- Method for producing 4-fluoro-3-(trifluoromethylsulfonyl)benzenesulfonamide
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The invention provides a method for producing 4-fluoro-3-(trifluoromethylsulfonyl)benzenesulfonamide. 2-nitroaniline is used as an initial raw material, is subjected to diazotization reaction, trifluoromethyl sulfonation reaction, fluoronation, chlorosulfonation reaction, and is reacted with ammonium hydroxide to finally produce the 4-fluoro-3-(trifluoromethylsulfonyl)benzenesulfonamide. Comparedwith reported synthesis methods, the method for producing the 4-fluoro-3-(trifluoromethylsulfonyl)benzenesulfonamide has the advantages that the reaction yield of the synthesis route is high, used reaction agents are economic and easy to obtain, reaction conditions are mild and controllable, and in a reaction process, column chromatography and purification are not needed, so that the method for producing the 4-fluoro-3-(trifluoromethylsulfonyl)benzenesulfonamide has wide commercial application prospects.
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Paragraph 0030
(2019/07/04)
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- SuFEx-enabled, agnostic discovery of covalent inhibitors of human neutrophil elastase
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Sulfur fluoride exchange (SuFEx) has emerged as the new generation of click chemistry. We report here a SuFEx-enabled, agnostic approach for the discovery and optimization of covalent inhibitors of human neutrophil elastase (hNE). Evaluation of our ever-growing collection of SuFExable compounds toward various biological assays unexpectedly revealed a selective and covalent hNE inhibitor: benzene-1,2-disulfonyl fluoride. Synthetic derivatization of the initial hit led to a more potent agent, 2-(fluorosulfonyl)phenyl fluorosulfate with IC50 0.24 μM and greater than 833-fold selectivity over the homologous neutrophil serine protease, cathepsin G. The optimized, yet simple benzenoid probe only modified active hNE and not its denatured form.
- Zheng, Qinheng,Woehl, Jordan L.,Kitamura, Seiya,Santos-Martins, Diogo,Smedley, Christopher J.,Li, Gencheng,Forli, Stefano,Moses, John E.,Wolan, Dennis W.,Barry Sharpless
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p. 18808 - 18814
(2019/09/30)
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- NEW ANTIFIBRINOLYTIC COMPOUNDS
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It relates to spirocyclic compounds of formula (I), or pharmaceutically or veterinary acceptable salts thereof, or any stereoisomers either of the compounds of formula (I) or of their pharmaceutically or veterinary acceptable salts, wherein A and B form a spirocyclic ring system wherein the spiro atom connecting A and B is a carbon atom and wherein A is a known 3-to 8- membered carbocyclic or heterocyclic monocyclic ring or a known 6-to 18- membered carbocyclic or heterocyclic polycyclic ring system; B is a known 4- to 7-membered carbocyclic or heterocyclic monocyclic ring; C is phenyl or a known 5-to 6-membered heteroaromatic ring; and Z and R1-R7 are as defined herein. It also relates to pharmaceutical or veterinary compositions containing them, and to their use in medicine, in particular as antifibrinolytic and antihemorrhagic agents.
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Page/Page column 62
(2015/07/23)
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- Processes To Make Apoptosis Promoters
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Processes to make compounds, including N-acylsulfonamide apoptosis promoters are disclosed.
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Page/Page column 33
(2009/12/28)
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- NOVEL COMPOUNDS
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The present invention relates to novel indole derivatives such as compounds of the formula (I): which possess antagonist potency at the 5-HT6 receptor and the use of such compounds or pharmaceutically acceptable salts or solvates thereof in the treatment of Alzheimer's disease and other CNS disorders.
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Page/Page column 34
(2008/06/13)
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- 2,4-Substituted indoles and methods of use
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The present invention provides a compound of the formula: a pharmaceutically acceptable salt or a prodrug thereof, where R1, R2, R3, R4, p and n are those defined herein. The present invention also provides compositions comprising, methods for using, and methods for preparing Compound of Formula I.
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Page/Page column 12
(2010/02/06)
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