📜2-氰基-3-氟-5-硝基吡啶1-氧化物置于铁粉,溶剂黄146体系中,用32%的收率获得产物3-氟-5-氨基吡啶-2-甲酸
参考文献:Discovery Of Novel Pyridyl Carboxamides As Potent Ccr5 Antagonists And Optimization Of Their Pharmacokinetic Profile In Rats
标题:Discovery Of Novel Pyridyl Carboxamides As Potent Ccr5 Antagonists And Optimization Of Their Pharmacokinetic Profile In Rats
摘要:A Novel Series Of Pyridyl Carboxamide-Based Ccr5 Inhibitors Was Designed,Synthesized,And Demonstrated To Be Highly Potent Against Hiv-1 Infection In Both Hos And Pbl Assays. Attempts To Evaluate This Series Of Compounds In A Rat Pk Model Revealed Its Instability In Rat Plasma. A Hypothesis For This Liability Was Proposed,And Strategies To Overcome This Issue Were Pursued,Leading To Discovery Of Highly Potent 40 And 41,Which Featured Dramatically Improved Rat Pk Profiles. (C) 2011 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmcl.2011.08.080