Easy-to-Implement Hydrogen Isotope Exchange for the Labeling of N-Heterocycles, Alkylkamines, Benzylic Scaffolds, and Pharmaceuticals.

ABSTRACT: Facilitating access to deuterated and tritiated complex molecules is of paramount importance due to the fundamental role of isotopically labeled compounds in drug discovery and development. Deuterated analogues of drugs are extensively used as internal standards for quantification purposes or as active pharmaceutical ingredients, whereas tritiated drugs are essential for preclinical ADME studies. In this report, we describe the labeling of prevalent substructures in FDA-approved drugs such as azines, indoles, alkylamine moieties, or benzylic carbons by the in situ generation of Rh nanoparticles able to catalyze both C(sp²)-H and C(sp³)-H activation processes. In this easy-to-implement labeling process, Rh nanocatalysts are formed by decomposition of a commercially ava

SUBMITTER: Levernier E 

PROVIDER: S-EPMC9088292 | biostudies-literature | 2022 Apr

REPOSITORIES: biostudies-literature