Synthesis of deuterium-labelled elliptinium and its use in metabolic studies

Abstract

The 9-hydroxy-2-(U-2H3) methylellipticinium acetate (elliptinium) was synthesized with an isotopic purity of at least 96%. The structure was confirmed by proton nuclear magnetic resonance and direct probe fast atom bombardment mass spectrometry. A mixture of elliptinium and its deuterated analogue was administered intravenously to rats. In urine, after analysis by liquid chromatography/mass spectrometry (LC/MS), unchanged drug and N-acetylcysteinylelliptinium were found. In bile, after ion-pair extraction and LC/MS, the glutathionylelliptinium was found in addition to the parent drug and the N-acetylcysteine adduct.