656304-67-5Relevant articles and documents
POLYMERIZABLE COMPOUND AND OPTICAL ANISOTROPIC BODY
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Paragraph 0103; 0104; 0107, (2017/07/26)
PROBLEM TO BE SOLVED: To provide a polymerizable compound exhibiting high stability without inducing precipitation of crystals when added to a polymerizable composition, to provide a polymerizable composition containing the above polymerizable compound, giving uniform homeotropic alignment in a polymer obtained by polymerizing the polymerizable composition, and to provide a polymer having a small haze value and little irregularity obtained by polymerizing the above polymerizable composition, and an optical anisotropic body using the polymer. SOLUTION: The present invention provides a compound represented by general formula (I) and provides a composition comprising the above compound, a polymer obtained by polymerizing the composition, and an optical anisotropic body or the like using the polymer. SELECTED DRAWING: None COPYRIGHT: (C)2017,JPOandINPIT
An efficient protocol for the palladium-catalysed Suzuki-Miyaura cross-coupling
Marziale, Alexander N.,Jantke, Dominik,Faul, Stefan H.,Reiner, Thomas,Herdtweck, Eberhardt,Eppinger, Joerg
supporting information; experimental part, p. 169 - 177 (2011/03/23)
The palladacyclic catalyst precursor received by ortho-palladation of ([1,1′-biphenyl]-2-yloxy)diisopropyl-phosphine represents a highly active system for Suzuki-Miyaura cross-coupling reactions when used in neat water. An efficient, broadly applicable and sustainable aqueous protocol was developed using 2.5 eq. of Na2CO3 as base, allowing the reaction to be performed under air and at ambient temperature with Pd loadings of 0.04 mol%. Coupling products are obtained in high yields and excellent purity by simple filtration with no organic solvents needed throughout the whole reaction. A broad variety of functional groups are tolerated and a large number of substrates can be applied with this protocol. The crystal structure of the palladacyclic catalyst precursor is presented as well as investigations targeting the nature of catalyst activation and the active catalytic species.
Diflunisal Analogues Stabilize the Native State of Transthyretin. Potent Inhibition of Amyloidogenesis
Adamski-Werner, Sara L.,Palaninathan, Satheesh K.,Sacchettini, James C.,Kelly, Jeffery W.
, p. 355 - 374 (2007/10/03)
Analogues of diflunisal, an FDA-approved nonsteroidal antiinflammatory drug (NSAID), were synthesized and evaluated as inhibitors of transthyretin (TTR) aggregation, including amyloid fibril formation. High inhibitory activity was observed for 26 of the compounds. Of those, eight exhibited excellent binding selectivity for TTR in human plasma (binding stoichiometry > 0.50, with a theoretical maximum of 2.0 inhibitors bound per TTR tetramer). Biophysical studies reveal that these eight inhibitors dramatically slow tetramer dissociation (the rate-determining step of amyloidogenesis) over a duration of 168 h. This appears to be achieved through ground-state stabilization, which raises the kinetic barrier for tetramer dissociation. Kinetic stabilization of WT TTR by these eight inhibitors is further substantiated by the decreasing rate of amyloid fibril formation as a function of increasing inhibitor concentration (pH 4.4). X-ray cocrystal structures of the TTR·182 and TTR·202 complexes reveal that 18 and 20 bind in opposite orientations in the TTR binding site. Moving the fluorines from the meta positions in 18 to the ortho positions in 20 reverses the binding orientation, allowing the hydrophilic aromatic ring of 20 to orient in the outer binding pocket where the carboxylate engages in favorable electrostatic interactions with the ε-ammonium groups of Lys 15 and 15′. The hydrophilic aryl ring of 18 occupies the inner binding pocket, with the carboxylate positioned to hydrogen bond to the serine 117 and 117′ residues. Diflunisal itself appears to occupy both orientations based on the electron density in the TTR·12 structure. Structure-activity relationships reveal that para-carboxylate substitution on the hydrophilic ring and dihalogen substitution on the hydrophobic ring afford the most active TTR amyloid inhibitors.
