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.
Guo Meichao
,
Kang Jinfeng
,
Hou Jiao
,
Zhang Qianqian
,
Yu Wenquan
,
Chang Junbiao
. Synthesis and Anti-HBV Evaluation of 5-Halogenated 2'-Deoxy-2'-β-fluoro-4'-azido Pyrimidine Nucleosides[J]. Chinese Journal of Organic Chemistry, 2020
, 40(1)
: 221
-225
.
DOI: 10.6023/cjoc201907054
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