替比夫定的合成

Synthesis of Telbivudine

L-核糖经1-位甲基化、乙酰化保护、糖苷化和脱保护制得1-(β-L-呋喃核糖基)-5-甲基尿嘧啶(7),7与丙酰溴进行酰化溴代、次磷酸脱溴,最后脱除糖基上保护基制得抗病毒药替比夫定,总收率约23%(以L-核糖计)。

Telbivudine, an antiviral agent, was synthesized from L-ribose by methylation, protection, reaction with silyl-5-methyluracil and deprotection to give 1-（β-L-ribofuranosyl）-5-methyluracil, which was subjected to acylation and bromination with propionyl bromide, debromination with hypophosphorous acid and then deprotection with an overall yield of about 23 % （based on L-ribose）.