摘要
本研究设计以下新路线合成2'-脱氧-β-尿苷。以2-脱氧核糖为原料,经甲基化、酰化、氯代"一锅法"制得1-氯-2-脱氧-3,5-O-二(4-氯苯甲酰基)-D-核糖,然后与2,4-二(三甲硅氧基)嘧啶耦合得3',5'-O-二(4-氯苯甲酰基)-2'-脱氧-β-D-尿苷,最后经氨/甲醇溶液脱酰基制得目标化合物,总收率49.7%,纯度98.0%。
An efficient synthetic route of 2'-deoxy-β-uridine was reported. Firstly, 1-chloro-2-deoxy-3,5-Obis(4-chlorobenzoyl)-D-glucopyranoside was prepared via methylation, acylation and chloro-substitution in one-pot by using 2-desoxyribose as the starting material. And then it reacted with 2,4-bis[(trimethylsilyl)oxy]pyrimidine to afford 3',5'-O-bis(4-chlorobenzoyl)-2'-deoxy-β-D-uridine. Finally, the target compound was got smoothly through deacylation reaction in ammonia/methanol solution with an overall yield of 49.7% in 98.0% purity.
引文
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