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Synthesis of a γ-Secretase Inhibitor
H. Li*, R. Xu*, D. Cole, J. W. Clader, W. J. Greenlee, A. A. Nomeir, L. Song, L. Zhang
Merck Research Laboratories, Kenilworth, USA
21 December 2010 (online)
Both β- and γ-secretase are important targets for the treatment of Alzheimer’s disease because of their central role in the production of β-amyloid peptide (Aβ). Extracellular accumulation of Aβ results in the formation of characteristic plaques leading to neurodegeneration, dementia, and death. The cis-2,6-disubstituted morpholine L is a lead γ-secretase inhibitor.