9-(2-膦酰甲氧乙基)腺嘌呤的合成

Synthesis of 9-(2-phosphonomethoxylethyl)adenine

9-(2-膦酰甲氧乙基)腺嘌呤是核苷类抗病毒药物阿德福韦酯合成的重要关键的中间体。为了改进阿德福韦酯的合成工艺,以腺嘌呤为起始原料,经烃化反应、水解反应两步制得9-(2-膦酰甲氧乙基)腺嘌呤,总收率约为30.3%。改进后的合成路线原料价廉易得,简化了操作步骤,优化了反应条件,降低了成本,提高了收率,具有较大的工业生产价值。

9-(2-phosphonomethoxylethyl)adenine is one kind of very important medical intermediates of Adefovir dipivoxil.9-(2-phosphonomethoxylethyl)adenine was synthesized by two steps of alkylation and hydrolysis with adenine as the starting materials.The improved process was easier,the raw materials were cheap and easy to obtain,and the total yield was high,which was suitable for industrial production.The total reaction yield was 30.3%.