Recent advances in iridium(I) catalysis towards directed hydrogen isotope exchange

Kerr, William and Paterson, Laura and Knox, Gary (2020) Recent advances in iridium(I) catalysis towards directed hydrogen isotope exchange. Journal of Labelled Compounds and Radiopharmaceuticals, 63 (6). pp. 281-295. ISSN 0362-4803 (

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The initial discovery and establishment of a family of novel iridium catalysts possessing N-heterocyclic carbene units alongside bulky phosphine ligands allowed selected substrates to be labelled using deuterium or tritium gas at desirably low catalyst loadings via an ortho-directed C-H insertion process. Such a method has broad applicability and offers distinct advantages within the pharmaceutical industry, directly facilitating the ability to carefully monitor a potential drug molecule’s biological fate. Over the past decade since these initial protocols were divulged, many additional advances have been made in terms of catalyst design and substrate scope. This review describes the broadened array of new iridium catalysts and associated protocols for direct and selective C-H activation and hydrogen isotope insertion within a number of new chemical entities of direct relevance to the pharmaceutical industry.