Preparation method of azithromycin dihydrate

C - Chemistry – Metallurgy – 07 – H

Patent

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C07H 17/00 (2006.01) A61K 31/7048 (2006.01) A61K 31/7052 (2006.01) C07H 17/08 (2006.01)

Patent

CA 2396426

This invention relates to a method for preparing azithromycin dihydrate from crude azithromycin by the gradual crystallization of azithromycin from acetone by the addition of a minimal amount of water to effect crystal formation is disclosed. This invention also relates to a method of making azithromycin from desmethyl-azithromycin by dissolving desmethyl-azithromycin in acetone, adding activated carbon, adding formaldehyde, adding formic acid; refluxing the desmethyl-azithromycin acetone solution, adding sodium hydroxide to induce precipitation of azithromycin, and isolating azithromycin.

L'invention concerne un procédé de préparation d'azithromycine dihydratée à partir d'azithromycine brute par cristallisation progressive de l'azithromycine dans l'acétone, avec addition d'une quantité minimale d'eau pour effectuer la formation de cristaux. L'invention concerne également un procédé de fabrication d'azithromycine à partir de desméthyl-azithromycine, consistant à dissoudre la desméthyl-azithromycine dans l'acétone, à ajouter du charbon actif, du formaldéhyde, puis de l'acide formique, à chauffer au reflux la solution acétonique de desméthyl-azithromycine, à ajouter de l'hydroxyde de sodium pour amorcer la précipitation de l'azithromycine et à isoler l'azithromycine.

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