Predicate |
Object |
assignee |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_bc71b77a52df56752db19cffd0d5a36b http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_444b3f5549d1f978107b93a39030c4c0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_114e4423ec77cbc8dab9d0a98909704e http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_1cf10b3c72c35c93eed18f3c94fe904e http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_7599b47ff01066fb65052e3fcd964011 http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_9dba6bdb55301082d299002228901a4c |
classificationCPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D333-34 |
classificationIPCInventive |
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D333-34 |
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 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_50cd70dd2e8d958ccf81f5274df93003 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fae2ef910d11aba8904968024893f9f9 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_0a088adc61a706ebec2fcb8f8102e7f5 |
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 |