Process for preparing 6-o-substituted erythromycin derivatives

US6437106B1 · kind B1 · utility

Assignee

• Abbott Laboratories · US

Inventors

• Eric J. Stoner · Kenosha, US
• Matthew Peterson · Redwood City, US
• Yi-Yin Ku · Buffalo Grove, US
• Russell D. Cink · Grayslake, US
• Arthur J. Cooper · Mentor, US
• Mahendra N. Deshpande · Gurnee, US
• Tim Grieme · Chicago, US
• Anthony R. Haight · Wadsworth, US
• David R. Hill · Gurnee, US
• Margaret Chi-Ping Hsu · Vernon Hills, US
• Steven A. King · Gurnee, US
• Marvin R. Leanna · Grayslake, US
• Elaine Chungmin Lee · Mundelein, US
• Maureen A. McLaughlin · Kenosha, US
• Howard E. Morton · Gurnee, US
• James J. Napier · Antioch, US
• Daniel Plata · Wadsworth, US
• Prasad Raje · Glenmont, US
• Michael Dolberg Rasmussen · Kenosha, US
• David A. Riley · Kenosha, US
• Jien-Heh J. Tien · Libertyville, US
• Steven J. Wittenberger · Mundelein, US

Key dates

• Filing date: Mar 3, 2000
• Grant date: Aug 20, 2002
• Expiry date: Mar 3, 2020

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P31/04
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

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.