- Method for pipeline continuous fluorination with fluorine salt as fluorine source
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The method comprises the following steps: dissolving a fluorine salt in an aqueous polar aprotic solvent as reaction liquid A, dissolving an aryl (heterocyclic) chloride in a polar aprotic solvent as reaction liquid B, and reacting a polar aprotic solvent in the reaction liquid A with a polar aprotic solvent of the reaction liquid B. The reaction medium consisting of the preheated reaction liquid A and the preheated reaction liquid B enters the reaction coil for a fluorination reaction, and the resulting product from the reaction coil is subjected to post-treatment to obtain the product. The method has the characteristics of no need of adding a phase transfer catalyst, continuous production, low production cost and the like.
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Paragraph 0056-0061; 0094-0096
(2021/10/27)
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- 1,5,7-TRISUBSTITUTED ISOQUINOLINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES
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The present disclosure relates to 1,5,7-trisubstituted isoquinoline derivatives, their preparation and pharmaceutical use. In particular, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof. The definitions of the groups in the formula can be found in the specification and claims.
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Paragraph 0181; 0183; 0245-0246
(2020/08/30)
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- Method for synthesizing 3-fluoro-4-(4-morpholinyl)aniline by using micro-channel reactor
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The invention provides a method for synthesizing 3-fluoro-4-(4-morpholinyl)aniline by using a micro-channel reactor. The micro-channel reactor comprises a preheating module group composed of one or more parallely-connected preheating modules and a reactio
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Paragraph 0027; 008-0059; 0067; 0075-0077; 0087
(2017/08/27)
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- Reactions of aromatic compounds with xenon difluoride
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Reactions of substituted benzenes C6H5R (R = Me, F, Cl, Br, CF3, NO2) with xenon difluoride in the presence of boron trifluoride–diethyl ether complex in weakly acidic (1,1,1,3,3-pentafluorobutane) and weakly basic media (acetonitrile) have been studied. These reactions lead to the formation of fluorobenzene derivatives FC6H4R (isomer mixture) together with isomeric difluorobenzenes and fluorinated and non-fluorinated biphenyls. The results have been compared with previously reported data obtained in other solvents using other catalysts.
- Bardin,Adonin, N. Yu.
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p. 1400 - 1407
(2016/11/29)
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- Copper-catalyzed hydrodefluorination of fluoroarenes by copper hydride intermediates
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Breaking bad: Efficient copper-catalyzed C-F bond activation has been achieved by replacing fluorine with hydrogen. A copper hydride is proposed as the active intermediate, which proceeds through a nucleophilic attack on the fluorocarbon, as determined by experimental and theoretical results (see structure; C gray, H white, Cu light red, F light blue; distances in ?).
- Lv, Hongbin,Cai, Yuan-Bo,Zhang, Jun-Long
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supporting information
p. 3203 - 3207
(2013/04/23)
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- Continuous flow coupling and decarboxylation reactions promoted by copper tubing
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A convenient and efficient flow method for Ullmann condensations, Sonogashira couplings, and decarboxylation reactions using a commercially available copper tube flow reactor (CTFR) is described. The heated CTFR effects these transformations without added metals (e.g., Pd), ligands, or reagents, and in greater than 90% yield in most cases examined.
- Zhang, Yun,Jamison, Timothy F.,Patel, Sejal,Mainolfi, Nello
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supporting information; experimental part
p. 280 - 283
(2011/04/15)
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- Efficient phosphorus catalysts for the halogen-exchange (Halex) reaction
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New families of monomeric to dendritic, and monocationic to multicationic (PNP) compounds have been prepared and tested as catalysts in halogen exchange (Halex) reactions. Some of them allow an increase in the efficiency of these reactions which are performed in some cases under the mildest conditions reported up to now.
- Lacour, Marie-Agnes,Zablocka, Maria,Duhayon, Carine,Majoral, Jean-Pierre,Taillefer, Marc
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supporting information; experimental part
p. 2677 - 2682
(2009/10/20)
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- Tandem of nucleophilic substitution of hydrogen and cyclocondensation with participation of nitro group in the synthesis of fluorine-containing 3-amino-1,2,4-benzotriazines
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Reactions of 3-fluoro-1-nitrobenzenes with guanidine hydrochloride in THF in the presence of ButOK gave isomeric 5-and 7-fluoro-containing 3-amino-1,2,4-benzotriazines. Springer Science+Business Media, Inc. 2006.
- Zhumabaeva,Kotovskaya,Perova,Charushin,Chupakhin
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p. 1243 - 1247
(2008/02/03)
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- Elemental fluorine Part 12. Fluorination of 1,4-disubstituted aromatic compounds
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Direct fluorination of a series of 1,4-disubstituted benzene derivatives in acid reaction media at convenient temperature leads, in many cases, to selectively fluorinated aromatic products in preparatively useful conversions and yields.
- Chambers, Richard D.,Hutchinson, John,Sparrowhawk, Matthew E.,Sandford, Graham,Moilliet, John S.,Thomson, Julie
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p. 169 - 173
(2007/10/03)
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- A novel method for the nitration of simple aromatic compounds
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Simple aromatic compounds such as benzene, alkylbenzenes, halogenobenzenes, and some disubstituted benzenes are nitrated in excellent yields with high regioselectivity under mild conditions using zeolite β as a catalyst and a stoichiometric quantity of nitric acid and acetic anhydride. The zeolite can be recycled, and the only byproduct is acetic acid, which can be separated easily from the nitration product by distillation; the process is inexpensive and represents an attractive method for the clean synthesis of a range of nitroaromatic compounds. For example, nitration of toluene gives a quantitative yield of mononitrotoluenes, of which 79% is 4-nitrotoluene; fluorobenzene gives a quantitative yield of mononitro compounds, of which 94% is 4-nitrofluorobenzene; and 2-fluorotoluene gives a 96% yield of mononitro products, of which 90% is the 5-nitro isomer and 10% is the 4-nitro isomer.
- Smith, Keith,Musson, Adam,DeBoos, Gareth A.
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p. 8448 - 8454
(2007/10/03)
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- PHASE-TRANSFER CATALYSIS IN THE FLUORODECHLORINATION OF CHLORONITROARENES
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The activity of phase-transfer catalysts during the fluorodechlorination of chloronitroarenes in the absence of aprotic polar solvents was compared.The optimum conditions for the process were selected.
- Deev, L. E.,Nazarenko, T. I.,Podsevalov, P. V.
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p. 1925 - 1929
(2007/10/03)
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- Process for the synthesis of fluorinated derivatives
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A process for the synthesis of fluorinated organic compounds and a reagent suitable for use in the process. The process is carried out by exchange with fluorides, while preferably agitating the reaction medium with ultrasonic sound.
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- A General Procedure for the Fluorodenitration of Aromatic Substrates
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The synthesis of several fluoroaromatic compounds by a new procedure of fluorodenitration of nitroarenes is reported.The methodology is based on the principle that the nitrite ion, generated during the fluorodenitration processes and responsible for most of the undesired side reactions, can be trapped with a suitable reagent, e.g., phthaloyl difluoride or tetrafluorophthaloyl difluoride.The yields of fluoro compounds thus obtained are good to excellent, and the procedure is of general application.
- Maggini, Michele,Passudetti, Margherita,Gonzales-Trueba, Guadalupe,Prato, Maurizio,Quintily, Ugo,Scorrano, Gianfranco
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p. 6406 - 6411
(2007/10/02)
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- Synthesis of Aromatic Fluoro Compounds by Nucleophilic Exchange of Nitro Groups by Fluoride
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The synthesis of aromatic fluoro compounds from the respective nitro compounds by nucleophilic substitution of nitrite by fluoride is described.Reasonable yields in case of nonactivated nitro compounds are only obtained if the nitrite formed in the reaction is eliminated by acylation. 1-Fluoro-3-nitrobenzene (2) was obtained from 1,3-dinitrobenzene (1), and 1-fluoro-3,5-dinitrobenzene (9) as well as 1,3-difluoro-5-nitrobenzene (10) from 1,3,5-trinitrobenzene (8) in yields up to 92percent by reaction of nitro compounds with potassium fluoride in sulfolane at 180-200 deg C in the presence of phthaloyl dichloride (6); 1,2-difluoro-4-nitrobenzene (12) was formed in 58percent yield from 2,4-dinitro-1-fluorobenzene (11) in the presence of pyromellitoyl tetrachloride (13).
- Effenberger, Franz,Streicher, Willi
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p. 157 - 162
(2007/10/02)
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- Tetraphenylphosphonium Salts-Grafted Copolymers as Catalysts for Halogen-Exchange Fluorinations
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Cross-linked styrene/2-(4-chlorophenyl)propene copolymer-grafted tetraphenylphosphonium salt was an effective and reusable catalyst for the reaction of aromatic chlorides with anhydrous potassium fluoride to afford the corresponding aromatic fluorides in good yields.
- Yoshida, Yasuo,Kimura, Yoshikazu,Tomoi, Masao
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p. 769 - 772
(2007/10/02)
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- General and Highly Efficient Syntheses of m-Fluoro Arenes Using Potassium Fluoride-Exchange Method
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Tetraphenylphosphonium bromide was found to be a suitable catalyst for the reaction of m-nitroaryl derivatives carrying cyano, nitro, chlorocarbonyl, trifluoromethyl, and chlorosulfonyl groups with potassium fluoride in the presence of a stoichiometric amount of phthaloyl dichloride, giving the corresponding m-fluoro aromatic derivatives in good yields.The catalyst was also found to be efficient for the fluorodesulfonylation of m-(fluorosulfonyl)aryl derivatives to afford m-fluoro arenes by the use of a reaction-distillation technique.
- Suzuki, Hiroshi,Yazawa, Naoto,Yoshida, Yasuo,Furusawa, Osamu,Kimura, Yoshikazu
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p. 2010 - 2017
(2007/10/02)
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- Tetraphenylphosphonium Bromide Catalyzed Fluorodenitrations and Fluorodesulfonylations. Efficient Syntheses of m-Fluoroaromatic Compounds
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Meta-fluoroaromatic compounds were effectively synthesized from m-nitroaromatic or m-fluorosulfonylaromatic compounds by replacement reaction with potassium fluoride in the presence of a catalytic amount of tetraphenylphosphonium bromide.
- Yazawa, Naoto,Suzuki, Hiroshi,Yoshida, Yasuo,Furusawa, Osamu,Kimura, Yoshikazu
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p. 2213 - 2216
(2007/10/02)
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- Preparation of fluorine-substituted aromatic compounds
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Fluorine-substituted aromatic compounds are obtained by reacting the corresponding nitro compound with a salt of hydrofluoric acid in the presence of an acid halide.
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- SYNTHESIS AND SOME PROPERTIES OF 3,4-DIFLUOROPHENYL TRANS-4 prime -SUBSTITUTED CYCLOHEXANE-1 prime -CARBOXYLATES.
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A new series of 3,4-difluorophenyl trans-4 prime -substituted cyclohexane-1 prime -carboxylates was synthesized in order to achieve a nematic compound of positive dielectric anisotropy and low viscosity. The effect of fluoro substituents on mesomorphic and physical properties was established by comparing these compounds with other fluorinated nematic compounds.
- Takatsu,Takeuchi,Sato
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p. 165 - 180
(2007/10/02)
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- Manufacture of substituted fluorobenzenes
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Fluorobenzenes are manufactured by reacting substituted chlorobenzenes with potassium fluoride in the presence of catalytic amounts of cesium fluoride and in the presence of certain solvents; m-nitrofluorobenzenes and m-cyanofluorobenzenes can also be manufactured in the absence of cesium fluoride. The products are starting materials for the manufacture of dyes, pharmaceuticals and pesticides.
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- Polycyclophenylpyrrolidines, their compositions and use
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Compounds of the formula STR1 where R4 X is a polycyclocoupled group and R1 and R2 are H or simple hydrocarbon and R3 has the same value and additionally simple acyl, can be made by a variety of syntheses. They have hypolipedemic and antiatherosclerotic properties, and are useful in that field.
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