Process for preparation of mycophenolic acid and ester derivatives thereof
AssigneeTEVA Gyógyszergyár Zártkörüen Müködö Részvénytársaság
InventorsVilmos Keri, Zoltan Czovek
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Abstract
Provided are processes for preparation of mycophenolic acid.
Claims10
A process for preparing an ester of mycophenolic acid, said process comprising the steps of:
- a) providing a concentrated aqueous alkaline mixture containing mycophenolic acid;
- b) admixing the mixture with a first water-immiscible solvent to form an aqueous phase and a first water-immiscible phase;
- c) separating the aqueous phase;
- d) admixing the aqueous phase with a second water-immiscible solvent at a pH of less than about 7 to form an aqueous phase and a second water-immiscible phase;
- e) separating the second water-immiscible phase;
- f) concentrating the second water-immiscible phase;
- g) crystallizing mycophenolic acid;
- and
- h) converting the mycophenolic acid of step (g) to an ester;
- wherein said ester is a morpholinoethyl ester or a C1-C4 alkyl ester.
Mycophenolic acid in solid state having a purity of at least about 99.5% as measured by HPLC area percentage, and characterized by a powder X-ray diffraction pattern substantially as depicted in FIG. 1A or FIG. 2A.
Mycophenolic acid in solid state having a of total impurity content of less than about 0.1% as measured by HPLC area percentage.
Mycophenolic acid in solid state having a melting point of about 141.6° C. to about 144.6° C., and characterized by a powder X-ray diffraction pattern substantially as depicted in FIG. 1A or FIG. 2A.
Dependencies are inferred from the claim text.