C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 489/12 (2006.01)
Patent
CA 2738066
An improved opiate synthesis scheme is provided. An improvement to the oxidation of oripavine and oripavine derivatives comprises the in-situ formation of the peroxacids required to oxidize the oripavine and oripavine derivatives to form an intermediate. An improvement to the reduction of the intermediate to form oxycodone and oxycodone derivatives comprises reduction utilizing a hydrogen transfer reagent. These improvements allow the production of oxycodone and oxycodone derivatives without isolation of the intermediate, providing a one-pot synthesis method.
L'invention porte sur un schéma de synthèse d'opiacés amélioré. Une amélioration apportée à l'oxydation d'oripavine et de dérivés d'oripavine comporte la formation in situ des peroxyacides nécessaires pour oxyder l'oripavine et les dérivés d'oripavine afin de former un intermédiaire. Une amélioration apportée à la réduction de l'intermédiaire pour former de l'oxycodone et des dérivés d'oxycodone comporte une réduction qui utilise un réactif de transfert d'hydrogène. Ces améliorations permettent la production d'oxycodone et de dérivés d'oxycodone sans isoler l'intermédiaire, ce qui fournit un procédé de synthèse monotope.
Mallinckrodt Inc.
Osler Hoskin & Harcourt Llp
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