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1. WO1996008461 - PROCESS FOR PREPARING SELEGILIN

Publication Number WO/1996/008461
Publication Date 21.03.1996
International Application No. PCT/EP1995/003460
International Filing Date 02.09.1995
Chapter 2 Demand Filed 17.01.1996
IPC
C07C 209/60 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
209Preparation of compounds containing amino groups bound to a carbon skeleton
60by condensation or addition reactions, e.g. Mannich reaction, addition of ammonia or amines to alkenes or to alkynes or addition of compounds containing an active hydrogen atom to Schiff's bases, quinone imines, or aziranes
CPC
C07C 209/60
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
209Preparation of compounds containing amino groups bound to a carbon skeleton
60by condensation or addition reactions, e.g. Mannich reaction, addition of ammonia or amines to alkenes or to alkynes or addition of compounds containing an active hydrogen atom to Schiff's bases, quinone imines, or aziranes
Applicants
  • KNOLL AKTIENGESELLSCHAFT [DE]/[DE] (AllExceptUS)
  • OTT-DEMBROWSKI, Silvia [DE]/[DE] (UsOnly)
  • CYRUS, Richard [DE]/[DE] (UsOnly)
  • SCHMIDT, Jörg [DE]/[DE] (UsOnly)
  • WAIBLINGER, Hans [DE]/[DE] (UsOnly)
Inventors
  • OTT-DEMBROWSKI, Silvia
  • CYRUS, Richard
  • SCHMIDT, Jörg
  • WAIBLINGER, Hans
Agents
  • KARAU, Wolfgang
Priority Data
P 44 32 610.613.09.1994DE
Publication Language German (DE)
Filing Language German (DE)
Designated States
Title
(DE) VERFAHREN ZUR HERSTELLUNG VON SELEGILIN
(EN) PROCESS FOR PREPARING SELEGILIN
(FR) PROCEDE DE FABRICATION DE SELEGILINE
Abstract
(DE)
Es wird ein Verfahren zur Herstellung von Selegilin-Hydrochlorid durch Umsetzen von R-(-)-N,$g(a)-Dimethyl-phenylethylamin mit 3-Brom-1-propin beschrieben, welches darin besteht, daß man die Substanzen im Molverhältnis von etwa 2:1 bis 30-50 °C in einem Lösungsmittelgemisch aus einem aromatischen Kohlenwasserstoff und Wasser in Abwesenheit eines Katalysators umsetzt und das Selegilin aus der organischen Phase isoliert und in das Hydrochlorid überführt.
(EN)
The invention concerns a process for preparing selegilin hydrochloride by reacting R-(-)-N,$g(a)-dimethyl-phenylethylamine with 3-bromo-1-propine, characterized in that the substances are reacted in a molar ratio of approximately 2:1 at a temperature of between 30 and 50 °C in a solvent mixture comprising an aromatic hydrocarbon and water without a catalyst, and the selegilin is isolated from the organic phase and converted into hydrochloride.
(FR)
Procédé de fabrication de chlorhydrate de sélégiline consistant à faire réagir la R-(-)-N,$g(a)-diméthyl-phényléthylamine avec la 3-bromo-1-propine, caractérisé en ce qu'on fait réagir les substances dans un rapport molaire d'environ 2/1, à une température comprise entre 30 et 50 °C, dans un mélange de solvants formé d'un hydrocarbure aromatique et d'eau, sans catalyseur, et en ce qu'on isole la sélégiline de la phase organique et qu'on la transforme en chlorhydrate.
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