以廉价的次黄嘌呤为原料,经过氯代、烷基化和氨解3步反应,得到了合成阿德福韦酯的重要中间体9-(2-羟乙基)-腺嘌呤,总收率68%。微波促进将反应时间从2h缩短到10min。反应规模可以扩大到200g,且所有中间产物和目标产物的分离纯化不需要柱层析。中间体和产物的结构经^1H NMR和^13C NMR确证。该方法原料廉价易得、反应快、操作简便。
The key intermediate of adefovir dipivosil 9-(2-hdroxyethyl)-adenine was synthesized from hypoxanthine through 3steps in the total yield of 68%.The reaction time was shortened dramatically from 120 min to 10 min under microwave irradiation.The structures of intermediates and the product were confirmed by ^1H NMR and ^13C NMR spectrum.This method has the advantages of available materials,rapid process and easy handling,which make this route more attractive for industrial application.