DIDIER PHILIPPE ROBERT SCHILS,JOANNES JOSEPHUS MARIA WILLEMS,BART PETRUS ANNA MARIA JOZEF MEDAER,ELISABETH THERESE JEANNE PASQUIER,PAUL ADRIAAN JAN JANSSEN,JAN HEERES,RUBEN GERARDUS GEORGE LEENDERS,JE
申请号：
IN11262/DELNP/2012
公开号：
IN2012DN11262A
申请日:
2012.12.27
申请国别(地区):
IN
年份:
2016
代理人:
摘要：
The present invention relates to a process 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, (1) which comprises reacting an intermediate of formula (IV), an appropriate acid addition salt or a stereochemically isomeric form thereof (M wherein W2 represents a suitable leaving group, with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent, optionally followed, if desired, by converting the free base into an acid addition salt by treatment with antacid, or conversely, the acid addition salt form into the free base by treatment with alkali end optionally followed, if desired, by preparing stereochemically isomeric forms, or quaternary amines thereof.
