- Regiospecific Synthesis of Mixed 2,3-Dihalobenzoic Acids and Related Acetophenones via Ortho-Metalation Reactions
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Concise general routes to mixed 2,3-dihalobenzoic acids and related acetophenones-based on directed ortho-metalation and ipso-desilylation reactions are described.
- Moyroud, Joel,Guesnet, Jean-Luc,Bennetau, Bernard,Mortier, Jacques
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- A gram-scale synthesis of multi-substituted arenes via palladium catalyzed C-H halogenation
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(6-Amino-2-chloro-3-fluorophenyl)methanol is prepared through both traditional methods and palladium catalyzed iterative C-H halogenation reactions. In comparison to traditional approach, the C-H functionalization strategy demonstrated a few advantages in
- Sun, Xiu-Yun,Sun, Yong-Hui,Rao, Yu
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p. 667 - 669
(2014/06/09)
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- METHOD OF TREATMENT
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This invention relates to the use of a sulfonamide substituted diphenyl urea compound to treat cystic fibrosis, or the symptoms associated with cystic fibrosis.
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Page/Page column 13
(2009/04/25)
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- INHIBITORS OF STEAROYL-COA DESATURASE
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity.
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- METHOD OF TREATMENT
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This invention relates to the use of sulfonamide substituted diphenyl urea compounds to treat endometriosis.
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Page/Page column 5
(2008/06/13)
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- IL-8 RECEPTOR ANTAGONISTS
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This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
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Page/Page column 12
(2010/11/08)
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- IL-8 RECEPTOR ANTAGONISTS
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This invention relates to novel compounds of Formula (I) to (VII), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
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- Il-8 receptor anatagonists
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This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
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- Lithiations directed by carboxylic acid, fluorine and chlorine: The regioselective synthesis of polysubstituted benzoic acids and acetophenones
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Lithiation/electrophilic quenching of ortho-lithiated benzoates allows the totally regiocontrolled synthesis of a wide range of 2,3-, 2,3,4-, and 2,3,4,5-polysubstituted benzoic acids and related acetophenones. Elsevier,.
- Moyroud, Joel,Guesnet, Jean-Luc,Bennetau, Bernard,Mortier, Jacques
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p. 133 - 141
(2007/10/03)
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- Directed lithiation of unprotected benzoic acids
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Benzoic acid gives the ortho-lithiated species 1 under standard conditions (s-BuLi-TMEDA-THF, -90 deg C).Reaction of 1 at -78 deg C with either methyl iodide, dimethyl disulfide, hexachloroethane, or 1,2-dibromotetrachloroethane gives the ortho-substituted product.Intramolecular competition between the carboxylic acid and methoxy, chloro, fluoro, or diethylamido functions in ortho- and -para-substituted benzoic acids establishes the carboxylic acid group to be of intermediate capacity in directing metallation.Complimentarity of directing effects is observed with the chloro and fluoro groups in the meta-substituted benzoic acid but not with the methoxy and trifluoromethyl groups.Electrophile introduction into meta- and para-lithiated benzoates occurs with equal efficacy and comparable scope.The 2,4-dihalogenobenzoic acids undergo hydrogen/metal exchange at the position flanked by both halogen substituents. 2,2-Difluoro-1,3-benzodioxole-4-carboxylic acid undergoes lithiation adjacent to the oxygen atom.By use of such methods, routes to benzoic acids contiguously tri- and tetra-substituted with a variety of functionalities have been developed.
- Bennetau, Bernard,Mortier, Jacques,Moyroud, Joel,Guesnet, Jean-Luc
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p. 1265 - 1272
(2007/10/02)
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- Processes for preparing ortho-substituted benzoic acids
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A novel process for the synthesis of ortho-substituted benzoic acid by lithiating an unprotected benzoic acid and a number of novel orth-substituted benzoic acids are described.
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