Process for preparing 6-O-alkenyl-substituted erythromycin derivatives

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. I...

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Hauptverfasser: ANTHONY R. HAIGHT, DAVID R. HILL, JAMES J. NAPIER, TIM GRIEME, PRASAD S. RAJE, JIEN-HEH J. TIEN, MARGARET CHI-PING HSU, STEVEN J. WITTENBERGER, MAHENDRA N. DESHPANDE, MARVIN R. LEANNA, MAUREEN A. MCLAUGHLIN, DAVID RILEY, MATTHEW J. PETERSON, ARTHUR J. COOPER, DANIEL J. PLATA, YI-YIN KU, MICHAEL RASMUSSEN, ERIC J. STONER, HOWARD E. MORTON, RUSSELL D. CINK, ELAINE C. LEE, STEVEN A. KING
Format: Patent
Sprache:eng
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Zusammenfassung: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.