121-51-7Relevant articles and documents
Aromatic Chlorosulfonylation by Photoredox Catalysis
Májek, Michal,Neumeier, Michael,Jacobi von Wangelin, Axel
, p. 151 - 155 (2017)
Visible-light photoredox catalysis enables the efficient synthesis of arenesulfonyl chlorides from anilines. The new protocol involves the convenient in situ preparation of arenediazonium salts (from anilines) and the reactive gases SO2and HCl (from aqueous SOCl2). The photocatalytic chlorosulfonylation operates at mild conditions (room temperature, acetonitrile/water) with low catalyst loading. Various functional groups are tolerated (e.g., halides, azides, nitro groups, CF3, SF5, esters, heteroarenes). Theoretical and experimental studies support a photoredox-catalysis mechanism.
Proline-Based Allosteric Inhibitors of Zika and Dengue Virus NS2B/NS3 Proteases
Millies, Benedikt,Von Hammerstein, Franziska,Gellert, Andrea,Hammerschmidt, Stefan,Barthels, Fabian,G?ppel, Ulrike,Immerheiser, Melissa,Elgner, Fabian,Jung, Nathalie,Basic, Michael,Kersten, Christian,Kiefer, Werner,Bodem, Jochen,Hildt, Eberhard,Windbergs, Maike,Hellmich, Ute A.,Schirmeister, Tanja
, p. 11359 - 11382 (2019)
The NS2B/NS3 serine proteases of the Zika and Dengue flaviviruses are attractive targets for the development of antiviral drugs. We report the synthesis and evaluation of a new, proline-based compound class that displays allosteric inhibition of both proteases. The structural features relevant for protease binding and inhibition were determined to establish them as new lead compounds for flaviviral inhibitors. Based on our structure-activity relationship studies, the molecules were further optimized, leading to inhibitors with submicromolar IC50 values and improved lipophilic ligand efficiency. The allosteric binding site in the proteases was probed using mutagenesis and covalent modification of the obtained cysteine mutants with maleimides, followed by computational elucidation of the possible binding modes. In infected cells, antiviral activity against Dengue virus serotype 2 using prodrugs of the inhibitors was observed. In summary, a novel inhibitor scaffold targeting an allosteric site shared between flaviviral NS2B/NS3 proteases is presented whose efficacy is demonstrated in vitro and in cellulo.
Preparation method of substituted benzene sulfonyl chloride
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Paragraph 0055-0058, (2021/05/08)
The invention provides a preparation method of substituted benzene sulfonyl chloride, which comprises the following steps: carrying out diazotization reaction on an aniline compound with a structure as shown in a formula I to obtain fluoboric acid diazonium salt with a structure as shown in a formula II; obtaining substituted benzene sulfonyl chloride with a structure as shown in a formula III from the fluoboric acid diazonium salt with the structure as shown in the formula II; wherein R is selected from any one of ortho-chlorine, bromine, methyl, chloromethyl, bromomethyl, nitro, cyano, acetyl, meta-chlorine, bromine, methyl, chloromethyl, bromomethyl, nitro, cyano, acetyl, para-chlorine, bromine, methyl, chloromethyl, bromomethyl, nitro, cyano and acetyl. The preparation method of the substituted benzene sulfonyl chloride provided by the invention is simple in reaction process, easy to operate, ideal in effect and suitable for industrial production.
Preparation method of meta-ester and meta-ester (by machine translation)
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Paragraph 0040-0043; 0058-0061; 0076-0079; 0094-0097, (2020/06/16)
The molar ratio of the reduction product, the ethylene oxide and the sodium phosphate is 7.4 - 7.7; the molar ratio of the reduction product, the ethylene oxide and the sodium phosphate ranges from 0.68 - 0.685: (0.54 - 0.58): 7 - 7.5; the molar ratio Pd / C catalyst in each process link is controlled to 1; the product quality is improved; the environmental pollutants are reduced; and the method has the advantages of environmental protection and environmental protection effects and is obtained by esterification reaction and synthesis of the intermediate ester and Pd / C at PH ranges of (0.52 - 0.63): (0.00.12) 0.0012; and the method comprises the following steps of reducing the product, reducing environmental pollutants and 0.45 - 0.46 reducing environmental pollutants by adding sodium chloride and a Pd/C catalyst to the condensation product after the reaction is complete. (by machine translation)