http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-110872258-B

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classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D233-86
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D233-86
filingDate 2018-09-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2021-05-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2021-05-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-110872258-B
titleOfInvention Preparation process of prostate cancer drug enzalutamide
abstract The present invention provides aA process for preparing Enzalutamide as the medicine of prostatic cancer includes such steps as catalytic nucleophilic substitution reaction between N-methyl-4-bromo-2-fluoro-benzamide and 2-aminoisobutyric acid under alkaline condition to obtain 2- (3-fluoro-4- (methylcarbamoyl) phenylamino) -2-methylpropanoic acid, esterification reaction to obtain 2-methoxyethyl 2- ((3-fluoro-4- (methylcarbamoyl) phenyl) amino) -2-methylpropionate, cyclization reaction between said product and 2-trifluoromethyl-4-isothiocyanatobenzonitrile to obtain 4- (3- (4-cyano-3-trifluoromethyl) phenyl) -5, 5-dimethyl-4-oxo-2-thioimidazol-1-yl) -2-fluoro-N-methylbenzamide, enzalutamide. The method provided by the invention overcomes the main defects in the prior art, avoids using high-toxicity reagents such as methyl iodide and the like, and has the advantages of mild reaction conditions, convenience and simplicity in post-treatment, improvement of total yield, reduction of reaction time, reduction of preparation cost, greenness and environmental friendliness, and suitability for industrial mass production.
priorityDate 2018-09-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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