Process for the preparation of quaternary N-alkyl morphine or morphinane alkaloid derivatives

Process for the preparation of quaternary N-alkyl morphine or morphinane alkaloid derivatives

The present invention relates to a process for the preparation of quaternary N-alkyl morphin or morphinan alkaloid derivatives of general formula (I) a or b: wherein A is -C(O)-, -C(S)-, -C(=CH 2 )- or -CHA 1 -, A 1 is hydroxy, alkoxy, or acyloxy, R 1 is hydrocarbyl or substituted hydrocarbyl, R 2 i...

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Bibliographische Detailangaben
Hauptverfasser: Heller, Sabrina, Lauterbach, Erik, Heinz Dr, Dinkel, Thomas, Hake, Stephanie, Eipert, Martin
Format: Patent
Sprache:eng ; fre ; ger
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Beschreibung
Zusammenfassung:The present invention relates to a process for the preparation of quaternary N-alkyl morphin or morphinan alkaloid derivatives of general formula (I) a or b: wherein A is -C(O)-, -C(S)-, -C(=CH 2 )- or -CHA 1 -, A 1 is hydroxy, alkoxy, or acyloxy, R 1 is hydrocarbyl or substituted hydrocarbyl, R 2 is hydrocarbyl or substituted hydrocarbyl, X is an anion, Y is hydrogen, hydroxy, alkoxy, or acyloxy. This is achieved by using a nucleophilic nitrogen, phosphor or sulfur containing base in the reaction mixture.