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Synfacts 2006(9): 0867-0867  
DOI: 10.1055/s-2006-942054
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New York

Synthesis of a γ-Secretase Inhibitor

Contributor(s): Philip Kocienski
J. P. Scott*, S. F. Oliver*, K. M. J. Brands, S. E. Brewer, A. J. Davies, A. D. Gibb, D. Hands, S. P. Keen, F. J. Sheen, R. A. Reamer, R. D. Wilson, U.-H. Dolling
Merck Sharp & Dohme Research Laboratories, Hoddesdon, UK and Merck Research Laboratories, Rahway, USA
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Publication History

Publication Date:
23 August 2006 (online)

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Significance

(-)-I is a γ-secretase inhibitor under development for the treatment of Alzheimer’s disease. Multikilo quantities were prepared in 13% overall yield by the route depicted. No chromatography was required. The key step is a highly stereo­selective intramolecular nitrile oxide-olefin cycloaddition leading to D.