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: GUILLEMONT JEROME E.G. JOHNSON & JOHNSON PHARM, SCHILS DIDIER P. R. JANSSEN PHARMACEUTICA N.V, HEERES JAN JANSSEN PHARMACEUTICA N.V, MEDAER B. P. A. M. J. JANSSEN PHARMACEUTICA N.V, PASQUIER E. T. J. JOHNSON & JOHNSON PHARMACEUTICAL R.&D, JANSSEN PAUL ADRIAAN JAN, WILLEMS JOANNES J. M. JANSSEN PHARMACEUTICA N.V, LEENDERS RUBEN GERARDUS GEORGE MERCA
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Sprache:eng ; slv
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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).