New compound antibiotic - Avibactam

In the synthetic study of avibactam sodium, the researchers prepared the target product (2S,5R)-7-oxo-N-sulfo-6-sulfooxy-1,6-diazabicyclo[3.2.1]octane-2-carboxamide disodium salt through a series of reactions using (2S,5R)-5-[(benzyloxy)amino]piperidine-2-carboxylic acid ethyl ester oxalate as the starting material. The process involves condensation, hydrolysis, sulfonamidation, deprotection, sulfonylation, and salt exchange to give a final purity of 99.3% and an overall yield of 15.7%. This study provides a new option for the synthesis of impurities in the avibactam sodium process and shows the importance of quality control of avibactam sodium.

On the other hand, regarding the process study for the synthesis of key intermediates of Avibactam, the researchers used L-pyroglutamic acid as starting material, esterification by green reagent ethanol and ethyl protection to avoid the use of high cost and low environmental friendliness of methylene benzene chloride reagent. In addition, the use of thiolide control system to open and expand the ring at low temperature avoided the use of dangerous diazomethane reagents and significantly reduced the generation of enantiomers of non-target configurations. Optimisation of reaction conditions and post-processing operations significantly improved the overall yield to 54%, and no enantiomers below 0.5% were detected by the IA chiral column.

These studies demonstrate that the synthetic processes for avibactam and its related compounds are being optimised to increase yields and purity while reducing environmental impact and production costs. The synthetic studies of impurities in the avibactam sodium process and the synthesis process of key intermediates show the efforts of researchers to ensure the quality and safety of avibactam. These research results are of great significance in understanding and improving the production process of avibactam, which will help to promote its application and development in the clinic.

SZEB supplies of a full set of impurities avibactam, research needs are welcome to consult, go to the official website to view more impurities in detail:www.biotech.com。