Synthesis and Evaluation of 2'-Deoxy-2'-Spirodiflurocyclopropyl Nucleoside Analogs
Xiao Liu1, Xueliang Xia1, Chenghai Sun1
1a Institute of Pharmaceutical Research , South China Normal University , Guangzhou , Guangdong , PR China.
Nucleosides, Nucleotides & Nucleic Acids
|August 25, 2016
Abstract:
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.
