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Title:
SIMPLE PREPARATION METHOD FOR AVIBACTAM
Document Type and Number:
WIPO Patent Application WO/2019/127903
Kind Code:
A1
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.

Inventors:
QI YUXIN (CN)
WANG BAOLIN (CN)
XU XIN (CN)
JU LIZHU (CN)
LI XINFA (CN)
Application Number:
PCT/CN2018/078073
Publication Date:
July 04, 2019
Filing Date:
March 06, 2018
Export Citation:
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Assignee:
XINFA PHARMACEUTICAL CO LTD (CN)
International Classes:
C07D211/60; C07D471/08
Domestic Patent References:
WO2012086241A12012-06-28
Foreign References:
CN103649051A2014-03-19
CN106749242A2017-05-31
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CN103649051A2014-03-19
CN105294690A2016-02-03
CN106866668A2017-06-20
US8148540B22012-04-03
US9284273B22016-03-15
US9567335B22017-02-14
CN102834395A2012-12-19
CN103328476A2013-09-25
CN106279163A2017-01-04
CN106565712A2017-04-19
US20100197928A12010-08-05
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Other References:
SENGUPTA, RITOBROTO ET AL.: "Stereochemical Investigation of Conjugate Additions of Carbon- and Heteronucleophiles to Ring-substituted Nitrosocyclohexenes", TETRAHEDRON, vol. 67, no. 43, 28 August 2011 (2011-08-28), pages 8229 - 8234, XP028389475, doi:10.1016/j.tet.2011.08.054
CHEMICAL ABSTRACTS, Columbus, Ohio, US; abstract no. 1192491-61-4
See also references of EP 3766869A4
Attorney, Agent or Firm:
JINAN JINDI INTELLECTUAL PROPERTY AGENCY CO., LTD. (CN)
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