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Synfacts 2011(9): 0927-0927  
DOI: 10.1055/s-0030-1260913
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of a γ-Secretase Inhibitor

Contributor(s): Philip Kocienski
J. Su*, H. Tang, B. A. McKittrick
Merck Research Laboratory, Kenilworth, USA
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Publication History

Publication Date:
19 August 2011 (online)

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Significance

γ-Secretase inhibitors are of interest for the treatment of Alzheimer’s disease. The key step in the synthesis of the target γ-secretase inhibitor is the stereoselective opening of the epoxide E using a (triarylthio)boron reagent F derived from reaction of BH3 with p-chlorobenzenethiol.