Improved preparation of oxymorphone from oripavine

Details Improved preparation of oxymorphone from oripavine Improved preparation of oxymorphone from oripavine

C - Chemistry, Metallurgy

07

D

C07D 489/08 (2006.01) A61K 31/485 (2006.01)

Patent

CA 2681740

An improved method for the preparation of oxymorphone from oripavine is provided. Oripavine is oxidized to form 14-hydroxymorphinone after which the oxidation reaction is quenched to prevent the formation of 1-1'-dimer side products. The 14-hydroxymorphinone is then reduced, typically by catalytic hydrogenation to form oxymorphone. The inventive method disclosed is further applicable to the production of morphinan derivatives.

L'invention concerne un procédé amélioré destiné à préparer de l'oxymorphone à partir d'oripavine. L'oripavine est oxydée pour former 14-hydroxymorphinone, après quoi la réaction d'oxydation est réprimée afin d'éviter la formation de sous-produits de type 1-1'-dimère. La 14-hydroxymorphinone est ensuite réduite, typiquement par hydrogénation catalytique, pour former de l'oxymorphone. Le procédé selon l'invention peut en outre être appliqué à la production de dérivés de morphinane.

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