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Iron-catalysed tritiation of pharmaceuticals.

Title	Iron-catalysed tritiation of pharmaceuticals.
Authors	Renyuan Pony Yu, David Hesk, Nelo Rivera, István Pelczer, Paul J Chirik
Magazine	Nature
Date	01/14/2016
DOI	10.1038/nature16464
Introduction	A thorough understanding of a drug's pharmacokinetic and pharmacodynamic characteristics within animal models is essential for drug development. These evaluations are conducted both in vivo and in vitro across various stages of development, from preclinical absorption, distribution, metabolism, and excretion (ADME) studies to advanced human clinical trials. The objective is to clarify a drug molecule's metabolic profile and assess its toxicity. Radiolabelled compounds, particularly those containing (14)C or (3)H isotopes, serve as effective and commonly used diagnostic tools for these assessments. Introducing radiolabels through synthetic chemistry allows for direct tracking of the drug molecule without substantially altering its structure or function. Given the prevalence of C-H bonds in drugs and the relative simplicity and cost-effectiveness of tritium ((3)H), it remains an ideal radioisotope for early ADME studies in the drug development process. This paper presents an iron-catalysed method for the direct (3)H labelling of pharmaceuticals via hydrogen isotope exchange, utilising tritium gas as the radioisotope source. The iron catalyst displays site selectivity that differs from current iridium catalysts, enabling isotopic labelling at complementary positions within drug molecules and thus providing additional diagnostic capability in drug development.
Quote	Renyuan Pony Yu, David Hesk and Nelo Rivera et al. Iron-catalysed tritiation of pharmaceuticals.. Nature. 2016. Vol. 529(7585). DOI: 10.1038/nature16464
Element	Hydrogen (H) , Carbon (C) , Iridium (Ir)
Topics	Biomedical Materials
Industry	Pharmaceutical Industry , Chemical & Pharmacy , Research & Laboratory

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