The preparation of tritium labeled methadone and its metabolites
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.
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