http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-109748885-B
Outgoing Links
Predicate | Object |
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classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D295-205 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 |
filingDate | 2017-11-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2020-08-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 2020-08-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | CN-109748885-B |
titleOfInvention | Ceritinib intermediate and preparation method of ceritinib |
abstract | The invention relates to a ceritinib intermediate and a preparation method of ceritinib. The ceritinib intermediate compound is 4-isopropoxy-5-guanidino-2-N-substituted piperidine-4-yl toluene nitrate (VII), and the preparation method comprises the steps of carrying out substitution reaction on 2-nitro-4, 5-dimethyl chlorobenzene and isopropanol in the presence of alkali to generate a compound III, then condensing with halogenated acetaldehyde acetal, and reducing ammonia-ammonium chloride-sodium borohydride to form a ring to obtain a compound IV; obtaining a compound V through amino protection; then catalytically hydrogenating and reducing nitro to amino in a solvent to obtain a compound VI; and (3) reacting the compound VI with cyanamide to prepare a compound VII. The invention also provides a method for preparing ceritinib by using the compound VII. The method has the advantages of cheap and easily obtained raw materials, simple and convenient operation, high reaction selectivity of each unit, small amount of waste water and environmental protection. |
priorityDate | 2017-11-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 166.