http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2019062561-A1

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filingDate 2018-09-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6a794b57cc7cf1fadb920a1bf909ad0a
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publicationDate 2019-04-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-2019062561-A1
titleOfInvention PROCESSES FOR THE SYNTHESIS OF FIROCOXIB AND INTERMEDIATE THEREOF
abstract The invention relates to methods of synthesizing firocoxib and an intermediate thereof. The synthesis of the first intermediate is carried out by methylation of p-bromopropiophenone or by Friedel-Crafts acylation of bromobenzene, avoiding the use of non-ecological thioethers as raw materials. The second intermediate is directly obtained by sulfonating the first intermediate, the sulfurization reaction and the oxidation reaction being shortened to a one-step reaction. The sulfonation step greatly simplifies the reaction steps, shortens the reaction time, and improves the efficiency thereof. The invention also relates to an N-bromosuccinimide (NBS) catalyst system adopted in the hydroxylation of the second intermediate to directly obtain the intermediate of firocoxib. Such an environmentally friendly process is suitable for large scale production, and the reaction rate is increased. The method for synthesizing firocoxib according to the present invention comprises the method for synthesizing the firocoxib intermediate and makes it possible to prepare firocoxib in a more moderate and more environmentally friendly manner.
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priorityDate 2017-09-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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