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A catalytic desymmetrization of strained alkenes by ring-opening of meso-diazabicycles with acyl anion nucleophiles is reported. Densely functionalized frans-1,2-hydrazinoacyl cyclopentene building blocks are obtained stereoselectively. The acyl anion equivalent is generated in situ under very mild conditions from readily available organoboron precursors.

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Pyridazine – Wikipedia,
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A simple convenient method has been developed for the preparation of N-acetyl-S-arylcysteines based on the Chan-Lam-Evans arylation of N,N?-diacetylcystine dimethyl ester with arylboronic acids and used to synthesize a series of arylmercapturic acids. Unlike copper-mediated N-arylation, the S-arylation of neither cysteine nor cystine derivatives proceeded satisfactorily in the presence of air. Wiley-VCH Verlag GmbH & Co. KGaA.

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This invention relates to novel compounds having the structural formula Ia or formula Ib below: (Ia,Ib), and their phatmaceutically acceptable salts, tautomers or in vivo hydrolysable precursors, compositions and methods of use thereof. These novel compounds provide a treatment or prophylaxis of Abeta related pathologies such as cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.

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Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.

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Three palladium catalysts supported on graphene oxide (GO) and on its composite with TiO2 (GO-TiO2) were prepared and characterized. The presence of Pd NPs of different diameters (4-89 nm) and size distributions was evidenced by TEM measurements. GO-supported palladium efficiently catalysed the carbonylative coupling of iodobenzenes with aryl boronic acids forming relevant diarylketones at 1 atm CO. The highest activity and recyclability were obtained for Pd/GO-TiO2. The emission behaviour of Pd/GO and Pd/GO-TiO2 catalysts indicated structural changes occurring during the catalytic reaction.

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Delocalized aromatic molecules with matched electron-donating and electron-withdrawing groups enhancing insulating performance of polyethylene blends

Seven delocalized aromatic molecules with electron-donating and electron-withdrawing groups are applied as voltage stabilizers to improve the insulation properties of polyethylene blends. Voltage stabilizers 1 wt% are added into the blends (90 wt% low-density polyethylene and 10 wt% high density polyethylene) by diffusion loading method. Electrical measurements including electrical treeing, space charge distribution, and direct current conductivity are conducted to disclose their effects. The results show that the co-existence of matched electron-donating and electron-withdrawing groups in the molecules is favorable for the insulation properties. A 50% increase of tree initiation voltage is achieved with the addition of 3-aminobenzoic acid, which is also able to inhibit the space charge and decrease the conductivity at lower temperature. Besides, the grafting sample of the optimal molecule is successfully prepared and displayed enhanced electrical properties. Finally, the common internal mechanism of the delocalized molecules on different electrical properties is revealed.

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Synthesis of novel styryl-: N -isopropyl-9 H -carbazoles for designing trans -conjugated regular silicon hybrid materials

An efficient synthesis and characterization of several new, conjugated styryl-carbazole compounds functionalized by monovinylsilanes in a stereocontrolled approach is presented. All N-organic derivatives were successfully examined in silylative coupling in the presence of ruthenium-hydride complexes 4 and 5. Furthermore, a novel class of vinylene-arylene linear oligomeric materials with 1,4-bis(dimethylvinylsilyl)naphthalene in the main chain was produced. Both reactions proceed very effectively, stereo- and regioselectively, allowing one to obtain E-isomer derivatives with high isolation yields.

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A practical method for the one-step preparation of 3-arylpropionic acids through rhodium-catalyzed 1,4-addition of arylboronic acids to acrylic acid is reported. The method is applicable to a broad scope of aryl boronic acids and displays a wide functional group tolerance operating in water as the optimal reaction medium. Georg Thieme Verlag Stuttgart · New York.

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Discovery of a 2-hydroxyacetophenone derivative as an outstanding linker to enhance potency and beta-selectivity of liver X receptor agonist

Our research found that the 2-hydroxyacetophenone derivative is an outstanding linker between the 1,1-bistrifluoromethylcarbinol moiety and the imidazolidine-2,4-dione moiety to enhance the potency and beta-selectivity of liver X receptor (LXR) agonist in our head-to-tail molecular design. The incorporation of this linker is 20-fold more potent than our previous compound (2) for LXR beta agonistic activity (EC50) in a GAL-4 luciferase assay. Furthermore, we also identified 5-[5-(1-methylethoxy)pyridyl-2-yl]-5-methylimidazoline-2,4-dione (54), which lowers the lipophilicity of 2-hydroxyacetophenone derivative. We revealed that a combination of our newly developed linker and hydantoin (54) plays a pivotal role in improving the potency and selectivity of LXRbeta. The optically separated (?)-56 increases high-density lipoprotein cholesterol levels without elevating plasma triglyceride levels and results in a decrease of the lipid accumulation area in the aortic arch in a high-fat- and cholesterol-fed low-density lipoprotein receptor knock-out mice. In this manuscript, we report that (?)-56 is a highly potent and beta-selective LXR agonist for use in the treatment of atherosclerosis.

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Synthesis of trifluoromethyl-substituted di- and terphenyls by site-selective suzuki-miyaura reactions of 1,4-dibromo-2-trifluoromethyl-benzene

The Suzuki-Miyaura reaction of 1,4-dibromo-2-(trifluoromethyl)benzene provides a convenient route for the synthesis of various trifluoromethylated di- and terphenyls. The reactions proceed with excellent site selectivity in favor of the 4-position due to steric and electronic reasons.

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