2-溴-5-硝基-3-甲基吡啶置于铁粉,溶剂黄146体系中,用 水 作为反应溶剂,化学反应 1.0H,以100%的收率获得产物5-氨基-2-溴-3-甲基吡啶 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
专利号:US-2024309003-A1 优先权日:2021-05-04 标题 :Heterocyclic compounds as triggering receptor expressed on myeloid cells 2 agonists and methods of use 发明人:HOUZE JONATHAN B; BOS MAXENCE; MANCUSO JOHN; FRANZONI IVAN; PANDYA BHAUMIK; KAPLAN ALAN 权利人:VIGIL NEUROSCIENCE INC 摘要:The present disclosure provides compounds of Formula I, useful for the activation of Triggering Receptor Expressed on Myeloid Cells 2 (“TREM2â€?). This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a neurodegenerative disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.