The synthesis of a benzamidine-containing NR2B-selective NMDA receptor ligand labelled with tritium or fluorine-18

摘要

A novel tritium or fiourine-18-labelled benzamidine-containing NR2B-selective NMDA receptor ligand has been synthesized. This compound was designed to contain the fluoromethoxy group to allow for the synthesis of a high specific activity, fluorine- 18-labelled PET tracer for imaging studies of the NR2B receptor. In addition to the fluorine-18-labelled compound, this compound was also tritium labelled. The tritiated ligand (11 Ci/mmol) was synthesized by a gas tritiation reaction of an aryl bromide precursor. The fluorine-18 ligand (2916 Ci/mmol), which was deuterated in the fluoromethoxy group to aid in metabolic stability, was synthesized by alkylating a phenolic precursor with [18F]fluoromethylbromide-d_2.