📜2-(4-硝基苯基)乙酰氯置于palladium On Activated Charcoal Lithium Aluminium Tetrahydride,氢气,碳酸氢钠,1-羟基苯并三唑一水物,N,N'-二环己基碳二亚胺体系中,用 四氢呋喃,乙醇,N,N-二甲基甲酰胺,丙酮 用作溶剂,25.0 °C,101.33 Kpa 条件下,反应 9.0H,反应生成依克立达
参考文献:Synthesis And Activity Against Multidrug Resistance In Chinese Hamster Ovary Cells Of New Acridone-4-Carboxamides
标题:Synthesis And Activity Against Multidrug Resistance In Chinese Hamster Ovary Cells Of New Acridone-4-Carboxamides
摘要:A Number Of Tricyclic Carboxamides Have Been Synthesized And Tested To Evaluate Their Ability To Reverse Multidrug Resistance In The (Chc)-C-R/5 Cell Line. Among Them The Acridone Derivatives Were The Most Potent,A Key Feature Is The Presence Of A Dimethoxybenzyl Or Phenethylamine Cationic Site,Separated From The Tricyclic Lipophilic Part By A Carbamoylphenyl Chain. Optimization Led To Compounds 2 Orders Of Magnitude More Active Than The Prototype Inhibitors Verapamil And Amiodarone. On The Basis Of In Vitro And In Vivo Activities,9,10-Dihydro-5-Methoxy-9-Oxo-N-[4-[2-(1,2,3,4-Tetrahydro-6,7-Dimethoxyisoquinol-2-yl)Ethyl]Phenyl]-4-Acridinecarboxamide (84) Has Been Selected For Further Development.
Doi:10.1021/jm00013A017