Process for the purification of macrolides

Details Process for the purification of macrolides Process for the purification of macrolides

C - Chemistry, Metallurgy

07

D

C07D 498/18 (2006.01)

Patent

CA 2548297

Process for the recovery of a macrolide in substantially pure form comprising: a) treatment of an impure or crude macrolide with water immiscible solvent, b) optional concentration of the mixture, c) treatment with ammonia gas to phase out impurities, d) separation of impurities, e) optional concentration of the phase containing the macrolide, f) loading on silica gel chromatography, optionally reversed phase or pretreated with silver, and elution of the macrolide, g) affording the macrolide in pure form, h) optional repetition of step f) and g) to afford the macrolide in substantially pure form. The macrolide is preferably tacrolimus, immunomycin or sirolimus.

L'invention concerne un procédé de récupération d'un macrolide sous une forme sensiblement pure. Le procédé comprend les étapes suivantes: a) traitement d'un macrolide impur ou brut avec un solvant immiscible dans l'eau; b) concentration facultative du mélange; c) traitement au gaz ammoniac destiné à éliminer progressivement les impuretés; d) séparation des impuretés; e) concentration facultative de la phase contenant le macrolide; f) chargement sur chromatographie sur gel de silice, à phase éventuellement inversée ou prétraité à l'argent, et élution du macrolide; g) récupération du macrolide sous une forme sensiblement pure; h) répétition facultative des étapes f) et g) pour récupérer le macrolide sous une forme sensiblement pure. Le macrolide est, de préférence, tacrolimus, immunomycine ou sirolimus.

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