Merck + Co., Inc.

Solvias Ag

Joseph D Armstrong, Iii

Yi Xiao

Nelo R Rivera

Thorsten Rosner

Yongkui Sun

Shane W Krska

Andrew S Thompson

Felix Spindler

Thomas R Verhoeven

Zhijian Lu

Yuan Cheng

David Askin

Kevin Tyler Chapman

James R Tata

Richard John Varsolona

Subharekha Raghavan

Michel M Chartrain

Joseph Leslie Duffy

Nancy J Kevin

Fengqi Zhang

R Scott Hoerrner

Thomas A Rano

Alan W Douglas

Lisa DiMichele

Steven A King

J Christopher McWilliams

Fred Fleitz

Daniel E Petrillo

Tracy Huening

Brian Anthony Kirk

Robert M Purick

Eugenia Njolito

Jennifer L Keller

Andrew M Clausen

Christophe Malan

The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives wherein the amino group is unprotected. The product chiral beta amino acid derivatives are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of an amine-unprotected prochiral beta-amino acrylic acid or derivative thereof in the presence of a rhodium metal precursor complexed with a chiral mono- or bisphosphine ligand.

Process for the preparation of enantiomerically enriched beta amino acid derivatives

The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives which are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of a prochiral beta amino acrylic acid derivative substrate in the presence of a transition metal precursor complexed with a chiral ferrocenyl diphosphine ligand.

Process for the preparation of chiral beta amino acid derivatives by asymmetric hydrogenation

&ggr;-Hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamide compounds are inhibitors of HIV protease and inhibitors of HIV replication. These compounds are useful in the prevention or treatment of infection by HV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described. These compounds are effective against HIV viral mutants which are resistant to HIV protease inhibitors currently used for treating AIDS and HIV infection.

Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides and uses thereof

The instant invention provides a homologation process for making a zincate homoenolate from a carbon bound enolate zincate, by treating the carbon bound enolate zincate with an alkoxy lithium reagent. The homologation step can be coupled with a homoaldol reaction, as well as with other transmetallation reactions, in a one pot process. The zincate homoenolate is a useful intermediate in the preparation of a variety of different end-products, such as HIV protease inhibitors and renin inhibitors.

Tandem asymmetric transformation process

A biotransformation process for the production of an intermediate used in the chemical synthesis of an antibiotic compound.

Bioconversion of beta keto-ester to (R) hydroxyester

.beta.- or .gamma.-Ketoesters and .beta.- or .gamma.-ketoamides are asymmetrically reduced with a Ru(II)-BINAP derived catalyst at about 40.degree. C. and about 50N/mm.sup.2 of hydrogen in the presence of a strong acid.

Asymmetric hydrogenation of beta- or gamma-ketoesters and beta- or

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Westfield, NJ, United States of America

Joseph D Armstrong, Iii