157394-65-5Relevant academic research and scientific papers
Catalyst-directed diastereoselectivity in hydrogenative couplings of acetylene to α-chiral aldehydes: Formal synthesis of all eight L-hexoses
Man, Soo Bong,Kong, Jong Rock,Krische, Michael J.
supporting information; experimental part, p. 4133 - 4135 (2009/05/27)
(Chemical Equation Presented) Hydrogenative coupling of acetylene to α-chiral aldehydes 1a-4a using enantiomeric rhodium catalysts ligated by (S)-MeO-BIPHEP and (R)-MeO-BIPHEP delivers the diastereomeric products of carbonyl-(Z)-buladienylation 1b-4b and 1c-4c, respectively, with good to excellent levels of catalyst directed diastereofacial selectivity. Diastereomeric L-glyceraldehyde acetonide adducts 1b and 1c were converted to the four isomeric enoates 6b, 8b, 6c, and 8c, representing a formal synthesis of all eight L-hexoses.
Phenylamide and pyridylamide beta-secretase inhibitors for the treatment of alzheimer's disease
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Page/Page column 17, (2008/06/13)
The present invention is directed to phenylamide and pyridylamide derivative compounds of which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind β-secretase in a N-terminal 10s-loop down conformation
Stauffer, Shaun R.,Stanton, Matthew G.,Gregro, Alison R.,Steinbeiser, Melissa A.,Shaffer, Jennifer R.,Nantermet, Philippe G.,Barrow, James C.,Rittle, Kenneth E.,Collusi, Dennis,Espeseth, Amy S.,Lai, Ming-Tain,Pietrak, Beth L.,Holloway, M. Katharine,McGaughey, Georgia B.,Munshi, Sanjeev K.,Hochman, Jerome H.,Simon, Adam J.,Selnick, Harold G.,Graham, Samuel L.,Vacca, Joseph P.
, p. 1788 - 1792 (2008/02/02)
A series of low-molecular weight 2,6-diamino-isonicotinamide BACE-1 inhibitors containing an amine transition-state isostere were synthesized and shown to be highly potent in both enzymatic and cell-based assays. These inhibitors contain a trans-S,S-methyl cyclopropane P3 which bind BACE-1 in a 10s-loop down conformation giving rise to highly potent compounds with favorable molecular weight and moderate to high susceptibility to P-glycoprotein (P-gp) efflux.
A Simple Method for Chelation Controlled Additions to α-Amino Aldehydes
Reetz, Manfred T.,Roelfing, Karin,Griebenow, Nils
, p. 1969 - 1972 (2007/10/02)
BOC- and Cbz-protected α-amino aldehydes derived from amino acids undergo stereoselective addition reactions with alkyl cuprates and manganese reagents, the chelation-controlled adducts being the major diastereomers (generally ds > 90percent).Undesired ra
