620-86-0Relevant academic research and scientific papers
Magnesiation of Aryl Fluorides Catalyzed by a Rhodium-Aluminum Complex
Fujii, Ikuya,Semba, Kazuhiko,Li, Qiao-Zhi,Sakaki, Shigeyoshi,Nakao, Yoshiaki
supporting information, p. 11647 - 11652 (2020/08/06)
We report the magnesiation of aryl fluorides catalyzed by an Al-Rh heterobimetallic complex. We show that the complex is highly reactive to cleave the C-F bonds across the polarized Al-Rh bond under mild conditions. The reaction allows the use of an easy-to-handle magnesium powder to generate a range of arylmagnesium reagents from aryl fluorides, which are conventionally inert to such metalation compared with other aryl halides.
Synchronous reactor based on reaction and separation using air oxidation of substituted toluene method for producing substituted phenyl formic acid (by machine translation)
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Paragraph 0053; 0054, (2016/12/01)
The invention discloses a synchronous reaction and separation-based reactor utilizing air oxidizing substituted toluene method for producing substituted phenyl of formic acid, the reaction separation synchronous reactor comprises a bubbling gravity reaction tower or stirring the reaction tower and constant temperature sedimentation tower; the upper part of the gas phase area including reaction tower tower , and the reaction zone of the middle lower part of the reaction gas outlet at the top of the; reaction region of the bubbling gravity reaction tower on the tower wall is provided with a plurality of groups of alternating distribution of the gravity sedimentation plate; stirring reaction tower is provided with a stirrer within the reaction zone; the bottom of the reaction zone of the reaction tower is provided with a gas inlet and the gas distributor; the reaction tower and the constant temperature sedimentation tower through the flange connection; is arranged in the constant temperature sedimentation tower can be used for the liquid through the microporous filter plate, constant temperature sedimentation tower in a microporous filter plate is arranged at the lower part of the circulation pipeline is connected to the upper part of the reaction zone of the reaction tower; using the separated synchronization reactor device for air oxidizing substituted toluene producing substituted benzoic acid, can not only reduce the excessive reaction to the product in the reactor, to obtain the high purity product substituted benzoic acid, prevent sedimentation tower reactor is connected between the pipeline and the blockage of the circulation pipeline, but also can realize at the same time in the reaction of the substituted benzoic acid in a timely and effective separation. (by machine translation)
METHOD OF REGIOSELECTIVE SYNTHESIS OF SUBSTITUTED BENZOATES
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Page/Page column 11; 12; 18; 19; 20, (2013/03/26)
A method of synthesis of para-substituted benzoate esters and acids is provided, wherein the para-substituted regioisomer is obtained substantially free of the meta-substituted impurity, the method comprising contacting a coumalate ester or acid and an un activated alkene at elevated temperature in the presence of a metal oxidation catalyst and an oxidant. The metal oxidation catalyst can be palladium, such as palladium on carbon, and the oxidant can be the oxygen gas in ambient air. The reaction can be carlied out without solvent or in high boiling hydrocarbon solvents such as mesitylene. When the un activated alkene is a monosubstituted alkene, yields of at least about 50 or 60% of para-substituted ester and acid products, respectively, are obtained, substantially free of the regioisomelic meta-substituted impurity.
3-Mercapto-1,2,4-triazoles and N-acylated thiosemicarbazides as metallo-β-lactamase inhibitors
Faridoon,Hussein, Waleed M.,Vella, Peter,Islam, Nazar Ul,Ollis, David L.,Schenk, Gerhard,McGeary, Ross P.
supporting information; experimental part, p. 380 - 386 (2012/02/04)
The production of β-lactamases is an effective strategy by which pathogenic bacteria can develop resistance against β-lactam antibiotics. While inhibitors of serine-β-lactamases are widely used in combination therapy with β-lactam antibiotics, there are no clinically available inhibitors of metallo-β-lactamases (MBLs), and so there is a need for the development of such inhibitors. This work describes the optimisation of a lead inhibitor previously identified by fragment screening of a compound library. We also report that thiosemicarbazide intermediates in the syntheses of these compounds are also moderately potent inhibitors of the IMP-1 MBL from Pseudomonas aeruginosa. The interactions of these inhibitors with the active site of IMP-1 were examined using in silico methods.
Aromatics from pyrones: Para-substituted alkyl benzoates from alkenes, coumalic acid and methyl coumalate
Kraus, George A.,Riley, Sean,Cordes, Travis
experimental part, p. 2734 - 2736 (2011/11/06)
The Diels-Alder reaction of coumalic acid and methyl coumalate with unactivated alkenes provides only para-substituted adducts in good yield.
Alpha-helical mimetics
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Page/Page column 73-74, (2011/05/18)
Benzoyl urea derivatives that are alpha helical peptides mimetics that mimic BH3-only proteins, compositions containing them, their conjugation to cell-targeting-moieties, and their use in the regulation of cell death are disclosed. The benzoyl urea derivatives are capable of binding to and neutralizing pro-survival Bcl-2 proteins. Use of benzoyl urea derivatives in the treatment and/or prophylaxis of diseases or conditions associated with deregulation of cell death are also described.
Amine Compounds
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Page/Page column 159, (2008/12/08)
There is provided a compound exhibiting an activity of suppressing immune response with reduced adverse drug reactions, which compound is useful in the chemotherapy for preventing or treating, for example, a wide range of various autoimmune diseases including systemic erythematodes, chronic rheumatoid arthritis, Type I diabetes, inflammatory bowel disease, biliary cirrhosis, uveitis, multiple sclerosis or other disorders, or chronic inflammatory diseases, or cancers, lymphoma or leukemia, or resistance to organ or tissue transplantation or rejection against transplantation. Novel amine compounds having an S1P1/Edg1 receptor agonist effect, possible stereoisomers or racemic bodies of the compounds, or pharmacologically acceptable salts, hydrates or solvates of the compound, the stereoisomers or the racemic bodies, or prodrugs of the compounds, the stereoisomers, the racemic bodies, the salts, the hydrates or the solvates, are provided.
Palladium-catalyzed direct arylation of aryl(azaaryl)methanes with aryl halides providing triarylmethanes
Niwa, Takashi,Yorimitsu, Hideki,Oshima, Koichiro
, p. 2373 - 2375 (2008/02/05)
Direct arylation of aryl(azaaryl)methanes with aryl halidas takes place at the benzylic position in the presence of a hydroxide base under palladium catalysis to yield triarylmethanes
Purinenucleoside derivative modified in 8-position and medical use thereof
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Page/Page column 25, (2010/11/28)
The present invention provides an 8-modified purinenucleoside derivative which is useful for diseases associated with an abnormality of plasma uric acid level. An 8-modified purinenucleoside derivative represented by the following formula (I), a prodrug thereof or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof, is useful for the prevention or treatment of gout, hyperuricemia, urinary lithiasis, hyperuricemic nephropathy or the like. In the formula, n is 1 or 2; RA is a hydrogen atom or a hydroxyl group; R1 is a hydrogen atom, a hydroxyl group, a thiol group, an amino group or a chlorine atom; ring J represents an optionally substituted 2-naphthyl group, or a group represented by the following general formula (II) wherein Y represents a single bond or a connecting group; ring Z represents an optionally substituted aryl group or heteroaryl group or the like; and R2 to R4, P1 and Q represents a halogen atom, a cyano group or the like.
ALPHA-HELICAL MIMETICS
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Page/Page column 142, (2010/02/15)
Benzoyl urea derivatives that are alpha helical peptide mimetics that mimic BH3-only proteins, compositions containing them, their conjugation to cell-targeting moieties, and their use in the regulation of cell death are disclosed. The benzoyl urea derivatives are capable of binding to and neutralising pro-survival Bcl-2 proteins. Use of the benzoyl urea derivatives in the treatment and/or prophylaxis of diseases or conditions associated with deregulation of cell death are also disclosed.
