- Preparation method of 1-fluoro-2-bromo-iodobenzene
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The invention provides a preparation method of 1-fluoro-2-bromo-iodobenzene. The method comprises the steps that 1-fluorine-2-amidogen-3-nitrobenzene is used as a raw material, 1-fluorine-2-bromine-3-nitrobenzene is obtained through a diazotization and bromination reaction, 1-fluoro-2-bromo-aminobenzene is obtained through a following reduction reaction, and then 1-fluoro-2-bromo-iodobenzene is obtained through a diazotization and iodination reaction. According to the preparation method, under the acidic condition, 1-fluoro-2-bromo-aminobenzene and sodium nitrite react in a solvent, hydrogen iodide or iodate is added to the mixed solution, and 1-fluoro-2-bromo-iodobenzene is obtained through a reaction. The preparation method of 1-fluoro-2-bromo-iodobenzene is high in safety, mild in reaction condition, low in cost, easy to operate and industrialize and high in utilization rate of iodine.
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Paragraph 0045; 0047; 0052; 0053; 0062; 0071
(2018/06/16)
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- 7-AMINOFUROPYRIDINE DERIVATIVES
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Compounds of Formula 1, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by TAK1 or for which an appropriate TAK1 inhibitor is effective. This Abstract is not limiting of the invention.
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Page/Page column 53
(2011/09/15)
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- Palladium-catalyzed aryl amination-heck cyclization cascade: A one-flask approach to 3-substituted indoles
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(Chemical Equation Presented) Two for the price of one: A Pd/dppf-based catalyst provides access to the title compounds from 1,2-dihalogenated aromatic compounds and allylic amines in a single reaction flask. The initial aryl amination step occurs with excellent selectivity for the aryl iodide to ensure the formation of a single indole regioisomer, which can be functionalized in situ by N-arylation (see scheme). dba = dibenzylideneacetone, dppf = 1,1′-bis(diphenylphospanyl)ferrocene.
- Jensen, Thomas,Pedersen, Henrik,Bang-Andersen, Benny,Madsen, Robert,Jorgensen, Morten
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p. 888 - 890
(2008/09/20)
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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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