Abbott Gmbh & Co Kg

Knoll Aktiengesellschaft

Chemische Fabrik Berg Gmbh

Abbott Gmbh & Co. Dg

Peter Klein

Marco Thyes

Klaus Martin Weber

Markus Grosse

Elmar Vilsmaier

Dieter Hix

Heinz Einig

Klaus Scheib

Robert Carter

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.

Method for the production of biperiden II

A process for preparing doxazosin mesylate in modification A which comprises dissolving doxazosin with methanesulfonic acid in methanol or a mixture of an aprotic, polar organic solvent and methanol, removing any turbidity from the resulting solution, and stirring the resulting clear solution until no further precipitate separates out, removing, washing with methanol, heating the precipitate in the moist state in ethanol and, after cooling, isolating the resulting product is described.

Conversion of modification D to modification A of doxazosin mesylate

Drugs comprising modification D of doxazosin mesylate are described. They are suitable for treating high blood pressure.

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Birkenheide, Germany

Peter Klein