138457-47-3Relevant academic research and scientific papers
Chemo- and Site-Selective Alkyl and Aryl Azide Reductions with Heterogeneous Nanoparticle Catalysts
Udumula, Venkatareddy,Nazari, S. Hadi,Burt, Scott R.,Alfindee, Madher N.,Michaelis, David J.
, p. 4423 - 4427 (2016/07/12)
Site-selective modification of bioactive natural products is an effective approach to generating new leads for drug discovery. Herein, we show that heterogeneous nanoparticle catalysts enable site-selective monoreduction of polyazide substrates for the generation of aminoglycoside antibiotic derivatives. The nanoparticle catalysts are highly chemoselective for reduction of alkyl and aryl azides under mild conditions and in the presence of a variety of easily reduced functional groups. High regioselectivity for monoazide reduction is shown to favor reduction of the least sterically hindered azide. We hypothesize that the observed selectivity is derived from the greater ability of less-hindered azide groups to interact with the surface of the nanoparticle catalyst. These results are complementary to previous Staudinger reduction methods that report a preference for selective reduction of electronically activated azides.
DUAL-ACTION INHIBITORS AND METHODS OF USING SAME
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Page/Page column 121, (2010/11/17)
Provided are compounds, compositions, and methods for treating diseases and conditions wherein an inhibitor of a kinase, such as rho kinase (ROCK), and an inhibitor of one or more of the monoamine transporters, such as NET or SERT, act in concert to improve the condition.
Synthesis, SAR and evaluation of [1,4′]-bipiperidinyl-4-yl-imidazolidin-2-one derivatives as novel CCR5 antagonists
Rotstein, David M.,Gabriel, Stephen D.,Manser, Nicole,Filonova, Lubov,Padilla, Fernando,Sankuratri, Surya,Ji, Changhua,deRosier, Andre,Dioszegi, Marianna,Heilek, Gabrielle,Jekle, Andreas,Weller, Paul,Berry, Pamela
scheme or table, p. 3219 - 3222 (2010/09/18)
Elaboration of our previously disclosed spiropiperidine template led to the development of a series of novel CCR5 antagonists. Results of SAR exploration and preliminary lead characterization are described.
SYNTHESIS OF 1,2-AMINOAZIDES. CONVERSION TO UNSYMMETRICAL VICINAL DIAMINES BY CATALYTIC HYDROGENATION OR REDUCTIVE ALKYLATION WITH DICHLOROBORANES.
Benalil, Aziza,Carboni, Bertrand,Vaultier, Michel
, p. 8177 - 8194 (2007/10/02)
1,2-aminoazides are easily prepared from 1,2-amino alcohols.Catalytic hydrogenation in the presence of palladium on charcoal or reductive alkylation with dichloroboranes afford with good yields unsymmetrically substituted vicinal diamines.
