3′-氧-叠氮甲基-β-胸苷的合成

Synthesis of 3′-O-azidomethyl-β-thymidine

以特戊酰基选择性保护β-胸苷的5′-羟基,再将3′-羟基硫甲基甲基化;然后以磺酰氯将硫甲基甲基氯代后再与叠氮钠反应,最后用碳酸钠脱掉保护基合成了3′-氧-叠氮甲基β-胸苷,其结构经1H NMR表征。

First,5′-hydroxyl group of β-thymidine was pivaloylated selectively,then the 3′-hydroxyl group was methylthiomethylated.The thiomethyl group was chlorinated by SO2Cl2,and then the chloride group was substituted by azide.Finally,5′-protecting group was removed by K2CO3 in methanol to give the desired product 3′-O-azidomethyl-β-thymidine.