Synfacts 2011(1): 0011-0011  
DOI: 10.1055/s-0030-1258975
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart ˙ New York

Synthesis of a γ-Secretase Inhibitor

Contributor(s): Philip Kocienski
H. Li*, R. Xu*, D. Cole, J. W. Clader, W. J. Greenlee, A. A. Nomeir, L. Song, L. Zhang
Merck Research Laboratories, Kenilworth, USA
Further Information

Publication History

Publication Date:
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.