About this Research Topic
The incorporation of radioactive nuclides into bioactive molecules has revolutionized the field of pharmaceutical research and development. Among the known radiolabeling applications, positron emission tomography (PET) is a non-invasive, quantitative imaging technology assessing biological and biochemical processes in living subjects. This imaging modality enhances our understandings of disease progression and provides valuable insights into the in vivo behavior of drug candidates during both preclinical and clinical development. These radioisotopes enriched ligands serve as informative biomarkers for oncology, cardiology, and neurodegenerative disorders, as well as critical tools for studying brain targets occupancy relationships for the central nervous system drug development.
PET requires molecules labeled with a positron-emitting radioisotope. Fluorine-18 is attractive for radiotracer design since a significant proportion of pharmaceuticals on the market bearing a fluorine or fluoroalkyl substituent, the appropriate physical and nuclear characteristics of fluorine-18 (97% beta+decay, 109.8 min half-life, 635 keV positron energy), and the metabolic stability of the C-F bond. Over the past decades, organic chemistry research has led to significant advances in fluorination chemistry, followed by late-stage 18F-raidofluorination chemistry, which has successfully boosted PET probes synthesis. However, the systematic incorporation of fluorine-18 radionuclides into organic architectures remains a long-standing synthetic problem owing to a series of chemical and operational challenges. We believe that the recent proliferation of fundamental fluorination methods is a positive development that will expand the chemical space available for preclinical and clinical PET tracer development.
This Research Topic aims to bring together active researchers to discuss the main challenges in this field and how to accelerate the connection between fundamental advances in organofluorine chemistry and real clinical research needs. The Topic Editors welcome Original Research, Mini Review, Review, and Perspective articles that address, but are not limited to the following themes:
• Novel chemistry for fluorination and fluoroalkylation
• Site-selective late-stage [18F]Fluorination methodology.
• Innovative approaches toward the radiosynthesis of organic small molecular PET radioligands.
• New protocols for the installations of other diverse and pharmaceutically useful isotopes.
PET requires molecules labeled with a positron-emitting radioisotope. Fluorine-18 is attractive for radiotracer design since a significant proportion of pharmaceuticals on the market bearing a fluorine or fluoroalkyl substituent, the appropriate physical and nuclear characteristics of fluorine-18 (97% beta+decay, 109.8 min half-life, 635 keV positron energy), and the metabolic stability of the C-F bond. Over the past decades, organic chemistry research has led to significant advances in fluorination chemistry, followed by late-stage 18F-raidofluorination chemistry, which has successfully boosted PET probes synthesis. However, the systematic incorporation of fluorine-18 radionuclides into organic architectures remains a long-standing synthetic problem owing to a series of chemical and operational challenges. We believe that the recent proliferation of fundamental fluorination methods is a positive development that will expand the chemical space available for preclinical and clinical PET tracer development.
This Research Topic aims to bring together active researchers to discuss the main challenges in this field and how to accelerate the connection between fundamental advances in organofluorine chemistry and real clinical research needs. The Topic Editors welcome Original Research, Mini Review, Review, and Perspective articles that address, but are not limited to the following themes:
• Novel chemistry for fluorination and fluoroalkylation
• Site-selective late-stage [18F]Fluorination methodology.
• Innovative approaches toward the radiosynthesis of organic small molecular PET radioligands.
• New protocols for the installations of other diverse and pharmaceutically useful isotopes.
Keywords: Fluorination, Fluoroalkylation, 18F-Radiolabeling, PET radiotracers, PET imaging
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