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assignee http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_bc71b77a52df56752db19cffd0d5a36b
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classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D333-34
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filingDate 2011-10-13-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2013-05-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_56fafb8f678ac941cc7a6cffb4400abd
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e076ad73ad022da023b779ef60e29918
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publicationDate 2013-05-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber US-8440844-B2
titleOfInvention Process for the preparation of β-amino alcohol
abstract A high-yielding enantioselective synthesis of the bioactive (S)—N-(5-chlorothiophene-2-sulfonyl)-β,β-diethylalaniol (7.b.2), a Notch-1-sparing γ-secretase inhibitor metabolite (with EC 50 =28 nM) effective in reduction of Aβ production in vivo, has been realized starting from readily available 3-pentanone. The key steps of the synthesis are proline-catalyzed α-aminooxylation and α-amination of aldehyde; the latter contributing an overall yield of 50-75% and 90-99% enantiomeric excess.
priorityDate 2011-06-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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