C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 489/02 (2006.01) C07D 489/08 (2006.01)
Patent
CA 2684458
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 concerne un plan de synthèse d'opiacés amélioré. Une amélioration de l'oxydation de l'oripavine et des dérivés d'oripavine comprend la formation in situ des peroxyacides requis pour oxyder l'oripavine et les dérivés d'oripavine afin de former un produit intermédiaire. Une amélioration de la réduction du produit intermédiaire pour former l'oxycodone et les dérivés d'oxycodone comprend une réduction à l'aide d'un réactif de transfert d'hydrogène. Ces améliorations permettent la production d'oxycodone et de dérivés d'oxycodone sans isoler le produit intermédiaire, aboutissant à un procédé de synthèse en cuve unique.
Berberich David Wayne
Cantrell Gary L.
Jiang Tao
Wang Peter X.
Mallinckrodt Inc.
Osler Hoskin & Harcourt Llp
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