(1RS,1'S)-PEAQX
Chemical Name: 1-[1(S)-(4-Bromophenyl)ethylamino]-1-(2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-yl)methylphosphonic acid
项目整合开发状态: Preclinical
项目研究机构: Novartis (Originator)
合成路线:Condensation of the quinoxaline aldehyde (I) with (S)-4-bromo-alpha-methylbenzylamine (II) produces imine (III).To this is added phosphinic acid dimethyl trimethylsilyl ester,generated in situ from dimethyl phosphite and chlorotrimethylsilane,to furnish the alpha-amino phosphonate (IV).Finally,hydrolysis of the methyl phosphonate and methoxy groups of (IV) under acidic conditions leads to the title compound
📌 参考资料/链接:
参考文献标题:5-Phosphonomethylquinoxalinediones as competitive NMDA receptor antagonist with a preference for the human 1A/2A,rather than 1A/2B receptor composition
文献作者:Auberson,Y.P.; Allgeier,H.; Bischoff,S.; Lingenhoehl,K.; Moretti,R.; Schmutz,M.
参考来源:Bioorg Med Chem Lett 2002,12(7),1099