2358-41-0Relevant academic research and scientific papers
Process for preparing sulfonamide compounds
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Paragraph 0415; 0470-0471; 0475-0476, (2020/07/24)
The invention relates to a process for preparing sulfonamide compounds. The sulfonamide compound is an inhibitor of Bcl-2/Bcl-xL and is prepared from a compound (3R)-1-(3-(4-(4-(4-(3-(2-(4-chlorphenyl)-1-isopropyl-4-methylsulfonyl-5-methyl-1H-pyrrole-3-yl
PROCESS FOR PREPARING SULFONAMIDE COMPOUNDS
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Page/Page column 74-75, (2020/09/03)
Provided are a process for preparing a sulfonamide compound which is an inhibitor of Bcl-2/Bcl-xL, including the compound (3R) -1- (3- (4- (4- (4- (3- (2- (4-chlorophenyl) -1-isopropyl-4-methylsulfonyl-5-methyl-1H-pyrrol-3-yl) -5-fluorophenyl) piperazine
Method for producing 4-fluoro-3-(trifluoromethylsulfonyl)benzenesulfonamide
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Paragraph 0029, (2019/07/04)
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.
Ortho-lithiation reaction of aryl triflones
Sumii, Yuji,Taniguchi, Misaki,Xu, Xiu-Hua,Tokunaga, Etsuko,Shibata, Norio
, p. 5635 - 5641 (2018/08/17)
The ortho-lithiation of substituted arenes is a powerful methodology to synthesize ortho-substituted arenes. While a wide variety of directed metalation groups (DMGs) have been reported, trifluoromethyl sulfone has never been used. We disclose the first example of ortho-lithiation of aryl triflones. We found that the trifluoromethyl sulfonyl group is not only an important structural motif in biologically active molecules and specialty materials, but also an excellent DMG moiety for ortho-metalation reactions. The use of a base that causes steric hindrance, LTMP, is the key for successful transformation to furnish a variety of ortho-substituted aryl triflones in good yields. Further functionalization of resulting ortho-substituted aryl triflones was demonstrated by metal-catalyzed coupling reactions.
ACYLSULFONAMIDE DERIVATIVES FOR TREATING SENESCENCE-ASSOCIATED DISEASES AND DISORDERS
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Paragraph 0135; 0137, (2017/07/14)
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.
Cu-catalyzed couplings of aryl iodonium salts with sodium trifluoromethanesulfinate
Cullen, Steven C.,Shekhar, Shashank,Nere, Nandkishor K.
, p. 12194 - 12201 (2014/01/06)
A convenient method for the preparation of aryl trifluoromethylsulfones from the reactions of diaryliodonium salts with sodium trifluoromethanesulfinate in the presence of copper catalysts is described. Cuprous oxide in DMF was found to be the optimal catalyst for the reaction. The reaction conditions are tolerant of various functional groups as well as of various counteranions of the iodonium salt. The synthetic utility of the process is demonstrated by performing the reaction on a preparative scale (88 g).
Profiling small molecule inhibitors against helix-receptor interactions: The Bcl-2 family inhibitor BH3I-1 potently inhibits p53/hDM2
Porter, Jason R.,Helmers, Mark R.,Wang, Ping,Furman, Jennifer L.,Joy, Stephen T.,Arora, Paramjit S.,Ghosh, Indraneel
supporting information; experimental part, p. 8020 - 8022 (2011/01/03)
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.
Processes To Make Apoptosis Promoters
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Page/Page column 34, (2009/12/28)
Processes to make compounds, including N-acylsulfonamide apoptosis promoters are disclosed.
Discovery of an orally bioavailable small molecule inhibitor of prosurvival B-cell lymphoma 2 proteins
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.
experimental part, p. 6902 - 6915 (2009/11/30)
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
ARYLSULFONAMIDE COMPOUNDS
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Page/Page column 30, (2008/12/05)
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
