SCHILS DIDIER P. R. JANSSEN PHARMACEUTICA N.V.,WILLEMS JOANNES J. M. JANSSEN PHARMACEUTICA N.V.,MEDAER B. P. A. M. J. JANSSEN PHARMACEUTICA N.V.,PASQUIER E. T. J. JOHNSON & JOHNSON PHARMACEUTICAL R.&D,SCHILS Didier P. R. Janssen Pharmaceutica N.V.,WILLEMS Joannes J. M. Janssen Pharmaceutica N.V.,MEDAER B
申请号：
SI200332275
公开号：
SI1529032T1
申请日:
2003.08.07
申请国别(地区):
SI
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).
