泛昔洛韦和喷昔洛韦的合成工艺改进  

An Improved Synthetic Process of Famciclovir and Penciclovir

作　　者：金鑫[1] 计立[1] 陈文霞[1] 钱武[1] 沈大冬[1] 

机构地区：[1]浙江医药股份有限公司研究院,浙江新昌312500

出　　处：《中国医药工业杂志》2016年第11期1352-1356,共5页Chinese Journal of Pharmaceuticals

摘　　要：以2-苄氧基乙醇为原料,经Appel溴代反应、缩合、还原、乙酰化、脱保护及溴化得关键中间体2-(2-溴乙基)-1,3-丙二醇二乙酸酯,与2-氨基-6-氯嘌呤缩合,经结晶纯化得9-(4-乙酰氧基-3-乙酰氧甲基丁基)-2-氨基-6-氯嘌呤,还原脱氯得泛昔洛韦(总收率32%),也可水解得喷昔洛韦(总收率37%,以2-苄氧基乙醇计)。所有中间体和产物纯化简单,操作简便,适合工业化放大生产。The key intermediate 2-（2-bromoethyl）propane-1,3-diyl diacetate was prepared via Appel bromination, condensation, reduction, acetylation, deprotection and bromination with 2-benzyloxyethanol as the starting material. Then it reacted with 2-amino-6-chloropurine via condensation to give 9- （4-acetoxy-3-acetoxymethylbutyl） -2- amino-6-chloropurine （4）, after a dechlorination, an anti-herpesvirus drug famciclovir was obtained with an overall yield of 32 % （based on 2-benzyloxyethanol）, if 4 was subjected to a acidic condition, penciclovir would be prepared with an overall yield of 37 % （based on 2-benzyloxyethanol）.

关 键 词：泛昔洛韦 喷昔洛韦 喷昔洛韦N-7异构体 抗疱疹病毒药物 

分 类 号：R978.7[医药卫生—药品]