http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-105622380-B

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classificationCPCAdditional http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D209-48
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C45-63
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C49-80
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C49-84
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C49-84
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C45-63
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D209-48
filingDate 2014-10-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2020-06-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2020-06-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-105622380-B
titleOfInvention A kind of preparation method of aprestel and intermediate thereof
abstract The present invention provides a preparation method and an intermediate of Apremilast. The present invention provides a kind of Apremilast intermediate represented by formula III, and the compound of formula III is sequentially reacted with methyl sulfinate, reductive amination, salt-forming with asymmetric acid, and 3-acetamido Reaction of phthalic anhydride yields Apst. The method for synthesizing aprestel provided by the invention can avoid using n-butyllithium n-hexane solution, not only reduces the production cost, but also facilitates the operation process, and greatly improves the safety in industrial production, and more For continuous production suitable for industrialization. The yield of the method for preparing 3-acetamidophthalic anhydride provided by the present invention is increased to 81%, the yield is relatively high, and the method is extremely suitable for the industrialized production of Apstar.
priorityDate 2014-10-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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