📜5-溴-2-甲氧基吡啶置于盐酸,正丁基锂,水体系中,用 四氢呋喃,正己烷 作为反应溶剂,化学反应 2.16H,反应生成 4-羟基-4-(6-甲氧基吡啶-3-基)环己酮
参考文献:Discovery Of Incb3284,A Potent,Selective,And Orally Bioavailable Hccr2 Antagonist
标题:Discovery Of Incb3284,A Potent,Selective,And Orally Bioavailable Hccr2 Antagonist
摘要:We Report The Identification Of 13 (Incb3284) As A Potent Human Ccr2 (Hccr2) Antagonist. Incb3284 Exhibited An Ic50 Of 3.7 Nm In Antagonism Of Monocyte Chemoattractant Protein-1 Binding To Hccr2,An Ic50 Of 4.7 Nm In Antagonism Of Chemotaxis Activity,An Ic50 Of 84 Mu M In Inhibition Of The Herg Potassium Current,A Free Fraction Of 58% In Protein Binding,High Selectivity Over Other Chemokine Receptors And G-Protein-Coupled Receptors,And Acceptable Oral Bioavailability In Rodents And Primates. In Human Clinical Trials,Incb3284 Exhibited A Pharmacokinetic Profile Suitable For Once-A-Day Dosing (T-1/2 = 15 H).
DOI:10.1021/ml200030Q