Process for preparing 6-o-alkenyl-substituted erythromycin...

Details Process for preparing 6-o-alkenyl-substituted erythromycin... Process for preparing 6-o-alkenyl-substituted erythromycin...

C - Chemistry, Metallurgy

07

H

C07H 17/08 (2006.01) A61K 31/7048 (2006.01) A61P 31/04 (2006.01)

Patent

CA 2375364

In one aspect, the invention relates to a process for preparing 6-O- substituted erythromycin derivatives comprising reacting 2'-substituted and optionally 4"-substituted 9-oxime erythromycin derivatives with an alkylating agent in the presence of a palladium catalyst and phosphine. In another aspect, the invention relates to processes for preparing 6-O-substituted erythromycin ketolides using the palladium-catalyzed alkylation reaction.

L'invention concerne d'une part une méthode de préparation de dérivés d'érythromycine substitués en 6-0, qui consiste à faire réagir des dérivés 9-oxime d'érythromycine substitués en 2' et éventuellement en 4'' avec un agent d'alkylation, en présence d'un catalyseur de palladium et de phosphine, et, d'autre part, des méthodes de préparation de cétolides d'érythromycine substitués en 6-0 au moyen de la réaction d'alkylation catalisée au palladium.

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