Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Other

Banyu Pharmaceutical Co. Ltd

Ulf H Dolling

John M Williams

David M Tschaen

Richard D Tillyer

Lisa F Frey

Edward J Grabowski

Ian Frank Cottrell

Ronald B Jobson

Mark Cameron

Apurba Bhattacharya

Nobuyoshi Yasuda

Richard John Varsolona

James A McCauley

Seemon H Pines

Daniel Richard Sidler

Richard Desmond

Lyndon C Xavier

Michael Stewart Ashwood

Alan W Douglas

David Hands

Karel M Brands

Robert Darrin Wilson

Ann Decamp

Antony J Davies

Dale L Rieger

Yulan Li

Yoshiaki Kato

Linghang Zhuang

Michael A Patane

Melissa S Egbertson

John S Wai

Paul N Devine

David Askin

Raymond Cvetovich

Philip J Pye

Louis S Crocker

Joseph S Amato

Jeremy Peter Scott

R Scott Hoerrner

Robert Wenslow

Hsien-Hsin Tung

Debra S Perlow

David R Lieberman

Karel M J Brands

Wei Han

Antony John Davies

Karel Marie Joseph Brands

Joseph Kukura, Ii

Brian K Johnson

Remy Angelaud

Danny Mancheno

Rowena D Ruzek

Renato T Skerlj

Bruce S Foster

Sarah Elizabeth Brewer

Deborah Camille Hammond

Ben Marcune

Essa Hsinyi Hu

Louis Crocker

Daniel Sidler

Joseph Ii Kukura

Hydroxy (tetra- or hexa-)hydronaphthyridine dione compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein a, R1?, R2?, R3?, R4? and R5? are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. 

HIV integrase inhibitors

There is provided stereoselective route to a compound of formula I: wherein R represents H or an alkali metal, Arrepresents 4-chlorophenyl and Arrepresents 2,5-difluorophenyl.

Stereoselective synthesis of a 4,4-disubstituted cyclohexanepropanoic acid

The present invention relates to a process for reducing the levels of organic solvents to pharmaceutically acceptable levels in thermally unstable crystalline carbapenem solids represented by formula I:or a salt thereof, wherein Rand R, are the same or different, and are selected from H, alkyl, aryl, and heteroaryl, comprising washing a carbapenem solid containing organic solvent with an organic solvent containing water; and using vacuum and/or inert gas (hydrated or dry) at low temperature to produce a compound of formula I containing pharmaceutically acceptable levels of organic solvents, wherein the water content of the crystalline carbapenem solid, correcting for organic solvents, is maintained at about 13% to about 25% during the process.

Process for making carbapenem compounds

The present invention relates to a process for the preparation of morpholine derivatives of formula (I) which are useful as a therapeutic agents.

Chemical synthesis of 1,2,4-triazolinone derivative

Chemical synthesis of morpholine derivatives

A stabilized carbapenem intermediate compound represented by the formula 1:

Stabilized carbapenem intermediates and improved process for carbapenem synthesis

This invention relates to a key intermediate in the synthesis of an endothelin antagonist and the synthesis of this key intermediate using an asymmetric conjugate addition reaction.

Asymmetric conjugate addition reaction

A process of synthesizing a compound of the formula 1: ##STR1## is described. A compound of the formula 2: ##STR2## is reacted with diphenylphosphinic chloride to activate the carboxylic acid group, and then reacted with methanesulfonyl chloride to produce a compound of formula 4: ##STR3## Compound 4 is then reacted with a group II metal sulfide source in water to produce a compound of formula 1.

Process for synthesizing carbapenem side chain intermediates

This invention relates to a key intermediate in the synthesis of an endothelin antagonist, the synthesis of this key intermediate and the synthesis of an endothelin antagonist using this intermediate in a stereoselective deoxygenation reaction.

Stereoselective deoxygenation reaction

Disclosed is a new process for producing finasteride which involves reacting the magnesium halide salt of 17.beta.-carboalkoxy-4-aza-5.alpha.-androst-1-en-3-one with t-butylamino magnesium halide, present in at least a 2:1 molar ratio to the ester, formed from t-butyl amine and an aliphatic/aryl magnesium halide at ambient temperature in an inert organic solvent under an inert atmosphere followed by heating and recovering the product finasteride. Also disclosed are two polymorphic crystalline Forms I and II of finasteride, and methods of their production.

Finasteride processes

Compounds formed by an asymmetric conjugate addition reaction

The invention encompasses a process for making compounds of Formula I useful in the treatment of inflammation and other cyclooxygenase-2 mediated diseases.

Process of preparing phenyl heterocycles useful as COX-2 inhibitors

The present invention provides a process for forming 5-(alkyl or alkoxy)carbonyl-6-alkyl-4-(aryl or alkyl)-3,4-2(1H)-dihydropyrimidinones by combining a .beta.-keto ester or diketone, an aldehyde and urea in the presence of a boron reagent, a metal salt (e.g., Cu.sub.2 O) and a catalyst (e.g., acid). The reaction is typically run in one pot in a solvent to afford dihydropyrimidinones in higher yields and with easier work up than previously known methods.

Process for making dihydropyrimidinones

A simple, high yielding synthesis of a-chloro ketones is described, involving acylation of Grignard and organolithium reagents with N-methoxy-N-methylchloroacetamide. The efficiency of the process is further enhanced by recycling N,O-dimethylhydroxylamine.

Synthesis of .alpha.-chloro or fluoro ketones

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Westfield, NJ, United States of America

Ulf H Dolling