http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-104072398-B
Outgoing Links
| Predicate | Object |
|---|---|
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D205-08 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D201-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D205-08 |
| filingDate | 2014-07-03^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2016-02-03^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2016-02-03^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CN-104072398-B |
| titleOfInvention | A kind of method of synthesizing Ezetimibe |
| abstract | The invention discloses a kind of new process of synthesis Ezetimibe (compound 1), belong to organic chemistry medicine synthesis field.The method is with aubepine, and 4-fluoroaniline and Pyroglutaric acid are (3R, 4S) beta-lactam nucleus of main raw material synthesis key intermediate (compound 9), then by the reduction of this compound and hydrolysis, obtains Ezetimibe.Raw material of the present invention is simple and easy to get, synthesis step is few, process stabilizing, the chirality tetra-atomic ring of key intermediate is directly constructed by single step reaction, obtain important intermediate (3R, 4S)-1-(4-fluorophenyl)-3-[(3S)-3-(4-fluorophenyl)-3-carbonyl propyl group]-4-(4-p-methoxy-phenyl)-2-azetidinone (compound 9), in product, targeted enantiomeric ratio is high, post-processing operation is simple, is easy to realize industrialization scale operation. |
| priorityDate | 2014-07-03^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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