2',3'-双脱氧尿苷的合成

摘要

2' and 3'-hydroxyl groups of uridine is protected by trimethyl orthoformate.The resulting 2',3'-O-(methoxymethylene)uridine is then treated with acetyl bromide to give 3',5'-di-O-acetyl-2'-bromo2'-deoxyuridine,which,after debromination in DMF by zinc-copper couple,catalytic hydrogenation and alcoholysis under basic condition,gives the desired 2',3'-dideoxyuridine.%以价廉易得的尿苷为原料,经原甲酸三甲酯选择性地保护2'和3 '位的羟基,得到的2 ',3'-O-甲氧甲叉尿苷与乙酰溴反应制得溴代核苷衍生物,再经脱溴、脱乙酰氧基成烯,催化氢化还原,碱性条件下醇解得到2 ',3 '-双脱氧尿苷.