以（间氯）苯甲酰基保护的2'-脱氧-2'-β-氟-4'-叠氮尿苷为起始原料，经过硝酸铈铵（CAN）介导的卤代、三氮唑活化、胺化、脱保护合成了一系列5-卤代的2'-脱氧-2'-β-氟-4'-叠氮嘧啶核苷类化合物.体外生物活性评价研究表明，5-氯代（6a）和5-碘代（6c）核苷衍生物具有很好的抗乙肝病毒活性，而且细胞毒性较小.
郭美超
,
康进峰
,
侯姣
,
张倩倩
,
于文全
,
常俊标
. 5-卤代-2'-脱氧-2'-β-氟-4'-叠氮嘧啶核苷的合成与抗乙肝病毒活性研究[J]. 有机化学, 2020
, 40(1)
: 221
-225
.
DOI: 10.6023/cjoc201907054
A series of 5-halogenated 2'-deoxy-2'-β-fluoro-4'-azido pyrimidine nucleosides were synthesized from m-chloro-benzoyl protected 2'-deoxy-2'-β-fluoro-4'-azido uridine via ammonium cerium nitrate (CAN)-mediated halogenation, activation by triazole, amination, and deprotection. In vitro biological evaluation demonstrated that 5-chloro (6a) and 5-iodo (6c) nucleoside derivatives possess potent anti-HBV (hepatitis B virus) activity with low cytotoxicity.
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