METHOD OF PRODUCING N-SULFAMINE-3-(2-GUANIDINETHIAZOL-4-YLMETHYLTHIO)-PROPIONEAMIDINE

METHOD OF PRODUCING N-SULFAMINE-3-(2-GUANIDINETHIAZOL-4-YLMETHYLTHIO)-PROPIONEAMIDINE

The invention relates to a new process for the preparation of N-sulfamyl-3-(2-guanidinothiazol-4-yl-methylthio)-propionitrile (famotidine) of the formula (I) (I) by S-alkylation of 2-guanidino-thiazol-4-yl-methanethiol obtained from S-(2-guanidino-thiazol-4-yl-methyl)-isothiourea dihydrochloride of...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: DERD DOMANI,HU, ERIK BOGSH,HU, FERENTS TRISHLER,HU, PETER DOD,HU, KALMAN KHARSHANI,HU, EVA FEKECH,HU, BELA KHEGEDYUSH,HU, EVA AGAI,HU, ISHTVAN SABADKAI,HU
Format: Patent
Sprache:eng ; rus
Schlagworte:
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
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Beschreibung
Zusammenfassung:The invention relates to a new process for the preparation of N-sulfamyl-3-(2-guanidinothiazol-4-yl-methylthio)-propionitrile (famotidine) of the formula (I) (I) by S-alkylation of 2-guanidino-thiazol-4-yl-methanethiol obtained from S-(2-guanidino-thiazol-4-yl-methyl)-isothiourea dihydrochloride of the formula (III) (III) by in situ treatment with a base, which comprises carrying out S-alkylation with a N-sulfamyl-3-halopropionamidine of the formula (II) (II) wherein X stands for halogen.