Process for preparing 4-[(1,6-dihydro-6-OXO-2-pyrimidinyl)amino]benzonitrile
AssigneeTibotec Pharmaceuticals Ltd.
InventorsDidier Philippe Robert Schils, Alfred Elisabeth Stappers
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Abstract
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.
Claims17
A process for preparing a compound of formula (I)
- wherein the compound of formula (I) is prepared by dealkoxycarbonylating a 4-oxo-1,6-dihydro-pyrimidinyl carboxylic acid ester of formula (II):
- wherein R is C1-4alkyl.
A process to prepare (E)-4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]-amino]-benzonitrile, wherein the process encompasses a process for preparing a compound of formula (I)
- wherein the compound of formula (I) is prepared by dealkoxycarbonylating a 4-oxo-1,6-dihydro-pyrimidinyl carboxylic acid ester of formula (II):
- wherein R is C1-4alkyl;
- followed by halogenation of the obtained compound of formula (I) resulting in a compound of formula (C);
- followed by coupling (E)-4-amino-3,5-dimethylcinnamonitrile (compound of formula B) with the obtained compound of formula (C) to give (E)-4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]-amino]-benzonitrile (compound of formula A)
Dependencies are inferred from the claim text.