- 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 0034; 0037; 0038; 0045; 0047-0048; 0052; 0054-0055
(2019/07/04)
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- A method of manufacturing a benzene derivative (trifluoromethylsulfonyl)
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PROBLEM TO BE SOLVED: To provide a method for producing a (trifluoromethylsulfonyl)benzene derivative which is useful as a medicine, an agricultural chemical, a functional material and a production intermediate thereof. SOLUTION: In this method, a (trifluoromethylsulfonyl)benzene derivative is produced by reacting diaryliodonium salt represented by general formula (1) with trifluoromethanesulfinic acid salt in the presence of a copper (I) salt. (In the formula, R1, R2, R3, R4, R5, R6, R7, R8, R9and R10each independently represents a hydrogen atom, a 1-6C alkyl group, a 1-6C haloalkyl group, a 1-6C alkoxy group, a 2-6C acyl group, (1-5C alkoxy)carbonyl group, a nitro group, a cyano group, a chlorine atom or a bromine atom). COPYRIGHT: (C)2013,JPOandINPIT
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Paragraph 0081; 0082
(2016/10/08)
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- Copper-Promoted Trifluoromethanesulfonylation and Trifluoromethylation of Arenediazonium Tetrafluoroborates with NaSO2CF3
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A tunable chemoselective trifluoromethanesulfonylation and trifluoromethylation of arenediazonium tetrafluoroborates with Langlois' reagent (NaSO2CF3) was developed. The Cu2O-catalyzed reaction in DMSO gave aryl trifluoromethanesulfones as the major products. On the other hand, the trifluoromethylated arenes were produced in the presence of oxidant tert-butyl hydroperoxide, CuBF4(MeCN)4, and 2,2′;6′,2 terpyridine (tpy). Both of these transformations proceed under mild conditions and tolerate functional groups.
- Zhang, Ke,Xu, Xiu-Hua,Qing, Feng-Ling
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p. 7658 - 7665
(2015/08/18)
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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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- 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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- Convenient one-pot procedure for converting aryl sulfides to nitroaryl sulfones
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When treated with nitrogen dioxide and ozone in inert solvent at 0°C or below, aryl sulfides underwent smooth oxidative nitration to give nitroaryl sulfones in good yield. Using this methodology, a series of mono- and di-nitrated aryl sulfones were prepared from methyl phenyl sulfide and diphenyl sulfide and their physical data are presented.
- Nose, Masatoshi,Suzuki, Hitomi
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p. 1065 - 1071
(2007/10/03)
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- PREPARATION AND FLUORINATION OF ARYLTRIFLUOROMETHYLSULPHONES
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A series of chloro- and nitrophenyl trifluoromethyl sulphides and sulphones have been synthesised from the corresponding aryl halides .The fluorination of these compounds by tetra-n-butyl ammonium fluoride and potassium fluoride has been investigated.Our results show that generally they are more susceptible to fluorodenitration than fluorodechlorination.
- Beaumont, Andrew J.,Clark, James H.
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p. 295 - 300
(2007/10/02)
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