Nucleosides, Nucleotides & Nucleic Acids 2006-01-01

Synthesis of 6-arylthio analogs of 2',3'-dideoxy-3'-fluoroguanosine and their effect against hepatitis B virus replication.

Takayoshi Torii, Tomoyuki Onishi, Kunisuke Izawa, Tokumi Maruyama, Yosuke Demizu, Johan Neyts, Erik De Clercq

文献索引：Nucleosides Nucleotides Nucleic Acids 25 , 655-665, (2006)

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摘要

A key compound, 2-amino-6-chlor-9-(2,3-dideoxy-3-fluoro-beta-D-erythro-pentofuranosyl)puine, was prepared from 2-amino-6-chloropurine riboside in 5 steps, then subjected to the nucleophilic displacement with benzenethiols to afford 6-arylthio congeners. These compounds showed a similar anti-HBV effect to that of 2',3' dideoxy-3'-fluoroguanosine.