Haraguchi Kazuhiro, Itoh Yoshiharu, Takeda Shingo, Honma Yosuke, Tanaka Hiromichi, Nitanda Takao, Baba Masanori, Dutschman Ginger E, Cheng Yung-Chi
School of Pharmaceutical Sciences, Showa University, Shinagawa-ku, Tokyo, Japan.
Nucleosides Nucleotides Nucleic Acids. 2004;23(4):647-54. doi: 10.1081/NCN-120030721.
A new anti-HIV agent 4'-cyano-2',3'-didehydro-3'-deoxythymidine (9) was synthesized by allylic substitution of the 3',4'-unsaturated nucleoside 14, having a leaving group at the 2'-position, with cyanotrimethylsilane in the presence of SnCl4. Evaluation of the anti-HIV activity of 9 showed that this compound is much less potent than the recently reported 2',3'-didehydro-3'-deoxy-4'-(ethynyl)thymidine (1).
一种新的抗艾滋病毒药物4'-氰基-2',3'-二脱氢-3'-脱氧胸苷（9）通过在四氯化锡存在下，使在2'-位带有离去基团的3',4'-不饱和核苷14与氰基三甲基硅烷进行烯丙基取代反应合成。对9的抗艾滋病毒活性评估表明，该化合物的效力远低于最近报道的2',3'-二脱氢-3'-脱氧-4'-(乙炔基)胸苷（1）。
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