摘要
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^(13)C 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.
出处
《精细石油化工》
CAS
CSCD
北大核心
2016年第3期74-78,共5页
Speciality Petrochemicals
基金
国家自然科学基金(21172059)
河南省高等学校重点科研项目(16A150042)
关键词
阿德福韦酯
微波促进
6-氯嘌呤
合成方法
adefovir dipivosil
microwave irradiation
6-chloropurine
synthetic methods
