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 PL373679(A1) 申请公布日期 2005.09.05
申请号 PL20030373679 申请日期 2003.08.07
申请人 JANSSEN PHARMACEUTICA NV. 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;GUILLEMONT JEROME EMILE GEORGES
分类号 A61K31/505;A61P31/18;C07B61/00;C07C253/20;C07C253/30;C07C255/07;C07C255/42;C07D239/48 主分类号 A61K31/505
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