http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-111763198-B
Outgoing Links
Predicate | Object |
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classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-12 |
filingDate | 2019-04-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2021-09-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 2021-09-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | CN-111763198-B |
titleOfInvention | Preparation method of 5-substituted cyclopropyl formylaminoindole derivative |
abstract | The invention provides a preparation method of a 5-substituted cyclopropyl formamidoindole derivative, and particularly relates to a preparation method of Tezacaftor. The method comprises the steps of taking 2-nitro-4-fluoro-5-halogenated phenylacetonitrile as an initial raw material, and carrying out ammonia substitution reaction, amidation reaction, dehydration condensation reaction, reduction cyclization reaction-elimination reaction, ring opening substitution reaction and catalytic hydrogenolysis reaction to obtain the Tezacaftor. The method has the advantages of cheap and easily-obtained raw materials, short reaction steps, simple, convenient and safe preparation method, easy realization and low cost; the design of the route of the invention fully combines the inherent characteristics of functional group reaction, ensures that the unit reaction activity of each step is proper and the selectivity is high, and provides essential guarantee for high yield and high purity of the product; the method has the advantages of high atom economy, high product yield and purity, less waste acid and waste water generation amount, environmental protection and suitability for industrial production. |
priorityDate | 2019-04-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 200.