CAS: 170570-01-1; 4-(5-(M-Tolyl)-3-(Trifluoromethyl)-1H-Pyrazol-1-yl)Benzenesulfonamide

3'-甲基苯乙酮置于sodium Methylate体系中,用 甲醇,乙醇 用作溶剂,化学反应 44.0H,反应生成4-[5-(3-甲基苯基)-3-三氟甲基-1H-吡唑-1-基]苯磺酰胺
参考文献:Synthesis And Biological Evaluation Of The 1,5-Diarylpyrazole Class Of Cyclooxygenase-2 Inhibitors: Identification Of 4-[5-(4-Methylphenyl)-3-(Trifluoromethyl)-1H-Pyrazol-1-Yl]Benzenesulfonamide (Sc-58635,Celecoxib)
标题:Synthesis And Biological Evaluation Of The 1,5-Diarylpyrazole Class Of Cyclooxygenase-2 Inhibitors: Identification Of 4-[5-(4-Methylphenyl)-3-(Trifluoromethyl)-1H-Pyrazol-1-Yl]Benzenesulfonamide (Sc-58635,Celecoxib)
摘要:A Series Of Sulfonamide-Containing 1,5-Diarylpyrazole Derivatives Were Prepared And Evaluated For Their Ability To Block Cyclooxygenase-2 (Cox-2) In Vitro And In Vivo. Extensive Structure-Activity Relationship (Sar) Work Was Carried Out Within This Series,And A Number Of Potent And Selective Inhibitors Of Cox-2 Were Identified. Since An Early Structural Lead (1F,Sc-236) Exhibited An Unacceptably Long Plasma Half-Life,A Number Of Pyrazole Analogs Containing Potential Metabolic Sites Were Evaluated Further In Vivo In An Effort To Identify Compounds With Acceptable Pharmacokinetic Profiles. This Work Led To The Identification Of Ii (4-[5-(4-Methylphenyl)-3-(Trifluoromethyl)-1H-Pyrazol-1-Yl]Benzenesulfonamide,Sc-58635,Celecoxib),Which Is Currently In Phase Iii Clinical Trials For The Treatment Of Rheumatoid Arthritis And Osteoarthritis.
Doi:10.1021/jm960803Q