Merck Sharp + Dohme Corp.

Mark Weisel

Nobuyoshi Yasuda

Jianguo Yin

Zhijian Liu

Matthew Franklin Hagan

The present invention relates to processes for the preparation of N-protected (2S,5R)-6-hydroxy-7-oxo-N-piperidin-4-yl-1,6-diazabicyclo[3.2.1]octane-2-carboxamide intermediates. 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.

Process for preparing beta-lactamase inhibitor hydroxylurea intermediates

An inertion funnel includes a hollow ring with an attachment point on an outside edge and a plurality of output apertures on the inside edge allows for an even flow of gas around the circumference of the ring and through the output apertures into a filter funnel below. The attachment point allows the attachment of a hose or other fitting through which gas flows into the hollow ring, which rests above and around the opening of the filter funnel. On the inside of the ring, an angled downward opening allows gas to flow out of the ring and into the filter funnel. Uniformly distributed around the opening are vanes that direct the flow of gas from the ring into the filter funnel below.

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Stewartsville, NJ, United States of America

Mark Weisel