http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-111138409-B
Outgoing Links
Predicate | Object |
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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 |
Incoming Links
Total number of triples: 138.