104197-14-0Relevant articles and documents
Method for preparing alkyloxy aromatic compound from fluoroaromatic compound
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Paragraph 0035; 0036, (2017/05/18)
The invention discloses a method for preparing an alkyloxy aromatic compound from a fluoroaromatic compound. The alkyloxy aromatic compound is highly-efficiently prepared through a reaction of the fluoroaromatic compound, a strong alkali, dimethyl sulfoxide and alcohol under certain conditions. The method has the advantages of no metal catalyst, mild and controllable reaction, simple process, good universality, and suitableness for large-scale industrial production.
NOVEL KINASE MODULATORS
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, (2011/06/10)
The present invention provides PI3K protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of kinase mediated diseases or disorders with them.
New oxabispidine compounds for the treatment of cardiac arrhythmias
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Page/Page column 54, (2008/06/13)
There is provided compounds of formula I, wherein R1, R2, R3, R41 to R46, X, Y and Z have meanings given in the description, which compounds are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias.
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.
Elemental fluorine Part 12. Fluorination of 1,4-disubstituted aromatic compounds
Chambers, Richard D.,Hutchinson, John,Sparrowhawk, Matthew E.,Sandford, Graham,Moilliet, John S.,Thomson, Julie
, p. 169 - 173 (2007/10/03)
Direct fluorination of a series of 1,4-disubstituted benzene derivatives in acid reaction media at convenient temperature leads, in many cases, to selectively fluorinated aromatic products in preparatively useful conversions and yields.
Cyclic hydrocarbon derivative and liquid crystal composition containing the same
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, (2008/06/13)
A cyclic hydrocarbon derivative represented by formula (I): STR1 wherein each of Y1 and Y2 is independently F, Cl, CN, OCN, SCN, OCF3, OCF2 H, OCF2 CF3, CF3, R, --OR, --COOR or --OCOR, wherein R is alkyl, alkenyl or alkoxyalkyl, provided that at least one of Y1 and Y2 is R, --OR, --COOR or --OCOR; each of Z, Z1, Z2, Z3 and Z4 is independently a single bond, --CH2 CH2 --, --CH=CH--, --C C--, --COO--, --OCO--, --CH2 O--, OCH2 --, --(CH2)4 --, --(CH2)3 --O-- or --O--(CH2)3 --; ring A is group of formula (II): STR2 wherein each of X1, X2, X3, X4, X5, X6, X7, X8, X9, and X10 is independently H or D, provided that at least one of them is D; each of rings K, L, J, M and N is independently trans-1,4-cyclohexylene, 1,4-cyclohexenylene, substituted trans-1,4-cyclohexylene, 1,4-phenylene, substituted 1,4-phenylene, 1,3-dioxane-2,6-diyl, pyrimidine-2,5-diyl, pyridine-2,5-diyl, pyarazine-2,5-diyl or a group of formula (III): STR3 wherein each of X11, X12, X13, X14, X15, X16, X17, X18, X19, and X20 is independently H or D, provided that at least one of them is D; in which the ring of formula (III) may be the same as or different from ring A; and k, l, m, and n each independently is 0 or 1, provided that the sum of k, l, m, and n is 0, 1 or 2. The compound is useful as an electro-optic liquid crystal display material.