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Predicate Object
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04
filingDate 2017-12-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2020-05-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2020-05-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-109970733-B
titleOfInvention A kind of simple preparation method of vemurafenib and its analogues
abstract The invention provides a simple and convenient preparation method of vemurafenib and its analogs, which utilizes para-substituted phenylacetaldehyde II and N-[2,4-disubstituted group-3-(cyano-n-propionyl)phenyl] N-Propanesulfonamide III azeotropically removes water under alkali catalysis, and undergoes a condensation reaction, and the obtained condensation product is condensed with a methylidene reagent V (N,N-dimethylformamide acetal or orthoformate triester), and then condensed with Aminocyclization yields vemurafenib or its analogs. Using the method of the invention to prepare vemurafenib has the advantages of low cost, mild process conditions, low operation requirements, short reaction time, high production efficiency, simple and convenient process operation, less waste water generation, green environmental protection, high yield and purity, and has It is beneficial to the green industrial production of vemurafenib. At the same time, the method of the present invention can prepare the vemurafenib analogs, which is of great significance for carrying out the research on the pharmacodynamics of the analogous compounds.
priorityDate 2017-12-28-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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