Easy-to-Implement Hydrogen Isotope Exchange for the Labeling of <i>N</i>-Heterocycles, Alkylkamines, Benzylic Scaffolds, and Pharmaceuticals
Etienne Levernier, Kevin Tatoueix, Sébastien Garcia‐Argote, V. F. Pfeifer, Ralf Kiesling, Edmond Gravel, Sophie Feuillastre, Grégory Pieters
Abstract
)-H activation processes. In this easy-to-implement labeling process, Rh nanocatalysts are formed by decomposition of a commercially available rhodium dimer under a deuterium or tritium gas atmosphere (1 bar or less), using the substrate itself as a surface ligand to control the aggregation state of the resulting metallic clusters. It is noteworthy that the size of the nanoparticles observed is surprisingly independent of the substrate used and is homogeneous, as evidenced by transmission electron microscopy experiments. This method has been successfully applied to the one-step synthesis of (1) deuterated pharmaceuticals usable as internal standards for MS quantification and (2) tritiated drug analogues with very high molar activities (up to 113 Ci/mmol).