The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
May. 14, 2013
Filed:
Oct. 13, 2011
Varun Rawat, Noida, IN;
Pandurang Vilasrao Chouthaiwale, Pune, IN;
Vilas Bhiku Chavan, Pune, IN;
Gurunath Mallappa Suryavanshi, Pune, IN;
Arumugam Sudalai, Pune, IN;
Varun Rawat, Noida, IN;
Pandurang Vilasrao Chouthaiwale, Pune, IN;
Vilas Bhiku Chavan, Pune, IN;
Gurunath Mallappa Suryavanshi, Pune, IN;
Arumugam Sudalai, Pune, IN;
Council of Scientific & Industrial Research, New Delhi, IN;
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=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.