http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-106496179-A

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filingDate 2016-10-19-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6b3ab5d7e0888449a1ea5f49f8cd627a
publicationDate 2017-03-15-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-106496179-A
titleOfInvention A kind of synthetic technique of ticagrelor intermediate
abstract The invention discloses a synthesis process of a ticagrelor intermediate, which is characterized in that the synthesis process comprises the following steps: 1) under acidic conditions, reacting benzaldoxime with cyclopentadiene to obtain the formula I 2) Under the catalysis of osmium tetroxide, hydrogen peroxide oxidizes the compound shown in formula I to obtain the compound shown in formula II; 3) under the catalysis of p-toluenesulfonic acid, the compound shown in formula II is reacted with acetone to obtain formula The compound shown in III; 4) in the presence of a base, the compound shown in formula III is reacted with 2-bromoethanol to obtain the compound shown in formula IV; 5) the compound shown in formula IV is reduced to obtain the ticagrelor intermediate . The raw materials of the method provided by the invention are cheap and easy to obtain, and the production cost is reduced; no need to use chiral raw materials, the cycloaddition reaction enables to obtain high stereoselective products, the steps are short, and the reaction yield is also particularly high, which is the advantage of ticagrelor. Synthesis offers new avenues.
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Total number of triples: 33.