http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-113651735-B

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classificationCPCAdditional http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C2602-08
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C315-04
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C45-46
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C315-02
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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C315-04
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C317-22
filingDate 2021-08-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2022-04-15-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2022-04-15-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-113651735-B
titleOfInvention Preparation method of HIF-2 alpha inhibitor PT2385
abstract The invention relates to a preparation method of a HIF-2 alpha inhibitor PT 2385. The method takes p-difluorobenzene as raw materialThe intermediate II is subjected to Friedel-crafts reaction with 3-chloropropionyl chloride to generate an intermediate II, the intermediate II is subjected to substitution reaction with sodium methyl mercaptide to generate an intermediate III, the intermediate VII is obtained through oxidation reaction, reduction reaction and two-step substitution reaction, the intermediate VIII is obtained through oxidation reaction, the intermediate VIII is reacted with n-butylamine to obtain a compound IX, the compound IX is subjected to fluorination reaction and hydrolysis reaction to obtain an intermediate X, and finally the final product PT2385 is obtained through asymmetric reduction reaction. Compared with the existing synthesis method, the process route provided by the invention has obvious advantages: the raw materials are cheap and easy to obtain, the operation is simple and convenient, the reaction steps are few, the total yield reaches 47.6 percent, multi-step high-temperature reaction is avoided, and the industrial production is easy to realize. 。
priorityDate 2021-08-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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