抗病毒药替比夫定的合成工艺研究

Synthetic process of telbivudine,an antivirus agent

目的改进抗病毒药替比夫定(telbivudine)的合成工艺。方法以L-阿拉伯糖为起始原料,经加成环合、取代、环合异构、保护卤代、脱卤、水解共6步反应合成目标化合物。结果与结论目标化合物的结构经1H-NMR、IR、MS谱确证。改进后的工艺无需柱色谱纯化,成本低廉,操作简便,适合工业化生产,总收率可达32.6%。

Aim To improve the synthetic process of telbivudine, an anfivirus drug. Methods The title compound was synthesized from L-arabinose via addition and cyclization, substitution, cyclization and isomerization,protection and halogenation, debalogenation,hydrolysis added up to six steps. Results and contusion The structure of telbivudine was confirmed by ^1 H-NMR, IR and MS. The improved process is suitable for industrial preparation and more practicaI owing to its advantages of low cost, convenient operations without column chromatography and good yield of 32.6%.