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Convenient Procedure for Preparing Naltrexone-15,16-3H2 and Naloxone-15-3H of High Specific Activity

Mercury(II) oxide oxidation of naltrexone (1a) and naloxone (1b) gave 15,16‐didehydronaltrexone (4a) and 15,16 didehydronaloxone (4b). Subsequent reduction of 4a with tritium gas afforded naltrexone‐15,16‐3H2 having a‐specific activity of 15.3 Ci/mmole. Subsequent equilibration of 4b with carrier free tritium oxide followed by sodium cyanoborohydride reduction yielded naloxone‐15‐3H having a specific activity of 4 Ci/mmole.

Citation

Brine, G., & Kepler, J. (1976). Convenient Procedure for Preparing Naltrexone-15,16-3H2 and Naloxone-15-3H of High Specific Activity. Journal of Labelled Compounds and Radiopharmaceuticals, 12(3), 401-408. https://doi.org/10.1002/jlcr.2580120310

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