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filingDate 2008-10-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2011-03-03-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber JP-WO2009054240-A1
titleOfInvention Method for producing disulfonic acid compound, asymmetric Mannich catalyst, method for producing β-aminocarbonyl derivative, and novel disulfonate
abstract Hexamethylphosphoramide (HMPA) was added to a reaction vessel containing (R) -1,1′-binaphthyl-2,2′-dithiol and potassium hydroxide. Next, the inside of the container was purged with oxygen, and stirred at 80 ° C. for 5 days under 7 atmospheres of oxygen. After cooling to room temperature, purification was performed to obtain potassium (R) -1,1′-binaphthyl-2,2′-disulfonate. (R) -1,1′-binaphthyl-2,2′-disulfonic acid obtained from this disulfonate and 2,6-diphenylpyridine were stirred in acetonitrile, and then the solvent was distilled off under reduced pressure. Thereafter, magnesium sulfate and distilled CH 2 Cl 2 were added, and the mixture was stirred at room temperature for 30 minutes. This solution was cooled to 0 ° C., benzaldehyde imine in which nitrogen was protected with Cbz, and then acetylacetone were added dropwise over 1 hour, and the mixture was further stirred at 0 ° C. for 30 minutes. As a result, the corresponding β-aminocarbonyl derivative was obtained with a yield of 91% and an enantiomeric excess of 90% ee.
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