Abbott Laboratories Corporation

Other

Abbvie Inc.

Ramiya H Premchandran

Steven A King

Sou-Jen Chang

Hemant H Patel

Steven J Wittenberger

Jien-Heh J Tien

Lawrence Kolaczkowski

Michael S Allen

Daniel J Plata

Stephen L Condon

Eric J Stoner

Subhash R Patel

John A DeMattei

Sukumar Manna

Paul J Nichols

Paul Nichols

Albert V Thomas

John J Demattei

Howard E Morton

Juliette K Busse

Francis A Kerdesky

Robert F Keyes

Gregory S Wayne

Lakshmi Bhagavatula

John E Lallaman

John E Hengeveld

Anne E Bailey

Ashok K Gupta

Todd S McDermott

Anne H Kemp

Richard R Copp, Jr

John E Dete

Xiaoxing Dong

Jonathan P Pease

Francis A J Kerdesky

Lakshima Bhagavatula

The invention relates to a process for preparing quinoline-substituted carbonate and carbamate compounds, which are important intermediates in the synthesis of 6-O-substituted macrolide antibiotics. The process employs metal-catalyzed coupling reactions to provide a carbonate or carbamate of formula (I) or (II) or a substrate that can be reduced to obtain the same.

Preparation of quinoline-substituted carbonate and carbamate derivatives

Disclosed herein is a process for the preparation of erythromycin derivatives, or pharmaceutically acceptable salts thereof, which contain an optionally substituted propargyl group at the 6-O-position.

Process for the preparation of 6-O-propargyl erythromycin derivatives

A process for the preparation of preparation of farnesyltransferase inhibitors of formula (I)

Process for the preparation of farnesyltransferase inhibitors

The claimed invention relates to a novel process of preparing N-demethyl-N-alkyl-4'-deoxy erythromycin A and B. The process comprises protecting the 2'-hydroxy or the 2'- and 11-hydroxy of a N-demethyl-4'-deoxy erythromycin derivative having the formula: ##STR1## where R.sub.b is H or OH, with a silyl protecting group and alkylating the N-position of the desosamine sugar.

Process for preparing N-demethyl-N-alkyl erythromycin derivatives

A process for the preparation of N-demethyl-4'-deoxy-erythromycins A and B, having the formula: ##STR1## wherein R.sup.a is H or OH, by stepwise addition of iodine and base to the N-dimethyl-4'-deoxyerythromycin, preferably, accompanied by sparging with an inert gas.

Process for preparation of N-demethyl-4'-deoxy-erthromycins A and B

Disclosed is an improved and efficient process for N-desmethylating the 3'-amino nitrogen of erythromycins and for converting the 3'-N-desmethylated erythromycins into 3'-N-substituted derivatives of 8,9-anhydro-erythromycin 6,9-hemiketals.

Process for N-desmethylating erythromycins and derivatives thereof

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Gurnee, IL, United States of America

Ramiya H Premchandran