C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 498/18 (2006.01) A61K 31/395 (2006.01) A61K 31/70 (2006.01) A61P 17/00 (2006.01) C07H 19/01 (2006.01)
Patent
CA 2584430
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.
Gyollai Viktor
Szabo Csaba
Heenan Blaikie Llp
Teva Gyogyszergyar Zartkoruen Mukodo Reszvenytarsasag
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