2-(1-Piperazinyl) pyrimidines, their salts and pharmaceutical compositions containing them
AssigneeSanofi
InventorsPaolo Carminati, Kathleen Biziere, Andre Hallot
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Abstract
The present invention relates to a process for preparing 2-(1-piperazinyl) pyrimidines of formula: ##STR1## in which one of the groups T and Q represents hydrogen, a hydroxyl or lower alkanoyloxy group, and the other represents hydrogen; and X represents: a group --CO--R.sub.1 a group ##STR2## an alkylene-COOY group an alkylene-CO--W group, according to which a 2-(1-piperazinyl) pyrimidine of formula: ##STR3## is reacted with a compound of formula AX in which A is selected from an atom of halogen and an activator group of the carboxylic function of the radical X.
Claims3
2-(1-piperazinyl)pyrimidines of formula:
- ##STR12## in which one of radicals T and Q represents hydrogen, a hydroxyl or lower alkylcarbonyl group and the other represents hydrogen;
- and X represents:
- a group CO--R.sub.1 where R.sub.1 is a lower alkyl
- a group ##STR13## where R.sub.2 is hydrogen, or a lower alkyl, phenyl, p-hydroxyphenyl, benzyl, p-hydroxybenzyl, hydroxymethyl, 1-hydroxyethyl or 3-indolylmethyl group and R.sub.3 is hydrogen, a lower alkylcarbonyl, a benzoyl or an acyl group derived from an amino acid selected from:
- glycine, phenylglycine, alanine, valine, leucine, isoleucine, phenylalanine, tyrosine, serine, threonine or tryptophane, or an acyl group derived from a dipeptide constituted from two of the amino acids mentioned above or R.sub.2 and R.sub.3 taken together form an ethylene group;
- a group Alk--COOY, where Alk represents an alkylene group with straight or branched chain having from 1 to 4 carbon atoms and Y is hydrogen or a lower alkyl;
- a group Alk--CH.sub.2 OZ, where Alk is as defined hereinabove and Z is hydrogen, or a lower alkyl, (Lower alkoxy)-lower alkyl, lower alkylcarbonyl group;
- a group Alk--CO--W where Alk is as defined hereinabove and W is a lower alkyl group,
- as well as the pharmaceutically acceptable acid addition salts thereof.
Dependencies are inferred from the claim text.