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filingDate 2018-05-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5aa49ef8f704ff49ab38b0b94b943ee0
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publicationDate 2019-11-19-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-110467580-A
titleOfInvention Methods for the Resolution of Chiral Enantiomers of the Recinard Axis
abstract The invention belongs to the field of pharmacy, and relates to a kind of Recinade (2-(5-bromo-4-(4-cyclopropylnaphthalene-1-yl)-4H-1,2,4-triazole-3-yl Methods for the resolution of the chiral enantiomers of the thio)acetic acid) axis. The invention adopts cheap and easy-to-obtain quinoline natural products and their derivatives quinine, cinchonine, quinidine or cinchonidine as resolving agents to react with racemates of Recinade in an organic solvent to form salts, Acidification dissociates the salt to obtain optically pure (R)- or (S)-2-(5-bromo-4-(4-cyclopropylnaphthalene-1-yl)-4H-1,2,4-tri oxazol-3-ylthio)acetic acid. The method of the invention is convenient to operate, and the chiral purity ee of the R-configuration Lecinard axis chiral enantiomer can reach 100%, and the total yield can reach more than 90%. The chiral purity ee of the chiral enantiomer of the S-configuration of the Lecinade axis can reach 99.9%, and the total yield is more than 80%. In addition, the used chiral resolution reagent is cheap and easy to obtain, can be conveniently recycled and reused, reduces the separation cost, and is beneficial to industrial production.
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