Tritium chemistry: history, current status and future developments; a brief review

Efficient tritiation of the translocator protein (18 kDa) selective ligand DPA‐714

“…Also, as it is the case for all these radioisotopes, positron emission will give rise to two 511‐keV antiparallel γ ‐rays, thus requiring specific handling precautions and infrastructures to limit the operator radiation dose. On the other hand, β ‐decaying long‐lived radioisotopes, such as tritium (T 1/2 : 12.32 years, E β ‐ max : 18.6 keV), remains the radionuclide of choice for preparing isotopically radiolabelled compounds and then accessing drug absorption, distribution, metabolism and excretion parameters or performing selected binding assays …”

“…On the other hand, β-decaying long-lived radioisotopes, such as tritium (T 1/2 : 12.32 years, Eβmax : 18.6 keV), remains the radionuclide of choice for preparing isotopically radiolabelled compounds and then accessing drug absorption, distribution, metabolism and excretion parameters or performing selected binding assays. 15,16 The aim of the present work was to prepare a tritium, isotopically labelled, version of DPA-714 ([ 3 H]DPA-714 (1d)), in order to support the development of the corresponding PET probe, seeking for alternative and additional information on this ligand and especially its binding to the TSPO, as well as bridging in vitro and in vivo studies performed with this tracer. A special care was given to the expected positioning of the tritium atoms in regard of the known in vivo metabolism of the tracer and to the selection of a tritiation synthesis pathway and process allowing the simultaneous introduction of theoretically two radioactive atoms, for an optimal value of specific radioactivity (SRA).…”

Rapid Protium–Deuterium Exchange of 4-Aminopyridines in Neutral D2O under Microwave Irradiation

“…3 H/D exchange is a valuable analytical tool in its own right in protein dynamics 8,9 and can serve as a useful model for analytical techniques involving protium-tritium exchange. 1,10,11 As a synthetic tool, H/D-exchange experiments received intensive study in the 1960s and 1970s, 5,6 leading to a number of advances in pH-dependent and metal-catalyzed processes. 12 With the recent development of higher performance mass spectrometers, and a renaissance of interest in C-H bond activation, 13 a plethora of H/D-exchange methods has now emerged, some using C-H activation technology.…”

Rhodium-Catalyzed, Efficient Deutero- and Tritiosilylation of Carbonyl Compounds from Hydrosilanes and Deuterium or Tritium

“…As already noted, , of the basic methods for introducing tritium (or deuterium) into organic molecules, synthetic procedures such as, for example, reductions with a hydride source (e.g., labeled borohydrides, organotinhydrides, etc.) are convenient as they provide high T- or D-incorporation, although they find important limitations by the chemistry required.…”

“…are convenient as they provide high T- or D-incorporation, although they find important limitations by the chemistry required. This has restricted so far the use of labeled hydrosilanes. , Hydrosilanes constitute one of the most powerful tools in synthetic organic chemistry . For example, the catalytic hydrosilylation of carbonyl functionalities is an extremely useful industrial and laboratory method for the synthesis of a wide range of organosilicon compounds. − The process combines in one step selective regiocontrol by formation of a C–H bond with protection of the alcohol as an alkoxysilane.…”