发明名称 PROCESSES FOR THE PREPARATION OF 4-[[4-[[-4-(2-CYANOETHENYL)-2,6-DIMETHYLPHENYL]AMINO]-2-PYRIMIDINYL]AMINO]BENZONITRILE
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).
申请公布号 EA007953(B1) 申请公布日期 2007.02.27
申请号 EA20050000325 申请日期 2003.08.07
申请人 JANSSEN PHARMACEUTICA N.V. 发明人 SCHILS DIDIER, PHILIPPE, ROBERT;WILLEMS JOHANNES, JOSEPHUS, MARIA;MEDAER BART, PETRUS, ANNA, MARIA, JOSEF;PASQIER ELISABETH, THERESE, JEANNE;JANSSEN PAUL, ADRIAN, JAN;HEERES JAN;LEEDERS RUBEN, GERARDUS, GEORGE;GULLEMONT JEROME, EMILE, GEORGES
分类号 C07C255/42;A61K31/505;A61P31/18;C07B61/00;C07C253/20;C07C253/30;C07C255/07;C07D239/48 主分类号 C07C255/42
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