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Synthesis of carbon-14 labelled cis-2-amino-1,9-dihydro-9-[4-(hydroxymethyl)-2-cyclopenten-1-yl]-6H-purine-6-one; [8-14C]carbovir
A promising anti-aids drug
Gopinathan, M., & Kepler, J. (1991). Synthesis of carbon-14 labelled cis-2-amino-1,9-dihydro-9-[4-(hydroxymethyl)-2-cyclopenten-1-yl]-6H-purine-6-one; [8-14C]carbovir: A promising anti-aids drug. Journal of Labelled Compounds and Radiopharmaceuticals, 29(6), 645-649. https://doi.org/10.1002/jlcr.2580290605
The synthesis of the title compound (3) is described. Treatment of a solution of triethyl [14C]orthoformate in dry chloroform with cis‐[4‐(2,5‐diamino‐6‐chloro‐4‐pyrimidinyl)‐amino]‐2‐cyclopentenyl carbinol (1) afforded crude 2. Hydrolysis of crude 2 with 2 N sodium hydroxide gave 3 in 34% overall radiochemical yield with specific activity of 19.6 mCi/mmol.