Discovery of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators with robust central efficacy
Herein we describe the discovery of a novel series of cyclopropyl chromane-derived pyridopyrazine-1,6-dione γ-secretase modulators for the treatment of Alzheimer's disease (AD). Using ligand-based design tactics such as conformational analysis and molecul
Pettersson, Martin,Johnson, Douglas S.,Rankic, Danica A.,Kauffman, Gregory W.,Am Ende, Christopher W.,Butler, Todd W.,Boscoe, Brian,Evrard, Edelweiss,Helal, Christopher J.,Humphrey, John M.,Stepan, Antonia F.,Stiff, Cory M.,Yang, Eddie,Xie, Longfei,Bales, Kelly R.,Hajos-Korcsok, Eva,Jenkinson, Stephen,Pettersen, Betty,Pustilnik, Leslie R.,Ramirez, David S.,Steyn, Stefanus J.,Wood, Kathleen M.,Verhoest, Patrick R.
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p. 730 - 743
(2017/04/27)
Regioselective synthesis of bioactive polyheterocycles: Sequential [3, 3] sigmatropic rearrangements of 6-(4-aryloxybut-2-yn-1-yloxy)[1]benzopyran- 2-ones
7a-Methyl-13,13a-dihydro-7aH-furo[3,2-c : 5,4-f']bis-[1]benzopyran-3- ones (4a-d) are regioselectively synthesised in 65-75% yields by the sequential rearrangements of 6-(4-aryloxybut-2-yn-1-yloxy)[1]benzopyran-2- ones (3a-d) in refluxing N,N-diethylanili
Majumdar,Chatterjee
p. 3849 - 3863
(2007/10/03)
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