http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-112279820-B

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classificationCPCAdditional http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-584
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D281-10
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D281-10
filingDate 2020-12-18-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2021-04-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2021-04-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-112279820-B
titleOfInvention Preparation method of 2- (4-methoxyphenyl) -3-hydroxy-2, 3-dihydro-1, 5-benzothiazepine
abstract The invention provides a preparation method of 2- (4-methoxyphenyl) -3-hydroxy-2, 3-dihydro-1, 5-benzothiazepine ketone. The preparation method comprises the steps of synthesizing an intermediate product 1 by taking o-aminothiophenol and methyl propiolate as raw materials, carrying out selective epoxidation to obtain an intermediate product 2, reacting the intermediate product 2 with 4-methoxyphenyl negative ions, carrying out Mitsunobu reaction to obtain an intermediate product 3, and hydrolyzing to obtain a product. In the cyclization process of the intermediate product 1, the Z-structure olefin has small tension, so the yield is high, the subsequent epoxidation is asymmetric epoxidation, the obtained intermediate product 2 has high optical purity and high yield, and the intermediate product 2 and 4-methoxyphenyl anions are SN 2 Reacting, and turning over the configuration at the adjacent position to obtain the product. The whole reaction process does not need to be split, and the total yield of the route is high and economic.
priorityDate 2020-12-18-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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