier, Philippe, Robert,WILLEMS, Joannes, Josephus, Maria,MEDAER, Bart, Petrus, Anna, Maria, Jozef,PASQUIER, Elisabeth, Therese, Jeanne,JANSSEN, Paul, Adriaan, Jan,HEERES, Jan,LEENDERS, Ruben, Gerardus, George
- 当前专利权人： JANSSEN PHARMACEUTICA N.V.,GUILLEMONT, Jérôme, Emile, Georges,SCHILS, Didier, Philippe, Robert,WILLEMS, Joannes, Josephus, Maria,MEDAER, Bart, Petrus, Anna, Maria, Jozef,PASQUIER, Elisabeth, Therese, Jeanne,JANSSEN, Paul, Adriaan, Jan,HEERES, Jan,LEENDERS, Ruben, Gerardus, George
- 当前专利权人地址： Turnhoutseweg 30, B-2340 Beerse BE
- 代理机构： JANSSEN PHARMACEUTICA N.V.
- 优先权： EP02078306.4 20020809
- 主分类号： C07C255/42
- IPC分类号： C07C255/42
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).
