Process for the preparation of 6-o-methyl erythromycin a...

Details Process for the preparation of 6-o-methyl erythromycin a... Process for the preparation of 6-o-methyl erythromycin a...

C - Chemistry, Metallurgy

07

H

C07H 17/08 (2006.01)

Patent

CA 2315209

The claimed invention provides a novel method of preparing 6-O-methyl erythromycin A. The process comprises the steps of reducing the 9-keto group of erythromycin A to form a 9-hydroxy erythromycin A, protecting the 9-, 2'-, and/or 4"-hydroxyl groups of erythromycin A, selectively methylating the 6-position of the 9-hydroxy erythromycin A derivative, deprotecting the hydroxyl groups and oxidizing the 9-hydroxyl to afford 6-O-methyl erythromycin A.

L'invention revendiquée concerne un nouveau procédé de préparation de 6-O-méthyle érythromycine A. Le procédé comprend les étapes consistant à réduire le groupe 9-céto d'érythromycine A pour former une 9-hydroxy érythromycine A, à protéger les groupes hydroxyle 9-2'-, et/ou 4" d'érythromycine A, à méthyler sélectivement la position 6 du dérivé de 9-hydroxy érythromycine A, à déprotéger les groupes hydroxyle et à oxyder le 9-hydroxyle pour obtenir la 6-O-méthyle érythromycine A.

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