http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-109020912-B
Outgoing Links
| Predicate | Object |
|---|---|
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D261-20 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D261-20 |
| filingDate | 2018-07-26-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2020-08-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2020-08-18-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CN-109020912-B |
| titleOfInvention | Synthesis process of C-Fos/AP-1 inhibitor |
| abstract | The invention belongs to the technical field of drug synthesis, and particularly relates to a synthesis process of a C-Fos/AP-1 inhibitor, which starts from cheaper raw materials of 2, 4-dimethoxybenzoic acid and 2-methoxypropionic acid, prepares acyl chloride by thionyl chloride, catalyzes a Friedel-crafts acylation reaction by aluminum trichloride to obtain a coupled product, then reacts for 30 minutes at 160 ℃ by using pyridine hydrobromide and sodium chloride to complete the reaction of demethylation and lactone ring formation in one step, the obtained product can be directly used for the next reaction without purification, introduces cyclopentyl through nucleophilic substitution, prepares methyl ester after opening the lactone ring, introduces benzisoxazole groups through nucleophilic substitution after purification, and removes protective groups to obtain a final product T5224; the method has the advantages of short route, purification only requiring three steps of Friedel-crafts acylation, lactone ring opening and introduction of benzisoxazolyl in the middle, low cost of raw materials, short reaction time of the process route and suitability for industrial production. |
| priorityDate | 2018-07-26-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 104.