利可替奈的合成  

Synthesis of Licostinel

作　　者：李荀[1] 胡清萍[2] 崔学桂[2] 徐文方[1] 

机构地区：[1]山东大学药学院,山东济南250012 [2]山东大学化学与化工学院,山东济南250100

出　　处：《中国医药工业杂志》2004年第8期453-454,共2页Chinese Journal of Pharmaceuticals

摘　　要：3,4-二氯苯胺经酰胺化、硝化、水解和还原反应制得4,5-二氯邻苯二胺,再经草酰化闭环、硝化反应制得NMDA受体拮抗剂利可替奈,总收率69%。Licostinel, a neuroprotective candidate was synthesized from 3,4-dichloroaniline by amidation, nitration,hydrolysis and reduction to give 4,5-dichlorobenzene-1,2-diamine which was acylated and cyclized with oxalic acidfollowed by nitration with an overall yield of 69.4%.

关 键 词：利可替奈 NMDA受体拮抗剂 合成 

分 类 号：R979.9[医药卫生—药品]