- Synthesis method of 2-bromo-3-fluobenzoic acid
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The invention discloses a synthesis method of 2-bromo-3-fluobenzoic acid. The method comprises the following steps of (1) using o-bromo fluorobenzene as starting raw materials; performing proton abstraction through lithium diisopropylamide; performing rea
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Paragraph 0023; 0026; 0029
(2018/06/16)
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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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- Pyrimidine Derivatives
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Novel pyrimidine derivatives of formula I to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them
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Page/Page column 37
(2009/01/20)
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- Promoting or preventing haloaryllithium isomerizations: Differential basicities and solvent effects as the crucial variables
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Deprotonation-triggered heavy halogen migrations should become a favorite tool in arene synthesis if their occurrence and outcome could be made predictable. Particularly attractive, though extremely rare, are stop-and-go situations where a first intermediate, generated by metalation, can be trapped at -100 °C, whereas at -75 °C halogen migration gives rise to an isomer. As shown now, one can conveniently produce the initial aryllithium species by halogen/metal interconversion in toluene at -100 °C, under conditions that preclude, halogen migration, and unleash the isomerization process by adding tetrahydrofuran at -75 °C.
- Heiss, Christophe,Rausis, Thierry,Schlosser, Manfred
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p. 617 - 621
(2007/10/03)
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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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- 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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p. 881 - 884
(2007/10/02)
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- Synthetic Entries to 6-Fluoro-7-substituted Indole Derivatives
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Three practical synthetic entries of functionalized 6-fluoro-7-substituted indole derivatives were developed in connection with the preparation of 7-fluoro-8-substituted-1,3,4,9-tetrahydropyranoindole-1-acetic acid derivatives 11.The first route, w
- McKittrick, Brian,Failli, Amedeo,Steffan, Robert J.,Soll, Richard M.,Hughes, Philip,et al.
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p. 2151 - 2163
(2007/10/02)
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