Methods of preparing pimecrolimus
AssigneeTEVA Gyógyszergyár Zártkörüen Müködö Részvénytársaság
InventorsViktor Gyollai, Csaba Szabo
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Abstract
The present invention provides a process for the preparation of pimecrolimus from ascomycin in which ascomycin is reacted with a conversion reagent that converts ascomycin to its activated derivative at C-32. The activated ascomycin is then reacted with chloride ion. The process of the invention requires fewer process steps than prior art processes, and does not require the protection of the ascomycin C-24 hydroxyl group or the purification of the activated ascomycin derivative.
Claims31
A process for preparing pimecrolimus comprising:
- a) dissolving ascomycin in an organic solvent;
- b) combining ascomycin with a base and a conversion reagent to obtain an activated ascomycin derivative;
- c) reacting the activated derivative of ascomycin with a chloride ion source to obtain pimecrolimus;
- and
- d) recovering the obtained pimecrolimus.
Pimecrolimus having a purity of at least about 95% area by HPLC.
Dependencies are inferred from the claim text.