Fast and efficient tritium labelling of the nonsteroidal anti‐inflammatory drugs naproxen, tolmetin, and zomepirac

Abstract

Abstract Fast and efficient tritium labelling of the nonsteroidal anti‐inflammatory drugs naproxen, tolmetin and zomepirac is reported. Naproxen along with its ( R )‐enantiomer were labelled by catalytic tritium–halogen exchange of the corresponding 5‐bromo derivatives providing [ 3 H]naproxen with a specific activity of 25.4 Ci/mmol. Tolmetin and zomepirac were labelled by the hydrogen isotope exchange reaction using Crabtree's catalyst. This provided [ 3 H]tolmetin and [ 3 H]zomepirac with specific activities of 80.8 and 64.3 Ci/mmol, respectively. All compounds were obtained in high radiochemical purity (>98%). Copyright © 2005 John Wiley & Sons, Ltd.