Method for the production of biperidin

Details Method for the production of biperidin Method for the production of biperidin

2006-04-18

2006-04-18

Desai, Rita (Department: 1625)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

active

07030247

ABSTRACT:
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.

REFERENCES:
patent: 2789110 (1957-04-01), Klavehn
patent: 6835839 (2004-12-01), Klein et al.
patent: 1 005 067 (1957-03-01), None
patent: 11189729 (1999-07-01), None
patent: WO 02/094800 (2002-05-01), None
Ronald Breslow and Uday Maitra, On the Origin of Product Selectivity in Aqueous Dies-Alder Reactions, Tetrahedron Letters. vol. 25. No. 12, pp 1239-1240, 1984, Great Britain.
Ullmans Enzykopadie der technischen Chemie, 4thEdition, vol. 21, Verlag Chemie, 1982, p. 627.
J. G. Dinwiddie and S. P. McManus (J. Org. Chem., 1965, 30, 766).

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