Process for the manufacture of 3-amino-substituted...

C - Chemistry – Metallurgy – 07 – J

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C07J 41/00 (2006.01) C07H 15/18 (2006.01) C07H 15/203 (2006.01) C07H 23/00 (2006.01) C07J 9/00 (2006.01) C07J 17/00 (2006.01) C07J 31/00 (2006.01)

Patent

CA 2193733

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.

Procédé de préparation et de fabrication de dérivés d'acide biliaire glycosylés à substitution amino en position 3. De nouveaux intermédiaires et composés apparentés sont également décrits. En particulier, la présente invention permet la conversion d'esters d'acide cholique en esters d'acide 3-amino-7,12-bis(glucosyl)cholique à l'aide d'un intermédiaire azide. Des conditions de purification et d'isolation du produit désiré sont en outre décrites et permettent d'obtenir un procédé de préparation global approprié pour la production à grande échelle.

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