http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2019127903-A1

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publicationDate 2019-07-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-2019127903-A1
titleOfInvention Simple preparation method for avibactam
abstract Provided is a preparation method for Avibactam, comprising using piperidin-5-one-2S-formate II as a raw material, subjecting same to a condensation reaction with O-protective group hydroxylamine hydrochloride, then performing reduction, chiral separation and hydrolysis under alkaline conditions to obtain 5R-substitutent oxyaminopiperidine-2S-formic acid V; and then subjecting the compound to a cyclic urea forming reaction and a chloroformylation reaction with phosgene, triphosgene or diphosgene, and performing amidation, deprotection, sulphation, and tetrabutylammonium amminiation to form a salt {[(2S,5R)-2-carbamoyl-7-oxo-1,6-diazacyclo[3.2.1]octane-6-yl]oxy}sulfonyltetra-n-butylammonium VII, and finally obtaining Avibactam I by means of ion exchange. The preparation method is simple, is easy to operate, has low raw material price, has low cost, has small amounts of "three wastes" emission, has high atomic utilization rate, is economical and environmentally friendly, and has high yield in each step, being beneficial to the industrial production of Avibactam.
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