http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-103694237-B
Outgoing Links
Predicate | Object |
---|---|
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D211-86 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D211-76 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D211-88 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D211-76 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 |
filingDate | 2014-01-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2016-03-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 2016-03-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | CN-103694237-B |
titleOfInvention | Preparation method and key intermediate of anticoagulant drug Apixaban |
abstract | The invention provides a preparation method and key intermediate of anticoagulant apixaban, the method comprising the following steps: (1). Using N-(4-nitrophenyl)-3,3-dichloro -2-oxopiperidine (compound 15) was used as the starting material, and compound 16 was obtained through reduction reaction; (2). Compound 16 was acylated with 5-bromopentanoyl chloride to obtain compound 17; (3). Compound 17 was obtained in Compound 18 is obtained by reacting in the presence of a cyclic condensation agent; (4). Compound 18 reacts with a base to obtain Compound 19; (5). Compound 19 reacts with Compound 4 to obtain Compound 6; (6). Compound 6 is finally subjected to Ammonium solution to Apixaban. Compared with the prior art, the present invention has the advantages of: 1) the synthetic route is more reasonable; 2) avoiding the use of expensive or toxic and irritating reagents; 3) the reaction by-products are few and easy to purify; 4) the total yield 5) the reaction is suitable for industrialized production. The reaction scheme is shown in the following formula. |
isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-113912598-A |
priorityDate | 2014-01-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 24.