Process for making morphine-6-glucuronide and its analogues using haloglucuronate ester intermediates

This is the National Phase Application of PCT/GB 00/02232 filed, Jun. 20, 2000. A process for manufacturing morphine-6-glucuronide and related compounds of the general structure of Formula 1: wherein optionally substituted morphine is conjugated with an optionally substituted member of a new class o...

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Hauptverfasser: Scheinmann, Feodor, Stachulski, Andrew Valentine, Ferguson, John, Law, Jane Louise
Format: Patent
Sprache:eng
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Zusammenfassung:This is the National Phase Application of PCT/GB 00/02232 filed, Jun. 20, 2000. A process for manufacturing morphine-6-glucuronide and related compounds of the general structure of 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 iodinium compound. The conjugation may be followed by conversion of Rof Formula 1 into hydrogen and/or the removal of the ester groups from the glucuronic residue at Rof Formula 1.