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The preparation of tritium labeled methadone and its metabolites
Author(s) -
Seltzman Herbert H.,
Wyrick Steven D.,
Pitt Colin G.
Publication year - 1981
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580180913
Subject(s) - chemistry , tritium , tritium illumination , specific activity , homogeneous , catalysis , sodium hydroxide , methadone , radiochemistry , catalytic hydrogenation , nuclear chemistry , organic chemistry , enzyme , pharmacology , medicine , physics , nuclear physics , thermodynamics
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 (ϕ 3 P) 3 RhCl resulted in specific introduction of tritium without scrambling. (+)‐Methadone‐1‐ 3 H (25 Ci/mmole) was obtained by oxidation of (‐)‐methadol‐1,2‐ 3 H 2 followed by sodium hydroxide exchange of the 2‐ 3 H.