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A convenient procedure for preparing naltrexone-15,16-3H2 and naloxone-15-3H of high specific activity

✍ Scribed by George A. Brine; John A. Kepler

Publisher
John Wiley and Sons
Year
1976
Tongue
French
Weight
328 KB
Volume
12
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

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‐^3^H~2~ 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‐^3^H having a specific activity of 4 Ci/mmole.

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