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新产品编号:1125311

Chemical Name: N-(6-Ethyl-7-nitro-2,3-dioxo-1,2,3,4-tetrahydroquinoxalin-5-ylmethyl)-N-methylglycine
项目整合开发状态: Biological Testing
项目研究机构: Pfizer (Originator)
合成路线:Hofmann degradation of tetrahydroisoquinoline (I) with ethyl bromoacetate in the presence of K2CO3 in refluxing acetone produced benzylamine derivative (II).Catalytic hydrogenation of the vinyl and nitro groups of (II) in the presence of Pd/C yielded phenylenediamine (III).This was cyclized with oxalic acid in 2 N HCl at 90 C to afford quinoxalinedione (IV).Finally,nitration of (IV) using KNO3 in cold H2SO4 gave the title compound.
📌 参考资料/链接:
参考文献标题:Design and synthesis of novel quinoxaline-2,3-dione AMPA/GlyN receptor antagonists: Amino acid derivatives
文献作者:Nikam,S.S.; Cordon,J.J.; Ortwine,D.F.; Heimbach,T.H.; Blackburn,A.C.; Vartanian,M.G.; Nelson,C.B.; Schwarz,R.D.; Boxer,P.A.; Rafferty,M.F.
参考来源:J Med Chem 1999,42(12),2266