Collection of Czechoslovak Chemical Communications p. 757 - 766 (2010)
Update date:2022-08-11
Topics:
Elbert, Tomas
Brehova, Petra
Holy, Antonin
9-(2-Phosphonomethoxyethyl)-2,6-diamino-[8-3H]purine (4), 9-(2-phosphonomethoxyethyl)- [8-3H]guanine (6) and (R)-9-(2-phosphonomethoxypropyl)-[8-3H]adenine (11) with specific activities of 10.9, 7.9 and 16 Ci/mmol, respectively, were prepared by a catalytic dehalogenation of the corresponding 8-bromo derivatives 1, 2 and 9. The rate of the exchange of the tritium label on C-8 of the purine ring in title compounds with the hydrogen of water under physiological pH at 20 °C was studied using 3H NMR. The loss of 3H-label attained 7% in [8-3H]tenofovir (11), 10% in [8-3H]PMEDAP (4) and 12% in [8-3H]PMEG (6) after the period of 3 weeks. Storage at a temperature of -196 °C in liquid nitrogen ensured a better than 97% radiochemical purity of the prepared labeled compounds even after a six-month period.
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