New pyrimidine derivatives

The invention comprises compounds of general formula: wherein R1 represents a hydrogen atom or an alkyl group containing not more than four carbon atoms, Hal represents a halogen atom, and n represents 1 or 2; and their non-toxic acid addition salts; and their preparation by reacting a halo-pyrimid...

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Bibliographische Detailangaben
Hauptverfasser: WRAGG WILLIAM ROBERT, LEE GLYN EVAN, ORTON DENNIS GEORGE, HEMINGWAY ELIZABETH JEAN
Format: Patent
Sprache:eng
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Zusammenfassung:The invention comprises compounds of general formula: wherein R1 represents a hydrogen atom or an alkyl group containing not more than four carbon atoms, Hal represents a halogen atom, and n represents 1 or 2; and their non-toxic acid addition salts; and their preparation by reacting a halo-pyrimidine of formula: with a compound of formula R1NH2. Halo-pyrimidines (II) may be obtained by reacting an amidine of formula: with an acetoacetic ester and a base to form a 2-halophenylalkyl -4- hydroxy -6- methylpyrimidine which is then treated with a phosphorus oxyhalide. p-Chlorophenacetamidine hydrochloride is prepared by the action of ammoniacal ethanol on ethyl p-chlorophenylacetiminate hydrochloride obtained from p-chlorobenzyl cyanide by treatment with hydrogen chloride in ethanol. Pharmaceutical compositions comprise pyrimidines I or their non-toxic acid addition salts in association with a pharmaceutical carrier. Solid (capsules, tablets, pills, powders, granules) and liquid (emulsions, suspensions) forms for oral administration are described. The compounds have diuretic, natriuretic and saluretic properties and act against hypertension.