📜3-氨基-2-氯吡啶置于正丁基锂,四甲基乙二胺,Sodium Hexamethyldisilazane,三氟乙酸,三氯氧磷体系中,用 四氢呋喃,正己烷,二氯甲烷 用作溶剂,化学反应 22.0H,反应生成4,8-二氯吡啶并[3,4-D]嘧啶
参考文献:Design And Evaluation Of Novel 8-Oxo-Pyridopyrimidine Jak1/2 Inhibitors
标题:Design And Evaluation Of Novel 8-Oxo-Pyridopyrimidine Jak1/2 Inhibitors
摘要:A Highly Ligand Efficient,Novel 8-Oxo-Pyridopyrimidine Containing Inhibitor Of Jak1 And Jak2 Isoforms With A Pyridone Moiety As The Hinge-Binding Motif Was Discovered. Structure-Based Design Strategies Were Applied To Significantly Improve Enzyme Potency And The Polarity Of The Molecule Was Adjusted To Gain Cellular Activity. The Crystal Structures Of Two Representative Inhibitors Bound To Jak1 Were Obtained To Enable Sar Exploration. (C) 2013 Published By Elsevier Ltd.
Doi:10.1016/j.Bmcl.2013.08.082