PROCESSES FOR THE PREPARATION OF 4-[[4-[[4- (2-CYANOETHENYL)-2, 6-DIMETHYLPHENYL]AMINO]-2-PYRIMIDINYL]AMINO]BENZONITRILE

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...

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Hauptverfasser: LEENDERS RUBEN GERARDUS GEORGE, SCHILS DIDIER PHILLIPPE ROBERT, JANSSEN PAUL PETER MARIA, HEERES JAN, PASQUIER ELISABETH THERESE JEANNE, JANSSEN GRAZIELLA MARIA CONSTANTINA, MEDAER BART PETRUS ANNA MARIA JOZEF, GUILLEMONT JEROME EMILE GEORGES, JANSSEN HERWIG JOSEPHUS MARGARETA, JANSSEN JASMINE JOSEE WERNER, ARTS THEODORA JOANNA FRANCISCA, JANSSEN MAROUSSIA GODELIEVE FRANK, JANSSEN PAUL ADRIAAN JAN, WILLEMS JOANNES JOSEPHUS MARIA
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Sprache:eng ; kor
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Zusammenfassung: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).