http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2009101634-A2

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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
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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

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