Abstract
Positron (β+) emission tomography (PET) is a powerful, noninvasive tool for the in vivo, three-dimensional imaging of physiological structures and biochemical pathways. The continued growth of PET imaging relies on a corresponding increase in access to radiopharmaceuticals (biologically active molecules labeled with short-lived radionuclides such as fluorine-18). This unique need to incorporate the short-lived fluorine-18 atom (t1/2 = 109.77 min) as late in the synthetic pathway as possible has made development of methodologies that enable rapid and efficient late stage fluorination an area of research within its own right. In this review we describe strategies for radiolabeling with fluorine-18, including classical fluorine-18 radiochemistry and emerging techniques for late stage fluorination reactions, as well as labeling technologies such as microfluidics and solid-phase radiochemistry. The utility of fluorine-18 labeled radiopharmaceuticals is showcased through recent applications of PET imaging in the healthcare, personalized medicine and drug discovery settings.
Keywords: Fluorine-18, radiochemistry, radiopharmaceutical synthesis, PET imaging, positron emission tomography.
Current Topics in Medicinal Chemistry
Title:Radiosyntheses using Fluorine-18: The Art and Science of Late Stage Fluorination
Volume: 14 Issue: 7
Author(s): Erin L. Cole, Megan N. Stewart, Ryan Littich, Raphael Hoareau and Peter J. H. Scott
Affiliation:
Keywords: Fluorine-18, radiochemistry, radiopharmaceutical synthesis, PET imaging, positron emission tomography.
Abstract: Positron (β+) emission tomography (PET) is a powerful, noninvasive tool for the in vivo, three-dimensional imaging of physiological structures and biochemical pathways. The continued growth of PET imaging relies on a corresponding increase in access to radiopharmaceuticals (biologically active molecules labeled with short-lived radionuclides such as fluorine-18). This unique need to incorporate the short-lived fluorine-18 atom (t1/2 = 109.77 min) as late in the synthetic pathway as possible has made development of methodologies that enable rapid and efficient late stage fluorination an area of research within its own right. In this review we describe strategies for radiolabeling with fluorine-18, including classical fluorine-18 radiochemistry and emerging techniques for late stage fluorination reactions, as well as labeling technologies such as microfluidics and solid-phase radiochemistry. The utility of fluorine-18 labeled radiopharmaceuticals is showcased through recent applications of PET imaging in the healthcare, personalized medicine and drug discovery settings.
Export Options
About this article
Cite this article as:
Cole L. Erin, Stewart N. Megan, Littich Ryan, Hoareau Raphael and Scott J. H. Peter, Radiosyntheses using Fluorine-18: The Art and Science of Late Stage Fluorination, Current Topics in Medicinal Chemistry 2014; 14 (7) . https://dx.doi.org/10.2174/1568026614666140202205035
DOI https://dx.doi.org/10.2174/1568026614666140202205035 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
Call for Papers in Thematic Issues
Chemistry Based on Natural Products for Therapeutic Purposes
The development of new pharmaceuticals for a wide range of medical conditions has long relied on the identification of promising natural products (NPs). There are over sixty percent of cancer, infectious illness, and CNS disease medications that include an NP pharmacophore, according to the Food and Drug Administration. Since NP ...read more
Current Trends in Drug Discovery Based on Artificial Intelligence and Computer-Aided Drug Design
Drug development discovery has faced several challenges over the years. In fact, the evolution of classical approaches to modern methods using computational methods, or Computer-Aided Drug Design (CADD), has shown promising and essential results in any drug discovery campaign. Among these methods, molecular docking is one of the most notable ...read more
Drug Discovery in the Age of Artificial Intelligence
In the age of artificial intelligence (AI), we have witnessed a significant boom in AI techniques for drug discovery. AI techniques are increasingly integrated and accelerating the drug discovery process. These developments have not only attracted the attention of academia and industry but also raised important questions regarding the selection ...read more
From Biodiversity to Chemical Diversity: Focus of Flavonoids
Flavonoids are the largest group of polyphenols, plant secondary metabolites arising from the essential aromatic amino acid phenylalanine (or more rarely from tyrosine) via the phenylpropanoid pathway. The flavan nucleus is the basic 15-carbon skeleton of flavonoids (C6-C3-C6), which consists of two phenyl rings (A and B) and a heterocyclic ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Small Peptide and Protein-based Molecular Probes for Imaging Neurological Diseases
Current Protein & Peptide Science MATra - Magnet Assisted Transfection: Combining Nanotechnology and Magnetic Forces to Improve Intracellular Delivery of Nucleic Acids
Current Pharmaceutical Biotechnology iRGD Co-Administration with Paclitaxel-Loaded PLGA Nanoparticles Enhance Targeting and Antitumor Effect in Colorectal Cancer Treatment
Anti-Cancer Agents in Medicinal Chemistry Monitoring T Cell Responses to Cancer Immunotherapy: Can We Now Identify Biomarkers Predicting Patients Who will be Responders
Current Cancer Therapy Reviews MiRNA-29: A microRNA Family with Tumor-Suppressing and Immune-Modulating Properties
Current Molecular Medicine Eicosanoids Derived From Arachidonic Acid and Their Family Prostaglandins and Cyclooxygenase in Psychiatric Disorders
Current Neuropharmacology Reversal of Tumor Induced Dendritic Cell Paralysis: A Treatment Regimen Against Cancer
Current Immunology Reviews (Discontinued) Role of Early Growth Response-1 in the Development of Alcohol-Induced Steatosis
Current Molecular Pharmacology Insight to Physiology and Pathology of Zinc(II) Ions and Their Actions in Breast and Prostate Carcinoma
Current Medicinal Chemistry Arsenic Trioxide-based Nanomedicines as a Therapeutic Combination Approach for Treating Gliomas: A Review
Current Nanoscience Tumour Gene Therapy Monitoring Using Magnetic Resonance Imaging and Spectroscopy
Current Gene Therapy Integrins in Drug Targeting-RGD Templates in Toxins
Current Pharmaceutical Design Targeting Glia Cells: Novel Perspectives for the Treatment of Neuropsychiatric Diseases
Current Neuropharmacology Role of Glioma-associated GLI1 Oncogene in Carcinogenesis and Cancertargeted Therapy
Current Cancer Drug Targets Risk Assessment of the Use of Autonomous Parvovirus-Based Vectors
Current Gene Therapy The Complex Biology of FOXO
Current Drug Targets Cytoskeleton-Anchoring of Conformational Mutant-Like p53, but Not Shorter Isoforms p53β and p47 (ΔN40p53) in Senescent Human Fibroblasts
Current Aging Science Hsp90: A Novel Target for Cancer Therapy
Current Topics in Medicinal Chemistry Strategies for the Preparation of Bifunctional Gadolinium(III) Chelators
Current Organic Synthesis Optical Imaging of Microvascular Morphology and Perfusion
Current Angiogenesis (Discontinued)