Tritiation of aryl thianthrenium salts with a molecular palladium catalyst.

ABSTRACT: Tritium labelling is a critical tool for investigating the pharmacokinetic and pharmacodynamic properties of drugs, autoradiography, receptor binding and receptor occupancy studies¹. Tritium gas is the preferred source of tritium for the preparation of labelled molecules because it is available in high isotopic purity². The introduction of tritium labels from tritium gas is commonly achieved by heterogeneous transition-metal-catalysed tritiation of aryl (pseudo)halides. However, heterogeneous catalysts such as palladium supported on carbon operate through a reaction mechanism that also results in the reduction of other functional groups that are prominently featured in pharmaceuticals³. Homogeneous palladium catalysts can react chemoselectively with aryl (p

SUBMITTER: Zhao D 

PROVIDER: S-EPMC8674128 | biostudies-literature | 2021 Dec

REPOSITORIES: biostudies-literature