新型2,2'-缩水-L-苏糖嘧啶膦酸核苷的合成  

Synthesis of Novel 2,2'-Anhydro-L-threosylpyrimidine Phosphonates

作　　者：朱传涛 王松 赵一凡 Herdewijn Piet 刘丰五 Zhu Chuantao;Wang Song;Zhao Yifan;Herdewijn Piet;Liu Fengwu(XNA Platform,Institute of Pharmaceutical Sciences,Zhengzhou University,Zhengzhou 450001;Key Laboratory of Advanced Drug Preparation Technologies,Ministry of Education,Zhengzhou University,Zhengzhou 450001;Medicinal Chemistry,Rega Institute for Medical Research,KU Leuven,Herestraat 49,3000,Leuven)

机构地区：[1]郑州大学药物研究院、XNA生物医学研究所,郑州450001 [2]郑州大学药物关键制备技术教育部重点实验室,郑州450001 [3]Medicinal Chemistry,Rega Institute for Medical Research,KU Leuven,Herestraat 49,3000 Leuven,Belgium

出　　处：《有机化学》2023年第9期3167-3173,共7页Chinese Journal of Organic Chemistry

摘　　要：首先通过九步反应合成了一系列L-苏糖嘧啶核苷膦酸酯. 用二乙胺基三氟化硫(DAST)处理L-苏糖嘧啶核苷膦酸酯, 分别以中高收率得到相应的2,2'-缩水-1-(L-苏糖)尿嘧啶核苷膦酸酯类似物. 对所得到的L-苏糖嘧啶核苷膦酸酯和2,2'-缩水-L-苏糖嘧啶膦酸核苷进行了初步的生物学评价, 未发现任何活性.A series of L-threoylnucleoside phosphonates were synthesized via a nine-step procedure firstly. When the L-threoylpyrimidine nucleoside phosphonate was treated by diethylaminosulphur trifluoride (DAST), all the tried pyrimidine L-threosylnucleoside phosphonate analogues produced corresponding 2,2'-anhydro-1-(L-threoyl)pyrimidine phosphonates in medium-high yields. The obtained L-threoylpyrimidine nucleoside phosphonates and 2,2'-anhydro-L-threosylpyrimidine phosphonic acids have not shown any activity by primary biological evaluations.

关 键 词：2 2'-缩水核苷 二乙胺基三氟化硫(DAST) L-苏糖嘧啶膦酸酯 

分 类 号：TQ460.1[化学工程—制药化工]