METHODS FOR PREPARING PIMECROLIMUS

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 req...

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Bibliographic Details
Main Authors SZABO, CSABA, GYOLLAI, VIKTOR
Format Patent
LanguageEnglish
French
Published 31.08.2006
Subjects
CHEMISTRY
DERIVATIVES THEREOF
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
NUCLEIC ACIDS
NUCLEOSIDES
NUCLEOTIDES
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
SUGARS
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Summary: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. L'invention porte sur un procédé de préparation de pimécrolimus à partir d'ascomycine selon lequel on fait réagir l'ascomycine avec un réactif de conversion qui convertit l'ascomycine en l'un de ses dérivés activés en C-32. On fait alors réagir l'ascomycine activée avec l'ion chlorure. Le procédé de l'invention présente moins d'étapes que les procédés antérieures et ne nécessite pas la protection du groupe hydroxyle d'ascomycine en C-24, ou la purification du dérivé d'ascomycine activée.
Bibliography:Application Number: WO2005US43541