The development and use of iridium(I) phosphine systems for ortho-directed hydrogen-isotope exchange

Rapid and efficient iridium‐mediated hydrogen‐tritium exchange labeling of pharmaceutical compounds is a key methodology in the life sciences industry. A review of the development and use of iridium(I) phosphine systems for ortho‐directed isotopic exchange is described to provide the reader with a comprehensive introduction to the area and to serve as a starting point for experimental investigators. Examples of useful catalyst systems and their application to different substrates types as well as potential areas for further development are discussed. Copyright © 2010 John Wiley & Sons, Ltd. Iridium(I) phosphine containing complexes can be used for ortho‐exchange deuteration and tritiation of aromatic substrates containing the appropriate directing group (DG). The labeling takes place most efficiently in DCM and uses isotopic hydrogen gas as the isotope donor. A review of the development and use of these catalytic systems is described to serve as an introduction to the area and provide a starting point for experimental investigators. Copyright © 2010 John Wiley & Sons, Ltd.