Abbott Gmbh & Co Kg

Abbott Gmbh & Co. Dg

Markus Grosse

Marco Thyes

Peter Klein

Klaus Martin Weber

Elmar Vilsmaier

The invention relates to a method for producing biperiden by reacting exo-1-(bi-cyclo[2.2.1]hept-5-en-2-yl)-3-piperidino-1-propanone with a phenylmagnesium compound. According to the invention, exo-1-(bi-cyclo[2.2.1]hept-5-en-2-yl)-3-piperidino-1-propanone can be obtained by reacting the exo-ether of enol silylene of formula (IV) with a compound of N-methylenepiperidinium.

Method for producing biperiden IV

The invention relates to a method for the production of biperiden by reacting an exo/endo mixture of 1-(bi-cyclo[2.2.1]hept-5-en-2-yl)-3-piperidino-1-propanone with a phenyl magnesium compound to form an isomer mixture of 1-(bi-cyclo[2.2.1]hept-5-en-2-yl)-1-phenyl-3-piperidino-1-propanol, whereby biperiden is obtained therefrom by conversion of said mixture into corresponding hydrochloride, isolation of said hydrochloride, reconversion to the free base and crystallization of said biperiden.

Method for the production of biperidin

The invention relates to a method for the production of biperiden by reacting an exo/endo mixture of 1-(bicyclo&lsqb;2.2.1.&rsqb;hept-5-en-2-yl) 3-piperidino-1-propanone with a phenyl magnesium compound, wherein the exo/endo ratio of 1-(bicylo&lsqb;2.2.1&rsqb;hept-5-en-2-yl)-3-piperidino-1-propanone is at least 4.5:1.

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Schwetzingen, Germany

Markus Grosse