PROCESSES FOR THE PREPARATION OF 4- 4- 4-(2 -CYANOETHENYL)-2,6-DIMETHYLPHENYL )AMINO) -2-PYRIMIDINYL)AMINO BENZONITRILE

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...

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Hauptverfasser: GUILLEMONT JEROME E.G. JOHNSON & JOHNSON PHARM, SCHILS DIDIER P. R. JANSSEN PHARMACEUTICA N.V, HEERES JAN JANSSEN PHARMACEUTICA N.V, MEDAER B. P. A. M. J. JANSSEN PHARMACEUTICA N.V, PASQUIER E. T. J. JOHNSON & JOHNSON PHARMACEUTICAL R.&D, JANSSEN PAUL ADRIAAN JAN, WILLEMS JOANNES J. M. JANSSEN PHARMACEUTICA N.V, LEENDERS RUBEN GERARDUS GEORGE MERCA
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creator GUILLEMONT JEROME E.G. JOHNSON & JOHNSON PHARM
SCHILS DIDIER P. R. JANSSEN PHARMACEUTICA N.V
HEERES JAN JANSSEN PHARMACEUTICA N.V
MEDAER B. P. A. M. J. JANSSEN PHARMACEUTICA N.V
PASQUIER E. T. J. JOHNSON & JOHNSON PHARMACEUTICAL R.&D
JANSSEN PAUL ADRIAAN JAN
WILLEMS JOANNES J. M. JANSSEN PHARMACEUTICA N.V
LEENDERS RUBEN GERARDUS GEORGE MERCA
description 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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subjects ACYCLIC OR CARBOCYCLIC COMPOUNDS
APPARATUS THEREFOR
CHEMISTRY
GENERAL METHODS OF ORGANIC CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title PROCESSES FOR THE PREPARATION OF 4- 4- 4-(2 -CYANOETHENYL)-2,6-DIMETHYLPHENYL )AMINO) -2-PYRIMIDINYL)AMINO BENZONITRILE
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