LEENDERS, RUBEN GERARDUS GEORGE,JANSSEN, PAUL,ADRIAAN,JAN,GUILLEMONT, JEROME, E.G.,SCHILS, DIDIER P. R.,WILLEMS, JOANNES J. M.,MEDAER, B. P. A. M. J.,PASQUIER, E., T. J.,HEERES, JAN
申请号:
DK03787813
公开号:
DK1529032T3
申请日:
2003.08.07
申请国别(地区):
DK
年份:
2013
代理人:
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).