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.
Ahmadibeni, Y., C. Dash, M. J. Hanley, S. F. J. Le Grice, H. K. Agarwal, and K. Parang. "Synthesis of nucleoside 5′-O-α, β-methylene-β-triphosphates and evaluation of their potency towards inhibition of HIV-1 reverse transcriptase." Organic & biomolecular chemistry 8, no. 6 (2010): 1271-1274.
Royal Society of Chemistry