- 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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- ACYLSULFONAMIDE DERIVATIVES FOR TREATING SENESCENCE-ASSOCIATED DISEASES AND DISORDERS
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Compounds represented by Formula (I) and (II) and salts thereof are described herein. The compounds or salts of Formula (I) and (II) may be used to treat senescence-associated diseases and disorders.
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- INHIBITING B-CELL LYMPHOMA 2 (BCL-2) AND RELATED PROTEINS
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Novel compounds inhibiting anti-apoptosis proteins B-cell lymphoma 2 (Bcl-2) and Bcl-XL include compounds of formula (I) and formula (II) disclosed herein, as well as liposome compositions comprising Bcl-2 inhibitor compounds. These compositions are usefu
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Paragraph 00151
(2017/09/05)
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- CHEMICAL COMPOUNDS
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The present invention relates to compounds of Formula (I): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit Bcl-2 and/or Bcl-XL activities and may be used for the treatment of cancer.
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Page/Page column 33
(2012/02/15)
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- Profiling small molecule inhibitors against helix-receptor interactions: The Bcl-2 family inhibitor BH3I-1 potently inhibits p53/hDM2
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We validate a practical methodology for the rapid profiling of small molecule inhibitors of protein-protein interactions. We find that a well known BH3 family inhibitor can potently inhibit the p53/hDM2 interaction.
- Porter, Jason R.,Helmers, Mark R.,Wang, Ping,Furman, Jennifer L.,Joy, Stephen T.,Arora, Paramjit S.,Ghosh, Indraneel
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supporting information; experimental part
p. 8020 - 8022
(2011/01/03)
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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 34
(2009/12/28)
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- Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins
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Overexpression of prosurvival proteins such as Bcl-2 and Bcl-XL has been correlated with tumorigenesis and resistance to chemotherapy, and thus, the development of antagonists of these proteins may provide a novel means for the treatment of can
- Park, Cheol-Min,Bruncko, Milan,Adickes, Jessica,Bauch, Joy,Ding, Hong,Kunzer, Aaron,Marsh, Kennan C.,Nimmer, Paul,Shoemaker, Alexander R.,Song, Xiaohong,Tahir, Stephen K.,Tse, Christin,Wang, Xilu,Wendt, Michael D.,Yang, Xiufen,Zhang, Haichao,Fesik, Stephen W.,Rosenberg, Saul H.,Elmore, Steven W.
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experimental part
p. 6902 - 6915
(2009/11/30)
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- ARYLSULFONAMIDE COMPOUNDS
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The invention relates generally to small molecules that mimic the biological activity of certain peptides and proteins, to compositions containing them and to their use. In particular, the invention relates to compounds of the general formula (I) that mim
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Page/Page column 30; 31
(2008/12/05)
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- An efficient synthesis of ABT-263, a novel inhibitor of antiapoptotic Bcl-2 proteins
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ABT-263, a newly developed Bcl-2 inhibitor, was efficiently synthesized. The key intermediates 4-(4-{[2-(4-chlorophenyl)-5,5-dimethylcyclohex-1-enyl] methyl}piperazin-1-yl)benzoic acid and 4-fluoro-3-[(trifluoromethyl)sulfonyl] benzenesulfonamide were eff
- Wang, Guangjun,Zhang, Hushan,Zhou, Jing,Ha, Chengyong,Pei, Duanqing,Ding, Ke
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experimental part
p. 2398 - 2404
(2009/04/07)
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