http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-109734661-B
Outgoing Links
| Predicate | Object |
|---|---|
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D215-48 |
| filingDate | 2018-09-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2021-12-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2021-12-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CN-109734661-B |
| titleOfInvention | Synthetic method of lenvatinib |
| abstract | The invention provides a synthetic method of lenvatinib. Firstly, 4-cyano-3-hydroxyaniline is used as an initial raw material, is methylated by dimethyl carbonate, is reacted and oximated by glucuronic acid at room temperature, forms 6-cyano-7-methoxy-4-quinolinone by ring closure under PPA condition, forms 6-cyano-7-methoxy-4-chloroquinolinone under the action of thionyl chloride, and synthesizes an intermediate 6-formamido-7-methoxy-4-chloroquinoline in lenvatinib through cyano hydrolysis under acidic condition. Then 4-hydroxy-2-chloroaniline and cyanogen bromide are reacted at a low temperature to form 4-hydroxy-2-chlorocyanamide, and the 4-hydroxy-2-chlorocyanamide and bromopropane are subjected to a Ritter reaction to synthesize another key intermediate 1- (2-chloro-4-hydroxyphenyl) -3-cyclopropyl urea of the lenvatinib. And finally, performing alkylation reaction on the two intermediates 6-formamido-7-methoxy-4-chloroquinoline and 1- (2-chloro-4-hydroxyphenyl) -3-cyclopropylurea in an alkaline environment to prepare the lenvatinib. The scheme has the advantages of mild reaction conditions, no virulent reagent, environmental friendliness and the like. |
| priorityDate | 2018-09-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 73.