CAS: 489-17-8; 4-Fluoro-2-Methylbenzenesulfonamide

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CAS号7079-48-3 4-氟-2-甲基苯磺酰基氯 | CAS号352-70-5 3-氟甲苯 | CAS号845823-04-3 4-氟-2-甲基苯硫酚 | CAS号845644-47-5 5-氟-2,3-二氢苯并[d]...

📜4-氟-2-甲基苯磺酰氯置于ammonium Hydroxide体系中,用 1,4-二氧六环 作为反应溶剂,化学反应 6.0H,以79%的收率获得产物4-氟-2-甲基苯磺酰胺
参考文献:Synthesis And Cyclooxygenase-2 Inhibiting Property Of 1,5-Diarylpyrazoles With Substituted Benzenesulfonamide Moiety As Pharmacophore: Preparation Of Sodium Salt For Injectable Formulation†
标题:Synthesis And Cyclooxygenase-2 Inhibiting Property Of 1,5-Diarylpyrazoles With Substituted Benzenesulfonamide Moiety As Pharmacophore: Preparation Of Sodium Salt For Injectable Formulation†
摘要:A Series Of 1,5-Diarylpyrazoles Having A Substituted Benzenesulfonamide Moiety As Pharmacophore Was Synthesized And Evaluated For Cyclooxygenase (Cox-1/cox-2) Inhibitory Activities. Through Sar And Molecular Modeling,It Was Found That Fluorine Substitution On The Benzenesulfonamide Moiety Along With An Electron-Donating Group At The 4-Position Of The 5-Aryl Ring Yielded Selectivity As Well As Potency For Cox-2 Inhibition In Vitro. Among Such Compounds 3-Fluoro-4-[5-(4-Methoxyphenyl)-3-Trifluoromethyl-1H-1-Pyrazolyl]-1-Benzenesulfonamide 3 Displayed Interesting Pharmacokinetic Properties Along With Antiinflammatory Activity In Vivo. Among The Sodium Salts Tested In Vivo,10,The Propionyl Analogue Of 3,Showed Excellent Antiinflammatory Activity And Therefore Represents A New Lead Structure For The Development Of Injectable Cox-2 Specific Inhibitors.
DOI:10.1021/jm020563G

专利信息

专利号:CN-119977905-A
优先权日:2025-01-03
标 题:Green synthesis method of saccharin and saccharin derivative