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A polymer-bound α,β-methylene-β-triphosphitylating reagent was synthesized and subjected to reactions with unprotected nucleosides, followed by oxidation, deprotection of cyanoethoxy groups, and acidic cleavage to afford nucleoside 5′-O-α,β-methylene-β-triphosphates. Among all the compounds, cytidine 5′-O-α,β-methylene-β-triphosphate inhibited RNase H activity of HIV-1 reverse transcriptase with a Ki value of 225 μM.


This is a pre-copy-editing, author-produced PDF of an article accepted for publication in Organic & Biomolecular Chemistry, volume 8, issue 6, 2010following peer review. The definitive publisher-authenticated version is available online at DOI: 10.1039/b922846b.


Royal Society of Chemistry



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