(Chemical Equation Presented) A practical and scaleable synthesis of the γ-secretase inhibitor 1 is reported. The inhibitor consists of a central trisubstituted cyclohexane core with appended propionic acid, 2,5-difluorophenyl, and 4-chlorophenylsulfonyl
Scott, Jeremy P.,Lieberman, David R.,Beureux, Olivier M.,Brands, Karel M. J.,Davies, Antony J.,Gibson, Andrew W.,Hammond, Deborah C.,McWilliams, Chris J.,Stewart, Gavin W.,Wilson, Robert D.,Dolling, Ulf-H.
p. 4149 - 4155
(2008/02/05)
The conformational bias of aryl, arylsulfonyl geminally substituted tertiary carbon centers: Applications in substrate-based stereocontrol
Intramolecular nitrile oxide-olefin cycloaddition to form hexahydrobenzisoxazole 14, which engenders a phenylsulfonyl, 2,5-difluorophenyl geminally substituted carbon substructure, proceeds with up to 99% ds. A rationalization of the high level of substra
Scott, Jeremy P.,Mullens, Peter R.,Brewer, Sarah E.,Brands, Karel M.J.,Chilenski, Jennifer R.,Davies, Antony J.,Gibb, Andrew D.,Lieberman, David R.,Oliver, Steven F.,Dolling, Ulf-H.
p. 1806 - 1810
(2008/02/05)
The new cyclohexylpropionic sulfone
Novel sulphones of formula I are disclosed: The compounds modulate the processing of amyloid precursor protein by gamma-secretase, and hence are useful in the treatment or prevention of Alzheimer's disease.
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Page/Page column 20-21
(2008/06/13)
Novel cyclohexyl sulphones
Novel sulphones of formula I are disclosed: The compounds modulate the processing of amyloid precursor protein by gamma-secretase, and hence are useful in the treatment or prevention of Alzheimer's disease.
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(2008/06/13)
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