阿德福韦酯的合成  

Synthesis of Adefovir Dipivoxil

作　　者：蒋晔[1] 徐智儒[1] 张丽芳[2] 张晓青[1] 

机构地区：[1]河北医科大学药学院,河北石家庄050017 [2]河北医科大学制药厂,河北石家庄050017

出　　处：《中国医药工业杂志》2007年第1期4-6,共3页Chinese Journal of Pharmaceuticals

摘　　要：用亚磷酸二乙酯和多聚甲醛经缩合、酯化得到对甲苯磺酸二乙氧基磷酰基甲酯(6)。另用腺嘌呤和碳酸亚乙酯反应得到9-(2-羟乙基)腺嘌呤,与6在NaH作用下缩合后,经水解、酰化等反应制得抗病毒药阿德福韦酯,总收率18%。Adefovir dipivoxil was synthesized by reaction of adenine and ethylene carbonate to give 9-（hydroxyethyl） adenine, which was subjected to condensation with 4-toluenesulfonic acid diethoxyphosphorylmethyl ester （6） in presence of Nail, hydrolysis and then acylation with an overall yield of 18 % （base on adenine）. Compound 6 was prepared from diethyl phosphate and paraformaldehyde by condensation and esterification.

关 键 词：阿德福韦酯 核苷类似物 合成 

分 类 号：R978.7[医药卫生—药品]