Silicon compounds in carbon-11 radiochemistry: present use and future perspectives

Positron emission tomography (PET) is a powerful functional imaging technique that requires the use of positron emitting nuclides. Carbon-11 (C-11) radionuclide has several advantages related to the ubiquity of carbon atoms in biomolecules and the conservation of pharmacological properties of the molecule upon isotopic exchange of carbon-12 with carbon-11. However, due to the short half-life of C-11 (20.4 minutes) and the low scale with which it is produced by the cyclotron (sub-nanomolar concentrations), quick, robust and chemospecific radiolabelling strategies are required to minimise activity loss during incorporation of the C-11 nuclide into the final product. To address some of the constraints of working with C-11, the use of silicon-based chemistry for C-11-labelling was proposed as a rapid and effective route for radiopharmaceutical production due to the broad applicability and high efficiency showed in organic chemistry. In the past years several organic chemistry methodologies have been successfully applied to C-11-chemistry. In this short review, we examine silicon-based C-11-chemistry, with a particular emphasis on the radiotracers that have been successfully produced and potential improvements to further expand the applicability of silicon in radiochemistry.

Automated summary

PET requires positron-emitting nuclides, with C-11 being advantageous due to the ubiquity of carbon atoms in biomolecules, but quick, robust, and chemospecific radiolabelling strategies are needed due to its short half-life and low production scale. The use of silicon-based chemistry for C-11-labelling has been proposed as a rapid and effective method, showing broad applicability and high efficiency in organic chemistry.