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Synthesis of [ 2 H 3 ]‐labelled sulfamethoxazole and its main urinary metabolites
Author(s) -
Heinkele Georg,
Mürdter Thomas E.
Publication year - 2007
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.1375
Subject(s) - chemistry , sulfamethoxazole , yield (engineering) , metabolite , medicinal chemistry , nuclear chemistry , radiochemistry , chromatography , biochemistry , antibiotics , materials science , metallurgy
Sulfamethoxazole was labelled at positions 3, 5, and 4′ by H/D exchange in a mixture of 5% 2 H 2 SO 4 and 95% 2 H 2 O (v/v) under reflux for 72h with good isotope incorporation and acceptable yield. Subsequently, [ 2 H 3 ]‐sulfamethoxazole‐ N 1 ‐glucuronide and [ 2 H 3 ]‐ N 4 ‐acetyl‐sulfamethoxazole were synthesized. Copyright © 2007 John Wiley & Sons, Ltd.