http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-2010104193-A2

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filingDate 2010-03-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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publicationDate 2010-09-16-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-2010104193-A2
titleOfInvention Intermediate compound for synthesizing pharmaceutical agent and production method thereof
abstract A production method of an optically active 2-{4-(5-substituted-oxadiazolyl) phenyl}morpholine which is useful as an intermediate for synthesizing a pharmaceutical agent is provided and the method comprises the following steps 1) to 4): 1) reacting a bromophenylmorpholine with a hexacyanoferrate(II) or a hydrate thereof at a temperature of from 110°C to 140°C in a reaction mixture comprising a Na 2 CO 3 , an organophosphorus compound, and a palladium catalyst in a polar aprotic solvent alone or combination of a polar aprotic solvent and other polar aprotic solvent or hydrocarbon solvent to give a cyanophenylmorpholine; 2) reacting the cyanophenylmorpholine with hydroxylamine or hydroxylamine hydrochloride at a temperature of from 10°C to 40°C in an aprotic polar solvent to give a hydroxylamine derivative; 3) reacting the hydroxylamine derivative with an acylation reagent selected from the group consisting of aliphatic acyl halides, aromatic acyl halides, aliphatic acyl anhydrides and aromatic acyl anhydrides; and 4) keeping the mixture obtained after step 3) at a temperature of from 60°C to 140°C to give a 2-{4-(5-substituted-oxadiazolyl) phenyl}morpholine.
priorityDate 2009-03-10-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID245837414
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226531754
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID458394811
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID75269
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID414812530
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID410510807
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226507197
http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID66603983
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID246500792
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID419515358
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http://rdf.ncbi.nlm.nih.gov/pubchem/compound/CID8028
http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID226504283
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID128004883
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID248513353
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http://rdf.ncbi.nlm.nih.gov/pubchem/substance/SID411225871
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Total number of triples: 374.