PROCESS FOR MAKING MORPHINE-6-GLUCURONIDE AND ITS ANALOGUES USING HALOGLUCURONATE ESTER INTERMEDIATES

PROCESS FOR MAKING MORPHINE-6-GLUCURONIDE AND ITS ANALOGUES USING HALOGLUCURONATE ESTER INTERMEDIATES

A process is provided for the manufacture of morphine-6-glucuronide and related compounds of the general structure shown in Formula (1), wherein optionally substituted morphine is conjugated with an optionally substituted member of a new class of intermediates, namely 1-haloglucuronate esters, in th...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: LAW, JANE LOUISE, FERGUSON, JOHN, SCHEINMANN, FEODOR, STACHULSKI, ANDREW VALENTINE
Format: Patent
Sprache:eng ; fre
Schlagworte:
APPARATUS THEREFOR
CHEMISTRY
DERIVATIVES THEREOF
GENERAL METHODS OF ORGANIC CHEMISTRY
METALLURGY
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
SUGARS
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Beschreibung
Zusammenfassung:A process is provided for the manufacture of morphine-6-glucuronide and related compounds of the general structure shown in Formula (1), wherein optionally substituted morphine is conjugated with an optionally substituted member of a new class of intermediates, namely 1-haloglucuronate esters, in the presence of iodine or an iodonium compound. This may be followed by a conversion of R1 (Formula (1)) into hydrogen and/or the removal of the ester groups from the glucuronic residue at R2 (Formula (1)).