55168-27-9Relevant academic research and scientific papers
Synthesis and evaluation of [2-(4-quinolyloxy)phenyl]methanone derivatives: Novel selective inhibitors of transforming growth factor-β kinase
Shimizu, Toshiyuki,Kimura, Kaname,Sakai, Teruyuki,Kawakami, Kazuki,Miyazaki, Tetsuko,Nakouji, Masayoshi,Ogawa, Akira,Ohuchi, Hitomi,Shimizu, Kiyoshi
supporting information; experimental part, p. 3326 - 3329 (2009/04/06)
We synthesized and evaluated various [2-(4-quinolyloxy)phenyl]methanone derivatives. These compounds had novel chemical structures that were distinct from those of previously reported inhibitors. Biological data suggested that these compounds inhibited transforming growth factor-β signaling by interacting with the ATP-binding pocket of the transforming growth factor-β type I receptor kinase domain. Here, we report on the synthesis and structure-activity relationships of the compounds in this series.
2-Amido-4-phenylthiazole Derivatives, The Preparation And The Therapeutic Use Thereof
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Page/Page column 9, (2008/06/13)
The disclosure relates to 2-amido-4-phenylthiazole derivatives of general formula (I) below: in which R1, R2, R3, Y, m, n, and p are as defined in the disclosure; as well as to their isomers, salts and solvates, to the pharmaceutical compositions containing them and to the therapeutic use thereof.
2-carbamide-4-phenylthiazole derivatives, preparation thereof and therapeutic use thereof
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Page/Page column 11, (2010/11/28)
The disclosure concerns 2-carbamide-4-phenylthiazole derivatives of general formula (I). The disclosure also concerns pharmaceutical compositions containing a compound of general formula (I) and to processes for preparing and methods of using compounds of
2-Acylamino-4-phenylthiazole derivatives, preparation thereof and therapeutic application thereof
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Page/Page column 17, (2008/06/13)
The invention relates to 2-acylamino-4-phenylthiazole derivatives of general formula (I): pharmaceutically acceptable acid-addition salts thereof, hydrates or solvates of such derivatives or such pharmaceutically acceptable acid addition salts, intermediates thereto, processes for the preparation thereof, and therapeutic application thereof.
O-acylation mechanism of p-substituted phenols with various alkanoyl chlorides under phase transfer catalysis conditions
Hashimoto, Iwao,Kawaji, Takatoshi,Mitoma, Yoshiharu,Simion, Alina M.,Semion, Cristian,Ishimoto, Keiko,Prakash, G.K. Surya,Olah, George A.,Tashiro, Masashi
, p. 149 - 155 (2007/10/03)
The phenolic ester synthesis between equimolecular amounts of phenols and various alkanoyl chlorides in the presence of aqueous sodium hydroxide solution in a two-phase system (20 mL of each 10% NaOH and dicloromethane, respectively) was reinvestigated under PTC conditions (10 mmol of tetrabutyl ammonium chloride, BNC). The esterification was complete within several minutes and the obtained ester was in high purity. For example, phenyl acetate was obtained quantitatively at 0°C in 5 minutes using a stoichiometric amount of BNC. This acylation procedure is technically simple and does not require anhydrous conditions. A bimolecular electrophilic attack of alkanoyl chloride against the ion-pair in the organic phase, which was formed between the quaternary ammonium cation and the phenoxide anion, must be a rate-determining step, because a plot of the logarithm of relative rate constants of various alkanoyl chlorides vs Taft's polar substituents constants (taking into account the steric constants, Es) gave a good linear relationship. We have found a simple, rapid, convenient, easily separating and efficient PTC technique to synthesize phenolic esters.
