Merck Sharp + Dohme Corp.

Steven P Miller

F George Njoroge

Frank W Bennett

Nobuyoshi Yasuda

Ashok Arasappan

Stephane L Bogen

John Fitzgerald Traverse

William W Leong

Shen-Chun Kuo

Marc Poirier

Yong-Li Zhong

John Limanto

Hongbiao Liao

Scott Trzaska

Yonggang Chen

Zhijian Liu

Kenneth Stanley Matthews

Jianshe Kong

Jennifer Albaneze-Walker

Lijun Wang

Thomas J Hunter

Randi M Smith

Azzeddine Lekhal

Patrice Demonchaux

Amadeo Ferreira

William M Leong

Scott T Trzaska

A process for the preparation of N-protected 6-(piperidin-4-ylcarbamoyl)piperidin-3-yl sulfonates of Formula (III): which comprises contacting a lactone of Formula (II): with an azacycloalkylamine of formula (II-Am): followed by contact with a sulfonyl halide of formula (II-Su): R&#x2014;SOW (II-Su) in the presence of tertiary amine base, wherein Pand Pare amine protective groups; k, p and q are 0, 1, or 2, and W, R, R, R, R, R, R, R, and Rare defined herein. Additional embodiments add a series of process steps leading to the synthesis of 7-oxo-1,6-diazabicyclo[3.2.1]octanes suitable for use as &#x3b2;-lactamase inhibitors. 

Process for the preparation of chiral tert-butyl 4-((1R,2S,5R)-6(benzyloxy)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamido)piperidine-1-carb derivatives and (2S,5R)-7-oxo-N-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide

Processes useful for the preparation of a Compound of Formula I: Formula (I). Intermediates useful for the preparation of the compound of Formula I, and processes useful for preparing said intermediates are disclosed. 

Enantio- and stereo specific synthesis of &#x3b2;-amino-&#x3b1;-hydroxy amides

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Monroe, NJ, United States of America

Steven P Miller