PROCESS FOR THE MANUFACTURE OF 3-AMINO-SUBSTITUTED GLYCOSYLATED BILE ACIDS

The present invention relates to a process for the preparation and manufacture of 3-amino-substituted glycosylated bile acid derivatives. Novel intermediates and related compounds are also disclosed. In particular, the present invention permits the conversion of cholic acid esters to the 3-amino-7,1...

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Bibliographische Detailangaben
Hauptverfasser: LIU, DASHAN, SOFIA, MICHAEL J, CHEN, ANNA K, KAKARLA, RAMESH, ZEBOVITZ, THOMAS C
Format: Patent
Sprache:eng ; fre
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Beschreibung
Zusammenfassung:The present invention relates to a process for the preparation and manufacture of 3-amino-substituted glycosylated bile acid derivatives. Novel intermediates and related compounds are also disclosed. In particular, the present invention permits the conversion of cholic acid esters to the 3-amino-7,12-bis(glucosyl)cholic acid esters via an azide intermediate. Conditions for the purification and isolation of the desired product is also disclosed to provide an overall manufacturing process suitable for large-scale production.