Improvements in macrolide production

C - Chemistry – Metallurgy – 07 – H

Patent

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C07H 17/00 (2006.01) A61K 31/7042 (2006.01) C07H 17/08 (2006.01)

Patent

CA 2330007

A process for the production of azithromycins by methylation of the nitrogen atom in position 9 of the ring structure in 9-deoxo-9a-aza-9a-homoerythromycins in the presence of formaldehyde and in the presence of a reducing agent in non-halogenated solvent; and azithromycin which is free from halogenated organic solvent in a stable anhydrous form; or in the form of a solvate with non-halogenated solvent with the exception of water.

L'invention concerne un procédé de fabrication d'azythromycines par la méthylation de l'atome d'azote en position 9 de la structure cyclique dans les 9-déoxo-9a-aza-9a-homoérythromycines en présence de formaldéhyde et d'un agent réducteur dans un solvant non halogéné, ainsi qu'un azythromycine exempt de solvant organique halogéné sous une forme anhydre stable, ou sous la forme d'un solvate avec un solvant non halogéné, exception faite de l'eau.

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