Recent Developments in Carbon-11 Chemistry and Applications for First-In-Human PET Studies

• Published in: Molecules (Basel, Switzerland) Vol. 28; no. 3; p. 931
• Main Authors: Pees, Anna, Chassé, Melissa, Lindberg, Anton, Vasdev, Neil
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 17.01.2023; MDPI
• Subjects: Amino acids; Analysis; Automation; Carbon compounds; Carbon dioxide; Carbon Radioisotopes - chemistry; Carbon-11; Evaluation; first-in-human; Fluorides; Green chemistry; Humans; Laboratories; Molecular dynamics; PET imaging; Physicochemical properties; positron emission tomography (PET); Positron-Emission Tomography; radiochemistry; Radiochemistry - methods; Radioisotopes - chemistry; Radiopharmaceuticals - chemistry; radiotracer; Reagents; Review; Canada; Carbon-11; first-in-human; radiotracer; positron emission tomography (PET); radiochemistry
• ISSN: 1420-3049; 1420-3049
• DOI: 10.3390/molecules28030931

Positron emission tomography (PET) is a molecular imaging technique that makes use of radiolabelled molecules for in vivo evaluation. Carbon-11 is a frequently used radionuclide for the labelling of small molecule PET tracers and can be incorporated into organic molecules without changing their physicochemical properties. While the short half-life of carbon-11 (11C; t½ = 20.4 min) offers other advantages for imaging including multiple PET scans in the same subject on the same day, its use is limited to facilities that have an on-site cyclotron, and the radiochemical transformations are consequently more restrictive. Many researchers have embraced this challenge by discovering novel carbon-11 radiolabelling methodologies to broaden the synthetic versatility of this radionuclide. This review presents new carbon-11 building blocks and radiochemical transformations as well as PET tracers that have advanced to first-in-human studies over the past five years.