3-氨基-5-溴三氟甲苯置于盐酸,Sodium Nitrite,二氧化硫,溶剂黄146,Copper(L) Chloride体系中,用 水 用作溶剂,化学反应 2.0H,反应生成3-溴-5-(三氟甲基)苯磺酰氯
参考文献:Design And Synthesis Of Benzenesulfonamide Derivatives As Potent Anti-Influenza Hemagglutinin Inhibitors
标题:Design And Synthesis Of Benzenesulfonamide Derivatives As Potent Anti-Influenza Hemagglutinin Inhibitors
摘要:Structural Optimization Of Salicylamide-Based Hemagglutinin (Ha) Inhibitor 1 Resulted In The Identification Of Cis-3-(5-Hydroxy-1,3,3-Timethylcyclohexylmethylamino)Benzenesulfonamide 28 And Its Derivatives As Potent Anti-Influenza Agents. The Lead Compound 28 And Its 2-Chloro Analogue 40 Can Effectively Prevent Cytopathic Effects (Cpe) Caused By Infection Of Influenza A/weiss/43 Strain (H1N1) With Ec(50) Values Of 210 And 86 Nm,Respectively. Mechanism Of Action Studies Indicate That 40 And Its Analogues Inhibit The Virus Fusion With Host Endosome Membrane By Binding To Ha And Stabilizing The Prefusion Ha Structure. With Significantly Improved Metabolic Stability,The Reported Series Represents The First Generation Of Orally Bioavailable Ha Inhibitors That Have A Good Selectivity Window And Potential For Further Development As Novel Anti-Influenza Agents.
Doi:10.1021/ml2000627