111939-08-3Relevant academic research and scientific papers
COMPOUNDS THAT INHIBIT PROTEASE CATHEPSIN S AND HCV REPLICATION
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Page/Page column 30-31, (2009/05/30)
The present invention is directed to compounds that have the dual property of acting as cathepsin S inhibitors and of inhibiting HCV replication. Such compounds are therefore useful in treating disease states that include hepatitis C, Alzheimer's disease,
Asymmetric desymmetrization of meso-pyrrolidine derivatives by enantiotopic selective C-H hydroxylation using (salen)manganese(III) complexes
Punniyamurthy,Katsuki, Tsutomu
, p. 9439 - 9454 (2007/10/03)
Chiral (salen)manganese(III) complexes 1 catalyzed the asymmetric desymmetrization of N-protected meso-pyrrolidine derivatives 3, 6-8, 15 and 18 by enantiotopic selective C-H oxidation in the presence of terminal oxidant iodosylbenzene. The oxidation occurred chemoselectively at the carbon α to the nitrogen atom to afford optically active hydroxypyrrolidine derivatives 9, 11, 13, 16, 19 and 21 that were further oxidized to chiral lactams with Jones reagent. The N-protecting groups of the meso-pyrrolidine derivatives have notable effect on the enantioselectivity.
Oxazaborolidine catalysed enantioselective reduction of cyclic meso-imides
Ostendorf, Martin,Romagnoli, Romeo,Pereiro, Isabel Cabeza,Roos, Eric C.,Moolenaar, Marinus J.,Speckamp, W. Nico,Hiemstra, Henk
, p. 1773 - 1789 (2007/10/03)
Full details of the enantioselective reduction of cyclic meso-imides catalysed by an enantiopure oxazaborolidine derived from (S)-α,α-diphenylprolinol are reported. Treatment of the imides with borane in the presence of the catalyst led to a mixture of cis- and trans-hydroxylactams and, after subsequent ethanolysis, to the corresponding diastereomerically pure trans-ethoxylactams. The enantiomeric excesses were shown to be 68-94% by HPLC-determination. One example, in which the ethoxylactam was converted into the benzenesulfonyllactam, could be crystallized to >99% enantiomeric purity.
