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PROCESSES FOR THE PREPARATION OF 4-[[4-[[4-(2-CYANOETHENYL)-2,6-DIMETHYLPHENYL]AMINO]-2-PYRIMIDINYL]AMINO BENZONITRILE
专利权人:
Janssen Pharmaceutica N.V.
发明人:
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,Jé
申请号:
IS7621
公开号:
IS2980B
申请日:
2004.12.29
申请国别(地区):
IS
年份:
2017
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).
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