13640-50-1Relevant academic research and scientific papers
Asymmetric Hydrogenation of Racemic Allylic Alcohols via an Isomerization-Dynamic Kinetic Resolution Cascade
Wang, Kun,Niu, Saisai,Guo, Xin,Tang, Weijun,Xue, Dong,Xiao, Jianliang,Sun, Huaming,Wang, Chao
supporting information, p. 3804 - 3809 (2022/02/05)
Prochiral racemic allylic alcohols are converted to enantioenriched chiral alcohols bearing adjacent stereocenters catalyzed by a diamine diphosphine Ru complex in the presence of tBuOK. The protocol features a broad substrate scope (56 examples) and high
Tetralone derivatives are MIF tautomerase inhibitors and attenuate macrophage activation and amplify the hypothermic response in endotoxemic mice
Garai, János,Krekó, Marcell,?rfi, László,Jakus, Péter Balázs,Rumbus, Zoltán,Kéringer, Patrik,Garami, András,Vámos, Eszter,Kovács, Dominika,Bagóné Vántus, Viola,Radnai, Balázs,Lóránd, Tamás
, p. 1357 - 1369 (2021/07/22)
Macrophage migration inhibitory factor (MIF) is a pro-inflammatory cytokine playing crucial role in immunity. MIF exerts a unique tautomerase enzymatic activity that has relevance concerning its multiple functions and its small molecule inhibitors have been proven to block its pro-inflammatory effects. Here we demonstrate that some of the E-2-arylmethylene-1-tetralones and their heteroanalogues efficiently bind to MIF’s active site and inhibit MIF tautomeric (enolase, ketolase activity) functions. A small set of the synthesised derivatives, namely compounds (4), (23), (24), (26) and (32), reduced inflammatory macrophage activation. Two of the selected compounds (24) and (26), however, markedly inhibited ROS and nitrite production, NF-κB activation, TNF-α, IL-6 and CCL-2 cytokine expression. Pre-treatment of mice with compound (24) exaggerated the hypothermic response to high dose of bacterial endotoxin. Our experiments suggest that tetralones and their derivatives inhibit MIF’s tautomeric functions and regulate macrophage activation and thermal changes in severe forms of systemic inflammation.
Basic Anion-Exchange Resin-Catalyzed Aldol Condensation of Aromatic Ketones with Aldehydes in Continuous Flow
Laroche, Benjamin,Saito, Yuki,Ishitani, Haruro,Kobayashi, Shū
supporting information, p. 961 - 967 (2019/05/02)
A general method for the aldol condensation of aromatic ketones with aldehydes was developed under continuous-flow conditions using a commercially available, strongly basic anion-exchange resin (A26) as catalyst. This procedure, in addition to exhibiting a wide substrate scope, promoted carbon-carbon bond formation under mild conditions using a quasi-stoichiometric ratio of starting reagents with good to excellent yields, thereby forming a limited amount of waste and allowing the process to be applied to sequential-flow systems. A proof of concept was developed in the first fully heterogeneously catalyzed two-step flow synthesis of donepezil, which is a blockbuster commercial anti-Alzheimer's drug.
NEW MATERIAL FOR TRANSPORTING ELECTRON AND ORGANIC ELECTROLUMINESCENT DEVICE USING THE SAME
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Paragraph 0119; 0120; 0121, (2016/10/10)
The present invention relates to a novel electron transport material represented by chemical formula 1 and an organic luminescent device using the same. By using the electron transport material, the organic luminescent device which has enhanced luminescent properties and improved electric power consumption by reinforcing driving voltage and inducing increase of power factor can be manufactured.
UV-light induced domino type reactions: Synthesis and photophysical properties of unreported nitrogen ring junction quinazolines
Palaniraja, Jeyakannu,Roopan, Selvaraj Mohana
, p. 37415 - 37423 (2015/05/20)
An expedient method for the synthesis of 5,6-dihydrobenzo[h][1,2,4]triazolo[5,1-b]quinazolines by UV light has been developed. Our aim was to synthesize various α, β-unsaturated carbonyl compounds and to further react them with different amines in DMF, in
Palladium-catalyzed asymmetric [3 + 2] trimethylenemethane cycloaddition reactions
Trost, Barry M.,Stambuli, James P.,Silverman, Steven M.,Schwoerer, Ulrike
, p. 13328 - 13329 (2007/10/03)
Transition-metal-catalyzed trimethylenemethane (TMM) [3 + 2] cycloadditions provide direct routes to functionalized cyclopentanes. This reaction has been shown to be a highly chemo-, regio-, and diastereoselective process. We report a palladium-catalyzed
Tetrahydronaphthalenes: Influence of heterocyclic substituents on inhibition of steroidogenic enzymes P450 arom and P450 17
W?chter, Gerald A.,Hartmann, Rolf W.,Sergejew, Tom,Grün, Gertrud L.,Ledergerber, Dorothea
, p. 834 - 841 (2007/10/03)
In search of new leads for selective inhibition of estrogen and androgen biosynthesis, respectively, heterocyclic substituted 2-(arylmethylene)-1- tetralones (1-4, 9-17), 2-(arylhydroxymethyl)-1-tetralones (5-8), exo- 1a,2,3,7b-tetrahydro-1H-cyclopropa[a]
