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Abstract
E-mail: hongjh@chosun.ac.krReceived December 5, 2012, Accepted December 20, 2012Efficient synthetic route to novel 2'-spirocyclopropanoid 4'-deoxythreosyl phosphonic acid nucleosides wasdescribed from 1,4-dihydroxy-2-butene. Cyclopropane moiety was prepared via ester enolate alkylation using(2-chloroethyl)dimethylsulfonium iodide. Synthesized nucleoside analogues 16, 19, 23 and 26 were tested foranti-HIV activity as well as cytotoxicity. However, none of them showed any anti-HIV activity or cytotoxicityup to 100 ”M.Key Words : Antiviral agent, Spironucleoside, Deoxythreosyl nucleoside, Phosphonic acid nucleosideIntroductionPhosphorus-modified nucleoside analogues, bearing aphosphonate group in the sugar moiety, have shown potentantiviral activity.
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