METHOD OF SELEGILINE'S HYDROCHLORIDE PRODUCTION

METHOD OF SELEGILINE'S HYDROCHLORIDE PRODUCTION

The present invention relates to a new method for preparing selegiline hydrochloride, particularly in the form of its (R)-(-)-enantiomer. Selegiline hydrochloride is a highly potent antiparkinsonic agent with low toxicity. The method of the invention consists in that 2-methylamino-1-phenylpropane is...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: FERENC MILAN RNDR.,CS, POSPISIL JOSEF,CS, HAJICEK JOSEF CSC.,CS, HRBATA JIRI PHARM. DR.,CS, KREPELKA JIRI CSC.,CS, PIHERA PAVEL,CS, KVAPIL LUBOMIR RNDR.,CS, BRUNOVA BOHUMILA CSC.,CS
Format: Patent
Sprache:eng
Schlagworte:
ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
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 present invention relates to a new method for preparing selegiline hydrochloride, particularly in the form of its (R)-(-)-enantiomer. Selegiline hydrochloride is a highly potent antiparkinsonic agent with low toxicity. The method of the invention consists in that 2-methylamino-1-phenylpropane is reacted with propargyl bromide and potassium carbonate, both in a molar excess of at least 10 %, based on the amount of 2-methylamino-1-phenylpropane, equivalent, with use of chloroform, methylene chloride, methanol or dimethylformamide as solvent, at a temperature within the range of from +5 DEG C to the boiling temperature of the reaction mixture; the formed base is converted into the hydrochloride using hydrogen chloride in isopropanol.