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The preparation of tritium labeled methadone and its metabolites
Seltzman, H., Wyrick, S. D., & Pitt, C. (1981). The preparation of tritium labeled methadone and its metabolites. Journal of Labelled Compounds and Radiopharmaceuticals, 18(9), 1365-1377. https://doi.org/10.1002/jlcr.2580180913
The synthesis and catalytic tritium reduction of 1,2‐dehydro analogs of (‐)‐methadol, (‐)‐α‐acetylmethadol, and (‐)‐α‐acetyl‐N‐normethadol afforded the labeled compounds with high specific activity (44‐60 Ci/ mmole). The use of the homogeneous catalyst (ϕ3P)3RhCl resulted in specific introduction of tritium without scrambling. (+)‐Methadone‐1‐3H (25 Ci/mmole) was obtained by oxidation of (‐)‐methadol‐1,2‐3H2 followed by sodium hydroxide exchange of the 2‐3H.