- Intramolecular direct arylation in the synthesis of fluorinated carbazoles
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The amination of 2-chloroanilines with aryl bromides and subsequent intramolecular direct arylation can be exploited in the synthesis of a range of fluorinated carbazoles, where the fluorine substituent can be introduced via the aniline, the aryl bromide or both substrates. Depending on substitution patterns, the two steps can either be performed in tandem in one-pot under microwave heating conditions or else require a two pot approach.
- Bedford, Robin B.,Betham, Michael,Charmant, Jonathan P.H.,Weeks, Amanda L.
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p. 6038 - 6050
(2008/12/20)
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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 14
(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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