Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Solvias Ag

Intervet International B.v.

Nelo R Rivera

Yi Xiao

Nobuyoshi Yasuda

Birgit Kosjek

Joseph D Armstrong, Iii

Thorsten Rosner

Paul Gerard Bulger

Yongkui Sun

Shane W Krska

Felix Spindler

Helen Y Chen

Timothy A Blizzard

Kenneth M Wells

Kevin Michael Belyk

Chunhua Yang

Sookhee Nicole Ha

Timothy Allen Blizzard

Mark S Jensen

Yaling Wang

Jason Eugene Imbriglio

Ian Mangion

Candido Gude

Jane Yang Wu

Jeffrey Donald Hermes

Michael Palucki

Michael Shevlin

Seongkon Kim

Christopher Joseph Welch

Rebecca T Ruck

Christopher J Mortko

Eugenia Njolito

Christophe Malan

Andrew M Clausen

Bramhananda N Reddy

Sreenivas Mende

Yadagiri R Pendri

Joseph Armstrong

A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: employing dynamic kinetic resolution (DKR). The DKR process involves an enzymatic enantioselective amination reaction catalyzed by transaminases. The process can be used to manufacture key intermediates in the preparation of poly (ADP-ribose) polymerase (PARP) inhibitors which may be useful for the treatment of cancer.

Biocatalytic transamination process

This invention relates to a resolution process for the preparation of fluoroleucine alkyl esters.

Process for preparing fluoroleucine alkyl esters

Substituted bicyclic beta-lactams of Formula I: (I), are &#x3b2;-lactamase inhibitors, wherein a, X, Rand Rare defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with &#x3b2;-lactam antibiotics. In particular, the compounds can be employed with a &#x3b2;-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to &#x3b2;-lactam antibiotics due to the presence of the &#x3b2;-lactamases.

&#x3b2;-lactamase inhibitors

An efficient synthesis for the preparation of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1 -carboxamide, by coupling (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride with 1,1'-carbonyldiimidazole ('CDI') as carbonyl source; and an efficient preparation of the potassium salt of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide.

Process for the preparation of CGRP antagonist

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

The invention discloses a novel process for the preparation of enantiomerically enriched mixtures of compounds of structural formula I which are useful intermediates in the synthesis of &agr;v&bgr;3 integrin receptor antagonists

Process to chiral integrin antagonist beta-amino acid intermediate

A novel process is provided for the preparation of 3-(5,6,7,8-tetrahydro-&lsqb;1,8&rsqb;-naphthyridin-2-yl)-propylamine which is useful in the synthesis of &agr;v integrin receptor antagonists. Also provided are useful intermediates obtained from the process.

Process and intermediates to a tetrahydro-&lsqb;1,8&rsqb;- Naphthyridine

A novel process is provided for the preparation of imidazolidinone &agr;v&bgr;3/&agr;v&bgr;5 integrin antagonists, and the useful intermediates obtained therein. These compounds are antagonists of &agr;v&bgr;3/&agr;v&bgr;5 integrin receptors and thus useful for inhibiting bone resorption and treating and preventing osteoporosis. Also disclosed is 3-&lcub;2-oxo-3-&lsqb;3-(5,6,7,8-tetrahydro-&lsqb;1,8&rsqb;naphthyridin-2-yl)-propyl&rsqb;imidazolidin-1-yl&rcub;-3(S)-(6-methoxy-pyridin-3-yl)-propionic acid in the form of a hemihydrate.

Process and intermediates for the preparation of imidazolidinone &agr;v integrin antagonists

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Scotch Plains, NJ, United States of America

Nelo R Rivera