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Synfacts 2007(10): 1009-1009  
DOI: 10.1055/s-2007-968955
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New York

Synthesis of a γ-Secretase Inhibitor

Contributor(s): Philip Kocienski
A. J. Davies*, J. P. Scott*
Merck Sharp & Dohme Research Laboratories, Hoddesdon, UK and Merck Research Laboratories, Rahway, USA
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Publikationsverlauf

Publikationsdatum:
07. November 2007 (online)

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Significance

γ-Secretase is an enzyme responsible for the accumulation of the Ab protein associated with Alzheimer’s disease. This efficient scalable synthesis of a γ-secretase inhibitor (five steps, 58% overall) features a crystallization-driven conversion of a mixture of tertiary alcohols into the desired trans-F. For another large-scale synthesis of the same inhibitor by the Merck group, see: J. Org. Chem. 2007, 72, 4149 and Synfacts 2007, 1010.