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Chapter 2 - Recent advances in deuterium and tritium chemistry
Hesk, D. (2026). Chapter 2 - Recent advances in deuterium and tritium chemistry. In Isotopically labeled compounds: Recent advances and emerging topics in synthesis and applications Elsevier in cooperation with RTI Press. https://doi.org/10.1016/B978-0-443-19154-1.00013-6
Hydrogen isotope exchange whereby a hydrogen on the target molecule is replaced by a deuterium or tritium with the aid of a suitable catalyst has been the dominant labeling method in pharmaceutical research over the past 15 years, specifically with homogeneous iridium(I), and continues to be the most popular method for preparation of high specific activity tritium-labeled compounds by virtue of its simplicity of setup and the increasing numbers of commercially available Ir(I) catalysts. This expanding choice of catalysts offers the possibility to deuterium- and tritium-label a much wider range of substrates than was possible with the first Heys catalyst, Crabtree's catalyst, and the first-generation Kerr catalysts. While tremendous progress has been made, limitations still exist, such as poisoning by nitrile groups and nonproductive catalyst binding with some pyridine-containing substrates. Efforts to use homogeneous Ir(I) to label peptides and proteins at high specific activity remain a work in progress.
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