📜1,4-二氯-2-碘苯置于platinum(Iv) Oxide Palladium Diacetate,三氯化铝,氯化亚砜,氢气,三乙胺体系中,用 二硫化碳,乙酸乙酯,乙腈 作为反应溶剂,化学反应 53.0H,反应生成 4,7-二氯-1-茚酮
参考文献:Synthesis And Sar Of Novel Di-And Trisubstituted 1,4-Dihydroquinoxaline-2,3-Diones Related To Licostinel (Acea 1021) As Nmda/glycine Site Antagonists
标题:Synthesis And Sar Of Novel Di-And Trisubstituted 1,4-Dihydroquinoxaline-2,3-Diones Related To Licostinel (Acea 1021) As Nmda/glycine Site Antagonists
摘要:A Series Of Novel Di-And Trisubstituted 1,4-Dihydroquinoxaline-2,3-Diones (Qxs) Related To Licostinel (Acea 1021) Was Synthesized And Evaluated As Antagonists For The Glycine Site Of The N-Methyl-D-Asparate (Nmda) Receptor. The In Vitro Potency Of These Antagonists Was Determined By Displacement Of The Glycine Site Radioligand [h-3]-5,7-Dichlorokynurenic Acid ([h-3]Dcka) In Rat Brain Cortical Membranes. Structure-Activity Relationship Studies Indicate That A Cyano Group Is A Good Replacement For The Nitro Group In The 5-Position Of Licostinel While 5-Carboxy,5-Ester,5-Ketone And 5-Amide Derivatives Showed Reduced Potency. 5,6-Cyclized Analogues Of Licostinel Also Showed Significantly Reduced Potency. Among The Trisubstituted Qxs Investigated,5-Cyano-6,7-Dichloro Qx And 5-Cyano-7-Chloro-6-Methyl Qx Are The Most Potent With Ic50 Values Of 32 Nm And 26 Nm,Respectively. (C) 2003 Elsevier Science Ltd. All Rights Reserved.
DOI:10.1016/s0968-0896(03)00059-2