http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-3543237-A1

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filingDate 2018-03-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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publicationDate 2019-09-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-3543237-A1
titleOfInvention Simple preparation method for avibactam intermediate
abstract The present invention discloses a simple process for preparing an intermediate for avibactam. In the invention, a compound of Formula III as the raw material is hydrolyzed in an alkaline condition, then acidized to prepare a compound of Formula IV, and the resulting compound of formula IV and a solid phosgene or diphosgene are concurrently subjected to the urea cyclization and the chloroformylation reaction in the presence of an organic base and a catalyst to obtain a compound of formula V, and then the compound of formula V is amidated to obtain the final product (II). In the present invention, a "one-pot" method is adopted for urea cyclization, chloroformylation, and amidation reaction, and the intermediate products do not need post-treatments such as separation and purification. The present invention uses an inexpensive and easily accessible raw material; the process is simple; the operability is strong; no specific protection agent or carbonylation reagent is required; the reaction has a high atom economy and a low cost. Besides, the production process is green and environment-friendly; the resulting product (II) has a high purity and yield, which facilitates cost reduction and green production of avibactam (I).
isCitedBy http://rdf.ncbi.nlm.nih.gov/pubchem/patent/KR-20190082194-A
priorityDate 2017-10-18-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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