1416134-44-5Relevant articles and documents
Method for synthesizing avibactam intermediate compound
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, (2019/11/20)
The invention relates to a method for synthesizing an avibactam intermediate compound. The specific synthetic route of the method is as described in the specification. According to a technical schemeof the invention, no precious metal catalyst is used, and no heavy metal pollution is produced; high yield and low cost are realized; and the method is mild in reaction condition and friendly to environment, and can realize industrial production.
B-LACTAMASE INHIBITOR AND APPLICATION THEREOF
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, (2018/03/07)
The present invention relates to a compound of Formula (I)-(IV) useful as β-lactamase inhibitor, a pharmaceutically acceptable salt, ester, solvate or stereoisomer thereof, wherein R1, R2, M and ring A have definitions as those in the specification. The present invention further relates to methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and uses of these compounds. For example, the compounds of the present invention can be used as β-lactamase inhibitors, for treatment and/or prophylaxis of diseases caused by bacterial infections, solving drug-resistance problems caused by β-lactamases, especially bacterial drug-resistant diseases caused by type B metallo-β-lactamases.
Development of a Manufacturing Route to Avibactam, a β-Lactamase Inhibitor
Ball, Matthew,Boyd, Alistair,Ensor, Gareth J.,Evans, Matthew,Golden, Michael,Linke, Simon R.,Milne, David,Murphy, Rebecca,Telford, Alex,Kalyan, Yuriy,Lawton, Graham R.,Racha, Saibaba,Ronsheim, Melanie,Zhou, Shao Hong
, p. 1799 - 1805 (2016/10/31)
Process development work to provide an efficient, robust, and cost-effective manufacturing route to avibactam, a β-lactamase inhibitor is presented herewith. Aspects of this optimization work include the counterintuitive introduction of a protecting group to effect a difficult urea formation and the use of controlled feed hydrogenation conditions to facilitate an elegant one pot debenzylation and sulfation reaction. Overall, the commercial process delivers avibactam in much improved yield with significant reduction in the environmental footprint.