Synthesis of [ 3 H]Org24598 using in-house prepared [ 3 H]MeI.

The synthesis of tritium-labelled glycine transporter 1 inhibitor Org24598 is reported. Because of the instability of the Org24598 skeleton under hydrogenation conditions, a synthetic approach using an in-house prepared tritium-labelled alkylating agent ([ 3 H]MeI, SA = 26.2 Ci/mmol) was employed. Alternative methods of labelling are discussed.