http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-108558838-B

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Predicate Object
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-04
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-04
filingDate 2018-04-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2021-04-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2021-04-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-108558838-B
titleOfInvention Production method of estrogen receptor modulator intermediate
abstract The invention provides a production method of an estrogen receptor modulator intermediate, which comprises the following steps: (1) toluene is taken as a solvent, 5-bromo-4-methyl-1H-indole, a catalyst 1 and 3, 4-dihydropyran are added for heating reaction; (2) stopping reaction, cooling to room temperature, adding sodium bicarbonate water solution, stirring, standing for layering, taking an organic phase, and concentrating the organic phase; (3) mixing the concentrated organic phase with dimethylformamide, adding potassium carbonate, and vacuum-pumping and filling nitrogen for replacement for 3 times by a water pump; (4) adding a catalyst 2 under the protection of nitrogen flow, and adding a cocatalyst; (5) introducing 1-butyne gas to react to obtain the product. The method adopts butyne as a raw material to replace expensive raw materials such as ethynyltrimethylsilane, iodoethane and the like in the prior art, and can be finished by one-step reaction, thereby greatly saving the production cost. The reaction can be completed in one step, the purity of the obtained product is high, and the isomerization of the product is low.
priorityDate 2018-04-20-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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