Abbott Laboratories Corporation

Merck Frosst Canada, Inc.

Medivir Ab

Other

Merck + Co., Inc.

Mediver Ab

Howard E Morton

M Robert Leanna

Anthony Ralph Haight

Timothy L Stuk

Jien-Heh J Tien

Michael S Allen

Hing L Sham

Yvan Guindon

Thomas J Sowin

Daniel S Reno

John W Gillard

Daniel J Plata

Timothy A Robbins

David Scarpetti

Linda M Lijewski

Christiane Yoakim

Francis A Kerdesky

Laura Melcher

Daniel W Norbeck

Chen Zhao

Yves Girard

Yi-Yin Ku

Steven A King

Michael Rasmussen

Denton C Langridge

William R Baker

Padam N Sharma

Prasad S Raje

John K Pratt

Rejean Fortin

Anthony K Fung

Sou-Jen Chang

David A Riley

Steven M Hannick

Timothy A Grieme

Bikshandarkoil A Narayanan

Lakshmi Bhagavatula

Bradley D Gates

Elaine C Lee

Tim Grieme

Zhenping Tian

Mike A Fitzgerald

Biswanath De

Daniel A Dickman

James J Napier

Steven J Wittenberger

Kirill A Lukin

Lawrence Kolaczkowski

Daniel Joseph Kerkman

Russell Drew Cink

David R Hill

Bruce W Horrom

Yu-Ming M Pu

Marvin Robert Leanna

Eric J Stoner

Arthur J Cooper

Stephen L Condon

Margaret Chi-Ping Hsu

Ramiya H Premchandran

Hormoz Mazdiyasni

Gregory S Wayne

Thomas M Zydowsky

Robert M Leanna

Bhadra Shelat

Chi-nung W Hsiao

Maureen Ann McLaughlin

John E Lallaman

Pulla Reddy Singam

Ashok K Gupta

Ramesh R Patel

Mahendra N Deshpande

Weijiang Zhang

Cynthia B Curty

Matthew John Peterson

Tiffany Spitz

John Bellettini

Daniel Plata

Jonathan P Pease

Francis A J Kerdesky

Greg Lannoye

Greg Wayne

Cheng-Xi Yang

David Riley

Marvin R Leanna

Maureen A Mclaughlin

Methods and novel intermediates for the preparation of acyclic nucleoside derivatives of the formula:where one of Rand Ris an amino acid acyl group and the other of Rand Ris a &#x2014;C(O)C-Csaturated or monounsaturated, optionally substituted alkyl and Ris OH or H; or a pharmaceutically acceptable salt thereof.

Synthesis of acyclic nucleoside derivatives

The instant invention discloses a process for the synthesis of substituted indole cell proliferation inhibitors.

Process for the preparation of cell proliferation inhibitors

The present invention relates to an efficient process for the preparation of 5-(substituted)-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-chromeno&lsqb;3,4-f&rsqb;quinolines.

Process for the preparation of 5-(substituted)-10 methoxy-2,2,4-trimethyl-2,5-dihydro-1H-chromeno &lsqb;3,4-F&rsqb; quinolines and derivatives thereof

The present invention relates to the preparation of chiral glucocorticoid receptor agents via biaryl atropisomers.

Process for the preparation of chiral glucocorticoid receptor agents

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

Process for the preparation of 5-(substituted)-10-methoxy-2,2,4-trimethyl-2,5-dihydro-1H-chromeno&lsqb;3,4-F&rsqb;quinolines and derivatives thereof

In one aspect, the invention relates to a process for preparing 6-O-substituted erythromycin derivatives comprising reacting 2&prime;-substituted and optionally 4&Prime;-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.

Process for preparing 6-o-substituted erythromycin derivatives

Methods and novel intermediates of the formula:

A process for the preparation of 5-hydroxymethylthiazole comprises reacting a compound of the formula, ##STR1## with a carboxylic acid salt (optimally in the presence of a quaternary ammonium salt) and hydrolyzing the resulting ester. Subsequent dechlorination gives 5-hydroxymethylthiazole.

Process for preparation of 5-hydroxymethylthiazole

Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R.sub.6 and R.sub.7 are each hydrogen or R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or R.sub.6 is as defined above and R.sub.7 is R.sub.7a OC(O)-- wherein R.sub.7a is loweralkyl or benzyl; or R.sub.6 and R.sub.7 taken together with the nitrogen atom to which they are bonded are ##STR4## wherein R.sub.f, R.sub.g, R.sub.h and R.sub.i are independently selected from hydrogen, loweralkyl, alkoxy, halogen and trifluoromethyl and R.sub.8 is hydrogen or --C(O)R' wherein R' is loweralkyl, alkoxy, benzyloxy or phenyl wherein the phenyl ring is unsubstituted or substituted with one, two or three substituents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or an acid addition salt thereof.

Process for the preparation of a disubstituted

Process for the preparation of a substituted 2.5-diamino-3-hydroxyhexane

Intermediates and processes are disclosed which are useful for the preparation of a substantially pure compound of the formula: ##STR1## wherein R.sub.6 and R.sub.7 are each hydrogen or R.sub.6 and R.sub.7 are independently selected from ##STR2## wherein R.sub.a and R.sub.b are independently selected from hydrogen, loweralkyl and phenyl and R.sub.c, R.sub.d and R.sub.e are independently selected from hydrogen, loweralkyl, trifluoromethyl, alkoxy, halo and phenyl; and ##STR3## wherein the naphthyl ring is unsubstituted or substituted with one, two or three substitutents independently selected from loweralkyl, trifluoromethyl, alkoxy and halo; or

Process for the preparation of a substituted 2.5-diamono-3-hydroxy-hexane

Process for the preparation of a substituted 2,5-diamino-3-hydroxyhexane

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Gurnee, IL, United States of America

Howard E Morton