C-14 oxidation of morphine derivatives

1 2 The present invention relates to process for the preparation of a 14-hydroxynormorphinone derivative of formula IV comprising reacting the compound of formula III, with a cobalt (II) oxidant in the presence of a mild base and air or oxygen as the cooxidant; wherein Ris (1C-7C)alkyl optionally su...

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Bibliographische Detailangaben
Hauptverfasser: Linders, Joannes Theodorus Maria, Vrijhof, Pieter
Format: Patent
Sprache:eng
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Zusammenfassung:1 2 The present invention relates to process for the preparation of a 14-hydroxynormorphinone derivative of formula IV comprising reacting the compound of formula III, with a cobalt (II) oxidant in the presence of a mild base and air or oxygen as the cooxidant; wherein Ris (1C-7C)alkyl optionally substituted with one or more chlorines, butenyl, vinyl, benzyl, phenyl or naphthyl; and Ris benzyl or benzyl substituted with one or more (1C-6C)alkoxy group or benzyl substituted with one or more halogen. The process is very suitable in the production of noroxymorphone.