http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-111138409-B

Outgoing Links

Predicate Object
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D295-088
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D333-56
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D333-56
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D295-088
filingDate 2020-01-03-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2021-02-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2021-02-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-111138409-B
titleOfInvention Preparation method of raloxifene hydrochloride and intermediate thereof
abstract The invention discloses a preparation method of raloxifene hydrochloride and an intermediate thereof, which comprises the steps of preparing a raloxifene hydrochloride precursor (intermediate 2) from 1- {4- [2- (piperidine-1-yl) ethoxy ] phenyl } -2- (2-mercapto-4-methoxyphenyl) ethanone (intermediate 1) and 4-methoxybenzoyl halide, demethylating and protecting, and preparing raloxifene hydrochloride from hydrochloric acid; intermediate 1 is formed from intermediate 3 (1- {4- [2- (piperidin-1-yl) ethoxy ] phenyl } -2- (2-benzylsulfanyl-4-methoxyphenyl) ethanone) debenzylated in trifluoroacetic acid to oxidize (3-methoxyphenyl) benzyl sulfide to the sulfoxide compound, which is then reacted with 1- [2- (4-ethynylphenoxy) ethyl ] piperidine to form intermediate 3; the method has the advantages of mild reaction conditions, less side reactions, high yield, cheap and easily-recycled reagent raw materials, and suitability for industrial large-scale production.
priorityDate 2020-01-03-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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