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

Abstract

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.

Keywords: COware gas reactor; GlyT1 inhibitor; [3H]Org24598; [3H]fluoxetine; [3H]methyl iodide preparation; [3H]methylation; [3H]thioanisol.