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filingDate 2018-03-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2020-06-16-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c69b2f56b0e5e3143c5c0243c02c762d
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publicationDate 2020-06-16-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber RU-2713400-C9
titleOfInvention Method of producing 5r-[(benzyloxy)amino]piperidine-2s-carboxylate and oxalates thereof
abstract FIELD: chemistry. n SUBSTANCE: invention relates to methods of producing 5R-[(benzyloxy)amino]piperidine-2S-carboxylate and its oxalate, where L-glutamic acid or sodium salt of L-glutamic acid as a starting material is reacted with monochloroacetic acid under alkaline conditions by a substitution reaction to obtain N-carboxymethyl-L-glutamic acid (compound III), then compound III is reacted with an alcohol in the presence of an acid reagent through an esterification reaction to obtain a diester of N-alkoxycarbonylmethyl-L-glutamic acid (compound IV), under action of a strong base, compound IV is subjected to intramolecular condensation to form a ring, hydrolysis with decarboxylation and esterification to obtain piperidin-5-one-2S-carboxylate (compound V), compound V is condensed with a hydrochloride salt of benzyloxyamine in the presence of an alkali to obtain 5-[(benzyloxy)imino]piperidine-2S-carboxylate (compound VI), compound VI is subjected to reduction and chiral separation to obtain 5R-[(benzyloxy)amino]piperidine-2S-carboxylate (IIb) oxalate, which is then neutralized to obtain 5R-[(benzyloxy)amino] piperidine-2S-carboxylate (IIa). Obtained 5R-[(benzyloxy)amino]piperidine-2S-carboxylate (IIa) or oxalate 5R-[(benzyloxy)amino]piperidine-2S-carboxylate (IIb) is used to obtain avibactam (I). n EFFECT: use of an inexpensive and readily available starting material which is characterized by high selectivity and is environmentally friendly and environmentally friendly during the production process. n 10 cl, 3 dwg, 17 ex
priorityDate 2017-08-18-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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