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 |