2-氨基-6-环丙胺基-9H-嘌呤的合成  

Synthesis of 2-Amino-6-cyclopropylamino-9H-purine

作　　者：周惠良[1] 胡奇林[1] 赵庆山[1] 刘万毅[1] 

机构地区：[1]宁夏大学化学与化工学院,宁夏银川750021

出　　处：《中国医药工业杂志》2008年第11期811-813,共3页Chinese Journal of Pharmaceuticals

基　　金：国家973前期预研项目(2006CB708606)

摘　　要：氰乙酸乙酯经亚硝化、与盐酸胍在乙醇钠存在下缩合闭环、Pd/C催化还原得2,4,5-三氨基-6-羟基嘧啶,与甲酸环合得鸟嘌呤,再经乙酰化、氯化、与环丙胺缩合得到抗病毒药阿巴卡韦中间体2-氨基-6-环丙胺基-9H-嘌呤,总收率约39%。2-Amino-6-cyclopropylamino-9H-purine, the key intermediate of abacavir was synthesized from ethyl cyanoacetate by nitrosation, cyclization with guanidine hydrochloride in the presence of EtONa and reduction to give 2,4,5-triamino-6-hydroxypyrimidine, which was subjected to cyclization with formic acid, acylation, chlorination and condensation with cyclopropylamine with an overall yield of about 39 %.

关 键 词：2-氨基-6-环丙胺基-9H-嘌呤 阿巴卡韦 中间体 合成 

分 类 号：O626[理学—有机化学]