Process for preparing ursodeoxycholic acid di-sodium...

C - Chemistry – Metallurgy – 07 – J

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C07J 31/00 (2006.01) C07J 9/00 (2006.01)

Patent

CA 2522720

Process for preparing ursodeoxycholic acid di-sodium 3,7-disulfate comprising: a) reacting ursodeoxycholic acid with sulfamic acid to give ursodeoxycholic acid di-ammonium 3,7-disulfate; b) treating ursodeoxycholic acid di-ammonium 3,7-disulfate with organic sodium bases or inorganic sodium bases and then treating the reaction mixture with an inorganic acid until a pH between 3.0 and 4.5 is reached to give ursodeoxycholic acid di-sodium 3,7-disulfate in solution; c) removing the salts present (by filtration) and then precipitating ursodeoxycholic acid di-sodium 3,7-disulfate by diluting with an organic solvent.

L'invention concerne un procédé de préparation d'acide ursodéoxycholique, 3,7-disulfate di-sodique consistant: a) à faire réagir de l'acide ursodéoxycholique avec de l'acide sulfamique pour obtenir de l'acide ursodéoxycholique, 3,7-disulfate di-ammonium, b) à traiter cet acide ursodéoxycholique, 3,7-disulfate di-ammonium avec des bases de sodium organiques ou des bases de sodium inorganiques puis à traiter ce mélange de réaction avec un acide inorganique jusqu'à ce qu'un pH entre 3,0 et 4,5 soit obtenu pour donner de l'acide ursodéoxycholique, 3,7-disulfate di-sodique en solution et c) à éliminer les sels présents (par filtration) puis à précipiter l'acide ursodéoxycholique, 3,7-disulfate di-sodique par dilution avec un solvant organique.

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