📜3-哌啶甲酸置于sodium Hydroxide,草酰氯,N,N-二甲基甲酰胺体系中,用 二氯甲烷,水 用作溶剂,化学反应生成1-苄氧羰基哌啶-3-甲酰氯
参考文献:Ccr5 Antagonists As Anti-Hiv-1 Agents. Part 3: Synthesis And Biological Evaluation Of Piperidine-4-Carboxamide Derivatives
标题:Ccr5 Antagonists As Anti-Hiv-1 Agents. Part 3: Synthesis And Biological Evaluation Of Piperidine-4-Carboxamide Derivatives
摘要:Replacement Of The 5-Oxopyrrolidin-3-Yl Fragment In The Previously Reported Lead Structure With A 1-Acetylpiperidin-4-Yl Group Led To The Discovery Of A Novel Series Of Potent Ccr5 Antagonists. Introduction Of Small Hydrophobic Substituents On The Central Phenyl Ring Increased The Binding Affinity,Providing Low To Sub-Nanomolar Ccr5 Antagonists. The Selected Compound 11F Showed Excellent Antiviral Activity Against Ccr5-Using Hiv-1 Replication In Human Peripheral Blood Mononuclear Cells (Ec50 = 0.59 Nm) And An Acceptable Pharmacokinetic Profile In Dogs. (C) 2004 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmc.2004.10.013