http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RU-2609006-C2
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_f5c780fbec7c920affdd794aec285892 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-519 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P35-00 |
| filingDate | 2013-08-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2017-01-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_889f7f4998ed7b7c48c708c75c47c1f9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8bd74b212f8bf6457d664a9c8f4cd130 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ded7b913492d37eef6bbae6bf2eedf88 |
| publicationDate | 2017-01-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | RU-2609006-C2 |
| titleOfInvention | Process for preparation of pemetrexed and lysin salt thereof |
| abstract | FIELD: chemistry. n SUBSTANCE: invention relates to a method of producing pemetrexed salt, having general formula I, where B+ denotes Na+ or protonated lysine, and having anticancer activity. Method includes following stages: a) reaction of 4-(2-(2-amino-4,7-dihydro-4-oxo-3H-pyrrolo(2,3-d)pyrimidin-5-yl)ethyl)benzoic acid (2) with diethyl-L-glutamate hydrochloride in presence of a binding agent to produce pemetrexed diethyl ester (3); b) hydrolysis of pemetrexed diethyl ester (3) to pemetrexed acid (5); c) forming salts with a base selected from NaOH or lysine, to produce corresponding pemetrexed salt. Method is characterized by that, that at step a) acid (2) is pre-converted in situ into corresponding sodium carboxylate or morpholine carboxylate, which can be separated or directly react, wherein used reaction solvent consists of water-alcohol mixture of solvents, where alcohol is selected from methanol, ethanol, isopropanol and n-propanol, and an intermediate compound of pemetrexed diethyl ester (3) is directly precipitated from reaction mixture with purity >98 %. Invention also relates to a (bi)lysine salt of N-[4-[2-(2-amino-4-oxo-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid (pemetrexed) of formula (1), which is more stable, synthesis method thereof and a pharmaceutical composition containing said salt. n EFFECT: method enables to directly precipitate intermediate pemetrexed diethyl ester into a reaction mixture, obtaining said ester with high purity. n 15 cl, 9 dwg, 3 tbl, 20 ex |
| priorityDate | 2012-08-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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