http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-107540677-B
Outgoing Links
| Predicate | Object |
|---|---|
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P3-10 |
| filingDate | 2017-09-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2020-05-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2020-05-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CN-107540677-B |
| titleOfInvention | Sitagliptin derivative or pharmaceutically acceptable salt thereof, and preparation method and application thereof |
| abstract | The invention relates to a sitagliptin derivative or pharmaceutically acceptable salt thereof, and a preparation method and application thereof, and belongs to the technical field of synthesis of pharmaceutical intermediates. In order to solve the problem that the existing chain is easy to generate low-energy conformation, the sitagliptin derivative or pharmaceutically acceptable salt thereof and a preparation method thereof are provided, wherein the method comprises the steps of carrying out coupling reaction on an enamine intermediate and a triazolo [4,3-a ] pyrazine compound in the presence of a coupling agent to obtain the intermediate; and then carrying out deprotection reaction on the intermediate to remove Boc group, and then carrying out cyclization reaction on the intermediate and hydroxylamine hydrochloride to obtain the corresponding sitagliptin derivative or pharmaceutically acceptable salt thereof. According to the invention, the amino group in the flexible chain alkyl in the molecular structure and the carbonyl are cyclized to form a stable five-membered ring structure, so that the low-energy isomerization phenomenon is effectively reduced, the stability of the medicine is improved, and the selectivity and the medication safety are improved. And the synthetic method is simple, and the use of expensive chiral reagents can be avoided. |
| priorityDate | 2017-09-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 86.