http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-109956941-B

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classificationCPCAdditional http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07B2200-07
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02A50-30
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-08
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-08
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-04
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-551
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-08
filingDate 2017-12-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2020-08-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2020-08-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-109956941-B
titleOfInvention A kind of simple preparation method of avibactam
abstract The invention provides a simple preparation method of avibactam, which takes piperidin-5-keto-2S-formate II as a raw material, undergoes condensation reaction with O-protective group hydroxylamine hydrochloride, and then undergoes reduction, chiral Split, hydrolyze under alkaline conditions to obtain 5R-substituent oxyaminopiperidine-2S-formic acid V; then carry out cyclic ureation, acid chlorination and amidation with phosgene, solid phosgene or diphosgene "one-pot method" Reaction, through deprotection, sulfuric esterification, tetrabutylammonium salt formation to obtain {[(2S,5R)-2-carbamoyl-7-oxo-1,6-diazacyclo[3.2.1] Octane-6-yl]oxy}sulfonyl tetra-n-butylammonium salt VII, and finally obtain Avibactam I through ion exchange. The preparation route of the invention is simple, easy to operate, low in raw material price, low in cost, low in "three wastes" discharge, high in atom utilization rate, economical and environmentally friendly, and high in yield in each step, which is beneficial to the industrialized production of avibactam.
priorityDate 2017-12-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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