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filingDate 1984-02-08-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f04f930a45fea5bbcd50a90d532704bc
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publicationDate 1985-08-29-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber JP-S60166650-A
titleOfInvention Preparation of acylamino-naphthalene derivative
abstract PURPOSE: To obtain the titled compound useful as a carcinostatic agent and a synthetic intermediate therefor in high yield, by reacting a racemic or optically active amino-ester derivative with a methylsulfinyl carbonion, desulfurizing the reaction product, and acylating the desulfurized product. n CONSTITUTION: A racemic or optically active amino-ester derivative of formula I (R is ester residue) is reacted with a methylsulfinyl carbonion in a solvent at -10W+60°C to give a sulfoxide derivative of formula II, which is then reduced with zinc dust, and desulfurized with aluminum amalgam, etc. to afford an amino-ketone derivative of formula III. The resultant compound of formula IIIis then acylated in the presence of an organic base by the conventional method to give the aimed substance of formula IV. The racemic amino-ester derivative is if necessary optically resolved with one of mandelic acid, tartaric acid, dibenzoyltastaric acid, camphorsulfonic acid and 3-bromo-camphorsulfonic acid for use. n COPYRIGHT: (C)1985,JPO&Japio
isCitedBy http://rdf.ncbi.nlm.nih.gov/pubchem/patent/JP-2016041687-A
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