Janssen Pharmaceutica Nv

Tibotec Pharmaceuticals Ltd.

Didier Philippe Robert Schils

Jan Heeres

Jérôme Emile Georges Guillemont

Paul Adriaan Jan Janssen

Elisabeth Therese Jeanne Pasquier

Ruben Gerardus George Leenders

Bart Petrus Anna Maria Jozef Medaer

Joannes Josephus Maria Willems

Alfred Elisabeth Stappers

This invention relates to a process for preparing 4-[(1,6-dihydro-6-oxo-2-pyrimidinyl)-amino]benzonitrile (I) starting from a 4-oxo-1,6-dihydro-pyrimidinylcarboxylic acid ester (II) or starting from a guanidine derivative which is reacted with an alkoxy-methylene malonic acid ester to an ester (II) which is converted to (I), which reaction sequence may be a one-pot procedure.

Process for preparing 4-[(1,6-dihydro-6-OXO-2-pyrimidinyl)amino]benzonitrile

Process for preparing 4-[(1,6-dihydro-6-oxo-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: in the presence of a suitable solvent; with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent;

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:  

Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]amino]-2-2pyrimidinyl]amino]benzonitrile

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Loupoigne, Belgium

Didier Philippe Robert Schils