134142-88-4Relevant academic research and scientific papers
2-Substituted 4-(trifluoromethyl)phenols by directed ortho-lithiation
Geneste,Schaefer
, p. 2259 - 2262 (2001)
A broad variety of 2-substituted 4-(trifluoromethyl)phenols can be prepared in a large scale by o-lithiation and reaction with electrophiles in good to excellent yields. The key for the selectivity is the superior ortho-directing effect of the THP-protect
ALLOSTERIC CHROMENONE INHIBITORS OF PHOSPHOINOSITIDE 3-KINASE (PI3K) FOR THE TREATMENT OF DISEASES ASSOCIATED WITH P13K MODULATION
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Paragraph 1166, (2021/10/11)
The disclosure relates to compounds of Formula (I) as allosteric chromenone inhibitors of phosphoinositide 3-kinase (PI3K) useful in the treatment of diseases or disorders associated with PI3K modulation, Formula (I), or a prodrug, solvate, enantiomer, st
Ru-based complexes as heterogeneous potential catalysts for the amidation of aldehydes and nitriles in neat water
Arafa, Wael Abdelgayed Ahmed
supporting information, p. 1056 - 1064 (2020/11/09)
Five novel heterogeneous mononuclear complex-anchored Ru(III) have been efficiently sono-synthesized and characterized by utilizing several analytical techniques. The assembled complexes could be utilized as effective, robust and recyclable (up to eight consecutive runs) catalysts for one-pot transformation of a vast array of nitriles and aldehydes to primary amides in H2O under aerobic conditions. Moreover, some unreported di- and tetra-amide derivatives were obtained also under the optimal conditions. The results of ICP/OES analysis demonstrated that there is no detected leaching of the recycled catalyst, which suggests the real heterogeneity of the present protocol. The present Ru-complexes exhibited superiority compared to other reported catalysts for amide preparation in terms of low catalyst load, short reaction time, low operating temperature, no hazardous additives required, and high values of TON (990) and TOF (1980 h11).
Exploration of phenylpropanoic acids as agonists of the free fatty acid receptor 4 (FFA4): Identification of an orally efficacious FFA4 agonist
Sparks, Steven M.,Aquino, Christopher,Banker, Pierette,Collins, Jon L.,Cowan, David,Diaz, Caroline,Dock, Steven T.,Hertzog, Donald L.,Liang, Xi,Swiger, Erin D.,Yuen, Josephine,Chen, Grace,Jayawickreme, Channa,Moncol, David,Nystrom, Christopher,Rash, Vincent,Rimele, Thomas,Roller, Shane,Ross, Sean
, p. 1278 - 1283 (2017/06/19)
The long chain free fatty acid receptor 4 (FFA4/GPR120) has recently been recognized as lipid sensor playing important roles in nutrient sensing and inflammation and thus holds potential as a therapeutic target for type 2 diabetes and metabolic syndrome. To explore the effects of stimulating this receptor in animal models of metabolic disease, we initiated work to identify agonists with appropriate pharmacokinetic properties to support progression into in vivo studies. Extensive SAR studies of a series of phenylpropanoic acids led to the identification of compound 29, a FFA4 agonist which lowers plasma glucose in two preclinical models of type 2 diabetes.
A transition metal complex compound, and the compound of the catalyst and a catalyst for large amt. pentavelent carried out in the presence of an olefin multimer manufacturing method
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Paragraph 0254-0256, (2019/08/28)
PROBLEM TO BE SOLVED: To provide a transition metal complex compound, to provide an olefin polymerizing catalyst, containing the compound, and having excellent activity, and to provide a method for producing the olefin polymer which is carried out in the presence of the catalyst.SOLUTION: There is provided the transition metal complex compound of compound 3, e.g. of chemical formula; and the olefin polymerizing catalyst including following components (A) and (B): (A) the transition metal compound; and (B) at least one compound selected from the group consisting of (B-1) an organometallic compound, (B-2) an organoaluminumoxy compound, and (B-3) a compound reactive with the transition metal compound (A), and forming an ion pair.
Efficient copper-catalyzed trifluoromethylation of aromatic and heteroaromatic iodides: The beneficial anchoring effect of borates
Gonda, Zsombor,Kovacs, Szabolcs,Weber, Csaba,Gati, Tamas,Meszaros, Attila,Kotschy, Andras,Novak, Zoltan
supporting information, p. 4268 - 4271 (2014/09/30)
Efficient copper-catalyzed trifluoromethylation of aromatic iodides was achieved with TMSCF3 in the presence of trimethylborate. The Lewis acid was used to anchor the in situ generated trifluoromethyl anion and suppress its rapid decomposition. Broad applicability of the new trifluoromethylating reaction was demonstrated in the functionalization of different aromatic and heteroaromatic iodides.
N-heterocyclic carbene-catalyzed hydroacylation of unactivated double bonds
Hirano, Keiichi,Biju, Akkattu T.,Piel, Isabel,Glorius, Frank
supporting information; experimental part, p. 14190 - 14191 (2010/02/15)
(Chemical Equation Presented) An intramolecular N-heterocyclic carbene (NHC)-catalyzed hydroacylation of unactivated double bonds is reported. Systematic variation of the catalyst structure revealed an N- mesitylthiazolylidene annulated with a seven-membered ring to be especially reactive. This NHC enables a unique C-C bond-forming reaction to afford substituted chroman-4-ones in moderate to excellent yields, even ones containing all-carbon quaternary centers.
MODULATORS OF DOPAMINE NEUROTRANSMISSION
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Page/Page column 54, (2009/12/05)
The present invention relates to novel 1-(2,3-dihydro-1,4-benzodioxin-2-yl)-methanamine derivatives, useful as modulators of dopamine neurotransmission, and more specifically as dopaminergic stabilizers. In other aspects the invention relates to the use o
Generally applicable organocatalytic tetrahydropyranylation of hydroxy functionalities with very low catalyst loading
Kotke, Mike,Schreiner, Peter R.
, p. 779 - 790 (2008/01/03)
This paper presents the first acid-free, organocatalytic tetrahydropyran and 2-methoxypropene protection of alcohols, phenols, and other ROH derivatives utilizing privileged N,N′-bis[3,5-bis(trifluoromethyl)phenyl]thiourea and a polystyrene-bound analogue. The reactions are broadly applicably (also on preparative scale), in particular, to acid-sensitive substrates such as aldol products, hydroxy esters, acetals, silyl-protected alcohols, and cyanohydrins. The catalytic efficiency is truly remarkably with turnover numbers of 100,000 and turnover frequencies of up to 5700 h-1 at catalyst loadings down to 0.001 mol%. The computationally supported mechanistic interpretation emphasizes the hydrogen bond assisted heterolysis of the alcohol and concomitant preferential stabilization of the oxyanion hole in the transition state. Georg Thieme Verlag Stuttgart.
Studies towards the conception of new selective PPARβ/δ ligands
Ekambome Bassene, Carine,Suzenet, Franck,Hennuyer, Nathalie,Staels, Bart,Caignard, Daniel-Henri,Dacquet, Catherine,Renard, Pierre,Guillaumet, Gerald
, p. 4528 - 4532 (2007/10/03)
In order to define new PPARβ/δ ligands, SAR study on the selective PPARβ/δ activator L-165,041 led to the identification of one key functional group for selective PPARβ/δ activation. Furthermore, taking advantage of SAR studies done elsewhere on the most selective PPARβ/δ ligand GW501516, the conception of new ligands showing good affinity for PPARβ/δ is reported. Finally, synthesis and biological evaluation of pyridine analogues have shown the benefical effect of the pyridine ring on the PPARβ/δ subtype selectivity.
