369-34-6Relevant academic research and scientific papers
Method for pipeline continuous fluorination with fluorine salt as fluorine source
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Paragraph 0056-0061; 0094-0096, (2021/10/27)
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.
1,5,7-TRISUBSTITUTED ISOQUINOLINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES
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Paragraph 0181; 0183; 0245-0246, (2020/08/30)
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.
Method for synthesizing 3-fluoro-4-(4-morpholinyl)aniline by using micro-channel reactor
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Paragraph 0027; 008-0059; 0067; 0075-0077; 0087, (2017/08/27)
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
Reactions of aromatic compounds with xenon difluoride
Bardin,Adonin, N. Yu.
, p. 1400 - 1407 (2016/11/29)
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.
Copper-catalyzed hydrodefluorination of fluoroarenes by copper hydride intermediates
Lv, Hongbin,Cai, Yuan-Bo,Zhang, Jun-Long
supporting information, p. 3203 - 3207 (2013/04/23)
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 ?).
Continuous flow coupling and decarboxylation reactions promoted by copper tubing
Zhang, Yun,Jamison, Timothy F.,Patel, Sejal,Mainolfi, Nello
supporting information; experimental part, p. 280 - 283 (2011/04/15)
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.
Efficient phosphorus catalysts for the halogen-exchange (Halex) reaction
Lacour, Marie-Agnes,Zablocka, Maria,Duhayon, Carine,Majoral, Jean-Pierre,Taillefer, Marc
supporting information; experimental part, p. 2677 - 2682 (2009/10/20)
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.
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
Zhumabaeva,Kotovskaya,Perova,Charushin,Chupakhin
, p. 1243 - 1247 (2008/02/03)
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.
Elemental fluorine Part 12. Fluorination of 1,4-disubstituted aromatic compounds
Chambers, Richard D.,Hutchinson, John,Sparrowhawk, Matthew E.,Sandford, Graham,Moilliet, John S.,Thomson, Julie
, p. 169 - 173 (2007/10/03)
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.
A novel method for the nitration of simple aromatic compounds
Smith, Keith,Musson, Adam,DeBoos, Gareth A.
, p. 8448 - 8454 (2007/10/03)
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.
