654-76-2Relevant academic research and scientific papers
ALPHA-(TRIFLUOROMETHYL-SUBSTITUTED ARYLOXY, ARYLAMINO, ARYLTHIO OR ARYLMETHYL)-TRIFLUOROMETHYL-SUBSTITUTED PHENYLACETIC ACIDS AND DERIVATIVES AS ANTIDIABETIC AGENTS
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Page/Page column 50, (2010/02/13)
Compounds having a formula (1) or a pharmaceutically acceptable salt or prodrug thereof, are provided, and are useful for the treatment of metabolic disorders.
Novel and selective 5-HT(2C/2B) receptor antagonists as potential anxiolytic agents: Synthesis, quantitative structure - Activity relationships, and molecular modeling of substituted 1-(3- pyridylcarbamoyl)indolines
Bromidge, Steven M.,Dabbs, Steven,Davies, David T.,Duckworth, D. Malcolm,Forbes, Ian T.,Ham, Peter,Jones, Graham E.,King, Frank D.,Saunders, Damian V.,Starr, Susannah,Thewlis, Kevin M.,Wyman, Paul A.,Blaney, Frank E.,Naylor, Christopher B.,Bailey, Fiona,Blackburn, Thomas P.,Holland, Vicky,Kennett, Guy A.,Riley, Graham J.,Wood, Martyn D.
, p. 1598 - 1612 (2007/10/03)
The synthesis, biological activity, and molecular modeling of a novel series of substituted 1-(3-pyridylcarbamoyl)indolines are reported. These compounds are isosteres of the previously published indole urea 1 (SB- 206553) and illustrate the use of aromatic disubstitution as a replacement for fused five-membered rings in the context of 5-HT(2C/2B) receptor antagonists. By targeting a region of space previously identified as sterically allowed at the 5-HT(2C) receptor but disallowed at the 5-HT(2A) receptor, we have identified a number of compounds which are the most potent and selective 5-HT(2C/2B) receptor antagonists yet reported. 46 (SB-221284) was selected on the basis of its overall biological profile for further evaluation as a novel, potential nonsedating anxiolytic agent. A CoMFA analysis of these compounds produced a model with good predictive value and in addition good qualitative agreement with both our 5-HT(2C) receptor model and our proposed binding mode for this class of ligands within that model.
Process for the preparation of trifluoromethylphenols
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, (2008/06/13)
A process for the preparation of a trifluoromethylphenol or the corresponding alkoxy compound which comprises contacting a halogenobenzotrifluoride of the formula STR1 in which X denotes halogen, R1, R2 and R3 denote hydrogen, trifluoromethyl or a substituent which promotes the replacement of X by a hydroxyl group and Y denotes hydrogen, a halogen or alkoxy, at least one of the substituents R1, R2 and R3 representing a trifluoromethyl group and at least one of them representing a substituent which promotes the replacement of the radical X by a hydroxyl group, with an excess aqueous alkali metal hydroxide in an alcoholic solution in the presence of a quaternary onium salt.
