羟乙基吡咯烷酮尿嘧啶的合成

Synthesis of Hydroxyethylpyrrolidonyluracil

报道了一种新的氮杂核苷类似物：羟乙基吡咯烷酮尿嘧啶（８）的合成．以丁二酐和２－氨基乙醇为原料，经酰化、环合、还原及烃氧基化反应制得１－乙酰氧乙基－５－乙氧基－２－吡咯烷酮（６），在四氯化钛存在下与三甲基硅尿嘧啶缩合，得到乙酰氧乙基吡咯烷酮尿嘧啶（７），在氨－甲醇体系中去乙酰基得到目的物：羟乙基吡咯烷酮尿嘧啶（８）．

Synthesis of a novel aza nucleoside analogue, 1 (1 (2 hydroxyethyl) 2 pyrrolidon 5 yl) uracil (8), was described. The intermediate (6) was obtained by acylation of 2 aminoethanol with succinic anhydride,followed by cyclization, reduction and alkoxylation. Condensation of (6) with TMSU in presence of TiCl 4 produced 1 (1 (2 acetoxyethyl) 2 pyrrolidon 5 yl) uracil (7). Deacylation of (7) gave final product (8).