Merck Sharp + Dohme Corp.

Michael Shevlin

John Y L Chung

Peter Emmanuel Maligres

John S Wai

Peter D Williams

Feng Xu

Shankar Venkatraman

Wayne J Thompson

Helen Y Chen

Dai-Shi Su

Dongfang Meng

James Francis Dropinski

Mark W Embrey

Zhiguo Jake Song

Timothy A Blizzard

Artis Klapars

John Limanto

Sookhee Nicole Ha

Jeremy Peter Scott

Thorsten E Fisher

Timothy Allen Blizzard

Tao Pei

Nelo R Rivera

Edward C Sherer

Jingjun Yin

Jason Eugene Imbriglio

Aaron J Moment

Ian Mangion

Zhijian Liu

Bryon Ladd Simmons

David C Dubost

Jeffrey Donald Hermes

Jane Yang Wu

Candido Gude

Neil A Strotman

Alan Michael Hyde

Richard C A Isaacs

Dietrich P Steinhuebel

Amude Kassim

Daniel A DiRocco

Susan L Zultanski

Seongkon Kim

Richard G Ball

Timothy James Wright

Matthew L Maddess

Ralph Calabria

Aaron M Dumas

Rebecca T Ruck

Eric J Choi

Mikhail Reibarkh

Rose Mathew

Tyler A Davis

Yi Ning Ji Chen

Louis Charles Campeau

Christopher J Mortko

Neil Campbell

Sarah L Trice

John YL Chung

Venugopal Gudipati

Matthew Maddess

The present invention relates to processes for the preparation of N-protected 4-((2S,5R)-5-((benzyloxy)amino)piperidine-2-carboxamido)piperidine-1-carboxylates. Such compounds have application in the preparation of beta-lactamase inhibitors such as 7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamides and esters, in particular, the beta lactamase inhibitor, (2S,5R)-7-oxo-N-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also encompasses intermediates useful in the disclosed processes and methods for their preparation.

Methods of preparing hydroxylamine derivatives useful in the preparation of anti-infective agents

The present invention is directed to a process for making Chloro-Substituted Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).

Process for making chloro-substituted nucleoside phosphoramidate compounds

Compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein X, X, Y, R, R, Rand Rare defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset or progression of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se (or as hydrates or solvates thereof) 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. Processes for making compounds of Formula I and intermediates thereof are also described.

HIV integrase inhibitors

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

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Middlesex, NJ, United States of America

Michael Shevlin