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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。
Using 2-benzyloxyethanol as raw material, the key intermediate 2- (2-bromoethyl) -1,3-propanediol diacetic acid was synthesized by the reaction of Appel bromination, condensation, reduction, acetylation, deprotection and bromination Ester and condensation with 2-amino-6-chloropurine, purified by crystallization to give 9- (4-acetoxy-3-acetoxymethylbutyl) -2-amino-6-chloropurine, (Total yield of 32%), but also hydrolyzed penciclovir (total yield of 37%, 2-benzyloxyethanol). All intermediates and products purified simple, easy to operate, suitable for industrial production amplification.