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US 2021/0101926 A1Published application
Synthesis of glycoconjugate derivatives of a bile acid
AssigneeDipharma Francis S.R.L.
InventorsAlessandro RESTELLI, Philipp CARBONI, Gabriele RAZZETTI
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Abstract
Processes for the synthesis and purification of glycoconjugate derivatives of cholic acid are provided herein.
Claims15
A process for preparing glycocholic acid of formula (I), or a salt thereof,
- comprising:
- reacting cholic acid of formula (II)
- with pivaloyl chloride in the presence of a base to give an activated intermediate of formula (III)
- reacting the obtained activated intermediate of formula (III) with glycine or with an ester or a salt thereof;
- in case of reacting with a glycine ester, hydrolyzing subsequently the ester;
- isolating glycocholic acid of formula (I) and optionally salification thereof.
3 more elements
A compound of formula (III):
A composition comprising glycocholic acid of formula (I)
- with a purity higher than 99.5%.
Dependencies are inferred from the claim text.