Predicate |
Object |
assignee |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_a781cda239b40a46772cf48f4954051e http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_459549086df37b5bed0003502de7e7aa http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_0253061d5166a5a1e2cd696092800442 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_3feedfac4eb71d6354b258319ef882b8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_1379a3d882972ff2e2b42a02df5fdf57 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_85fd4e25e88227037cf7cde642ff3014 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_09af057fad15cc0dfebbe1d55b566fc0 |
classificationCPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 |
classificationIPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 |
filingDate |
2009-02-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dc718c90653455a9e8d27936d950e43a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7e6b96f8a13679c6788788118b21f785 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7d63ba5471240814bcb1c0516b5f99a7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_208a783d0bd72bd529b84b936995ce1a http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3081f85bfd033bbf89c969e923feb85f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_80c059d1d60f899f3eae4878ab853975 |
publicationDate |
2009-08-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber |
WO-2009101634-A2 |
titleOfInvention |
A novel process for the preparation of eszopiclone |
abstract |
The present invention is related to a novel process for the preparation of eszopiclone (II), that comprises the following steps: (a) preparation of zopiclone (I) by reaction of 6-(5-chloropyridin-2-yl)-5-hydroxy-7-oxo- 5,6-dihydropyrrolo[3,4-b]pyrazine-5-one (5-OH-Py) (III) with chloro-carbonyl-4- methyl-piperazine (CMP) free base (IV) or its acid addition salt in the presence of diazabicylo [5.4.0]undec-7-ene (DBU) or a mixture of DBU and other bases; (b) resolution of racemic zopiclone with dibenzoyl-D-tartaric acid in suitable solvent wherein dibenzoyl-D-tartaric acid addition salt of eszopiclone is separated by the addition of a nitrile solvent; (c) optional purification of dibenzoyl-D-tartaric acid addition salt of eszopiclone by dissolution in solvent selected from alcohols, ketones or mixture thereof followed by the precipitation by adding a nitrile solvent; (d) conversion of the dibenzoyl-D-tartaric acid addition salt of eszopiclone to obtain the eszopiclone free base (II) by treating with an alkaline solution; (e) purification of eszopiclone by dissolving in nitrile solvent followed by addition of ketonic solvent. The eszopiclone (II) obtained by the process of the present invention has chiral purity greater than 99.9% and less amounts of organic volatile impurities. The present invention further provides novel crystalline form B of eszopiclone- Dibenzoyl-D-tartarate salt (V) and its preparation. |
isCitedBy |
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-2345654-A1 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-11713296-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8461334-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/JP-2020007252-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2010052475-A1 |
priorityDate |
2008-02-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type |
http://data.epo.org/linked-data/def/patent/Publication |