Liu Xiao, Xia Xueliang, Sun Chenghai, Lin Cai, Zhou Yiqian, Hussain Muzammal, Tang Fei, Liu Lu, Li Xue, Zhang Jiancun
a Institute of Pharmaceutical Research , South China Normal University , Guangzhou , Guangdong , PR China.
b Guangzhou Institutes of Biomedicine and Heath , Chinese Academy of Sciences , Guangzhou , PR China.
Nucleosides Nucleotides Nucleic Acids. 2016 Sep;35(9):479-94. doi: 10.1080/15257770.2016.1202965. Epub 2016 Aug 11.
The preparation of 2'-deoxy-2'-siprodifluorocyclopropany-lnucleoside analogs has been achieved from α-d-glucose in several steps. The key step in the synthesis was the introduction of the difluorocyclopropane through a difluorocarbene type reaction at the 2'-position. Then, a series of novel 2'-deoxy-2'-spirodifluorocyclopropanyl nucleoside analogs were synthesized using the Vorbrüggen method. All the synthesized nucleosides were characterized and subsequently evaluated against hepatitis C and influenza A virus strains in vitro.
已通过几步反应从α-d-葡萄糖制备出2'-脱氧-2'-螺二氟环丙基核苷类似物。合成中的关键步骤是通过二氟卡宾型反应在2'-位引入二氟环丙烷。然后，使用Vorbrüggen方法合成了一系列新型的2'-脱氧-2'-螺二氟环丙基核苷类似物。对所有合成的核苷进行了表征，并随后在体外针对丙型肝炎病毒和甲型流感病毒株进行了评估。
