- Synthesis, characterization and pharmacological evaluation of1-(2-chloro-6-fluorophenyl)-5-methylindolin-2-one: A new anti-inflammatory compound with reduced gastric ulceration properties
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The new compound 1-(2-chloro-6-fluorophenyl)-5-methylindolin-2-one (1), designed using the prodrug approach, was easily obtained in 85% yield and characterized by nuclear magnetic resonance, elemental analysis, mass spectrometry and infrared spectroscopy.
- Dos Santos, Jean Leandro,Chelucci, Rafael,Chiquetto, Richard,Chung, Man Chin,Campos, Michel Leandro,Peccinini, Rosangela Goncalves
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- Process for phenylacetic acid derivatives
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A process for the production of a compound of Formula I, or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable prodrug ester thereof, comprising cleaving a lactam of formula II wherein the symbols are as defined, with a base; and precursors therefor and processes for the preparation of the precursors. The compounds of Formula I are pharmaceutically active compounds which are selective inhibitors of Cyclooxygenase II.
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Page/Page column 17
(2008/12/04)
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- Synthesis of new N-aryl oxindoles as intermediates for pharmacologically active compounds
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Various new N-aryl oxindoles were synthesized as intermediates for the preparation of pharmacologically active 2-(N-arylamino)-phenylacetic acids. Two novel approaches were explored for the construction of diarylamine and N-aryl oxindole core structures, in addition to Buchwald-arylamination and Smiles rearrangement. Condensation of anilines with 2-oxo-cyclohexylidene-acetic acid derivatives and subsequent dehydrogenation is a new and viable method for the preparation of N-aryl oxindoles. Graphical Abstract.
- Acemoglu, Murat,Allmendinger, Thomas,Calienni, John,Cercus, Jacques,Loiseleur, Olivier,Sedelmeier, Gottfried H.,Xu, David
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p. 11571 - 11586
(2007/10/03)
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- Certain 5-alkyl-2-arylaminophenylacetic acids and derivatives
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Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1is chloro or fluoro; R2is hydrogen or fluoro; R3is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4is hydrogen or fluoro; and R5is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.
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