http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-109970763-B
Outgoing Links
| Predicate | Object |
|---|---|
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D498-04 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D498-04 |
| filingDate | 2017-12-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2021-10-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2021-10-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CN-109970763-B |
| titleOfInvention | Preparation method of DGAT1 inhibitor |
| abstract | The invention belongs to the technical field of medicines, and particularly relates to a novel preparation method of DGAT1 inhibitor 4-amino-6- (3, 5-dimethyl-4- (3-methyl-1- (2,2, 2-trifluoroethyl) -1H-pyrazol-4-yl) phenyl) -7, 8-dihydropyrimidine [5,4-f ] [1,4] oxazepine-5 (6H) -one-hydrochloride. 3, 5-dimethyl-4- (3-methyl-1- (2,2,2 trifluoroethyl) -1H-pyrazol-4-yl) aniline-hydrochloride is used as a starting material and is subjected to condensation reaction with chloroethyl chloroformate to generate an intermediate 1; the intermediate 1 is alkylated in alcohol and alkali solution and then hydrolyzed to generate an intermediate 2; the intermediate 2 and 4, 6-dichloropyrimidine-5-acyl chloride are subjected to condensation reaction to generate an intermediate 3; after alkylation of the intermediate 3, intramolecular ring closure reaction is carried out to generate an intermediate 4; the intermediate 4 is aminated in dioxane solution of ammonia to generate an intermediate 5; and (5) forming salt in acetone solution of hydrochloric acid to obtain the finished product. All reaction intermediates of the invention are solid and are easy to purify. |
| priorityDate | 2017-12-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 208.