Method for the purification of mycophenolate mofetil
AssigneeDSM Sinochem Pharmaceuticals Netherlands B.V.
InventorRobertus Mattheus De Pater
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Abstract
The present invention provides a method for the preparation of mycophenolate mofetil wherein mycophenolic acid or an amine salt of mycophenolic acid is esterified with 2-morpholinoethanol, the resulting mixture is extracted into water at a pH-value between 1.0 and 3.0, and mycophenolate mofetil is back-extracted in a water-immiscible solvent at a pH-value between 3.0 and 5.0.
Claims7
Method for the preparation of mycophenolate mofetil comprising the steps of:
- (a) esterification of mycophenolic acid or an amine salt of mycophenolic acid with 2-morpholinoethanol;
- (b) contacting the mixture obtained in step (a) with water at a pH-value between 1.0 and 3.0;
- (c) separating the aqueous phase from the mixture obtained in step (b);
- (d) contacting the aqueous phase obtained in step (c) with a water-immiscible solvent;
- (e) separating the non-aqueous phase from the mixture obtained in step (d), characterized in that step (d) is carried out at a pH-value between 3.0 and 5.0.
A composition comprising mycophenolate mofetil and between 0.002% (w/w) and 0.05% (w/w) of a compound of formula (1):
A pharmaceutical composition comprising mycophenolate mofetil and between 0.002% (w/w) and 0.05% (w/w) of a compound of formula (1):
A medicament which comprises mycophenolate mofetil and between 0.002% (w/w) and 0.05% (w/w) of a compound of formula (1):
Dependencies are inferred from the claim text.