TY - JOUR
T1 - Silicon Compounds in Carbon-11 Radiochemistry: Present Use and Future Perspectives
AU - Luzi, Federico
AU - Gee, Tony
AU - Bongarzone, Salvatore
N1 - Funding Information:
King’s College London and UCL Comprehensive Cancer Imaging Centre is funded by the CRUK and EPSRC in association with the MRC and DoH (England). The research was supported by the Wellcome’s Multi-User Equipment ‘A multiuser radioanalytical facility for molecular imaging and radionuclide therapy research’ [212885/Z/18/Z]. It was additionally supported by the Wellcome/EPSRC Centre for Medical Engineering at King’s College London [WT 203148/Z/16/Z] and the EPSRC Centre for Doctoral Training in Medical Imaging [EP/L015226/1]. The authors also acknowledge PMB Alcen for the financial support.
Publisher Copyright:
© 2021 The Royal Society of Chemistry.
PY - 2021/8/28
Y1 - 2021/8/28
N2 - Positron emission tomography (PET) is a powerful functional imaging technique that requires the use of positron emitting nuclides. Carbon-11 (11C) 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 11C (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 11C nuclide into the final product. To address some of the constraints of working with 11C, the use of silicon-based chemistry for 11C-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 11C-chemistry. In this short review, we examine silicon-based 11C-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.
AB - Positron emission tomography (PET) is a powerful functional imaging technique that requires the use of positron emitting nuclides. Carbon-11 (11C) 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 11C (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 11C nuclide into the final product. To address some of the constraints of working with 11C, the use of silicon-based chemistry for 11C-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 11C-chemistry. In this short review, we examine silicon-based 11C-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.
UR - http://www.scopus.com/inward/record.url?scp=85113765966&partnerID=8YFLogxK
U2 - 10.1039/d1ob01202a
DO - 10.1039/d1ob01202a
M3 - Review article
SN - 1477-0520
VL - 19
SP - 6916
EP - 6925
JO - ORGANIC AND BIOMOLECULAR CHEMISTRY
JF - ORGANIC AND BIOMOLECULAR CHEMISTRY
IS - 32
ER -