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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%。
Objective To improve the synthetic process of antiviral drug telbivudine. Methods L-arabinose was used as the starting material to synthesize the target compound by addition-cyclization, substitution, cyclization isomerisation, protection of halogenation, dehalogenation and hydrolysis in 6 steps. Results and Conclusions The structures of target compounds were confirmed by 1H-NMR, IR and MS spectra. The improved process does not require purification by column chromatography. The method has the advantages of low cost, simple operation and suitable for industrialized production, and the total yield can reach 32.6%.