Abstract
Rapid and efficient methods using no-carried-added [18F]fluoride as the source of fluorine-18 for nucleophilic aromatic fluorination play an important role in the development of new radiopharmaceuticals for positron emission tomography (PET). Molecules that bear electron-rich aromatic moieties are especially difficult to label by direct single-step nucleophilic no-carrier-added radiofluorination. Classical Balz-Schiemann reaction with its modifications, Wallach reaction and diaryliodonium salts methodology are a few methods to enable this. The present review provides a critical overview of these chemical methods with the emphasis on diaryliodonium salt as precursors for the direct introduction of [18F]fluoride into electron-rich arenes in synthesis of 18F-labeled molecules for PET scanning.
Keywords: Aromatic fluorination, Arylfluoride, Balz-Schiemann reaction, Diaryliodonium salts, 18F-labeled molecules, PET, Triazene.
Current Organic Chemistry
Title:18F-Labeled Aryl-Tracers through Direct Introduction of [18F]fluoride into Electron-Rich Arenes
Volume: 17 Issue: 23
Author(s): Mitja Kovac, Sylvie Mavel and Marko Anderluh
Affiliation:
Keywords: Aromatic fluorination, Arylfluoride, Balz-Schiemann reaction, Diaryliodonium salts, 18F-labeled molecules, PET, Triazene.
Abstract: Rapid and efficient methods using no-carried-added [18F]fluoride as the source of fluorine-18 for nucleophilic aromatic fluorination play an important role in the development of new radiopharmaceuticals for positron emission tomography (PET). Molecules that bear electron-rich aromatic moieties are especially difficult to label by direct single-step nucleophilic no-carrier-added radiofluorination. Classical Balz-Schiemann reaction with its modifications, Wallach reaction and diaryliodonium salts methodology are a few methods to enable this. The present review provides a critical overview of these chemical methods with the emphasis on diaryliodonium salt as precursors for the direct introduction of [18F]fluoride into electron-rich arenes in synthesis of 18F-labeled molecules for PET scanning.
Export Options
About this article
Cite this article as:
Kovac Mitja, Mavel Sylvie and Anderluh Marko, 18F-Labeled Aryl-Tracers through Direct Introduction of [18F]fluoride into Electron-Rich Arenes, Current Organic Chemistry 2013; 17 (23) . https://dx.doi.org/10.2174/13852728113179990022
DOI https://dx.doi.org/10.2174/13852728113179990022 |
Print ISSN 1385-2728 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5348 |
Call for Papers in Thematic Issues
Advances of Heterocyclic Chemistry with Pesticide Activity
Global food safety and security will continue to be a global concern for the next 50 years and beyond. Plant diseases have had a significant impact on food safety and security throughout the entire food chain, from primary production to consumption. While conventional chemical pesticides have been traditionally used for ...read more
Calculation design of covalent/metal organic framework based catalysts
This research area combines theoretical computation and screening with machine learning for the design of covalent/metal organic framework-based catalysts, bridging the disciplines of organic chemistry, physical chemistry, computational chemistry, materials science, and machine learning. It covers several critical aspects: designing and synthesizing organic catalysts for improved performance, applying computational methods ...read more
Carbohydrates conversion in biofuels and bioproducts
Biomass pretreatment, hydrolysis, and saccharification of carbohydrates, and sugars bioconversion in biofuels and bioproducts within a biorefinery framework. Carbohydrates derived from woody biomass, agricultural wastes, algae, sewage sludge, or any other lignocellulosic feedstock are included in this issue. Simulation, techno-economic analysis, and life cycle analysis of a biorefinery process are ...read more
Catalytic C-H bond activation as a tool for functionalization of heterocycles
The major topic is the functionalization of heterocycles through catalyzed C-H bond activation. The strategies based on C-H activation not only provide straightforward formation of C-C or C-X bonds but, more importantly, allow for the avoidance of pre-functionalization of one or two of the cross-coupling partners. The beneficial impact of ...read more
Related Journals
- 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
-
Antiangiogenic Agents: Studies on Fumagillin and Curcumin Analogs
Current Pharmaceutical Design Renal COX-2, Cytokines and 20-HETE: Tubular and Vascular Mechanisms
Current Pharmaceutical Design A Mini Review on Biological Activities of Pyridazinone Derivatives as Antiulcer, Antisecretory, antihistamine and Particularly Against Histamine H3R
Mini-Reviews in Medicinal Chemistry Alginates in Pharmaceutics and Biomedicine: Is the Future so Bright?
Current Pharmaceutical Design Live Yeast Cell Derivative Induces c-fos Expression in THP-1 Monocytes
Medicinal Chemistry Mechanisms Linking Leptin to Arterial and Venous Thrombosis: Potential Pharmacological Targets
Current Pharmaceutical Design The Hemoglobins of Fishes Living at Polar Latitudes - Current Knowledge on Structural Adaptations in a Changing Environment
Current Protein & Peptide Science Natural Monoclonal Antibodies and Cancer
Recent Patents on Anti-Cancer Drug Discovery Medical Systemic Therapies for Hepatocellular Carcinoma: Clinical Perspectives and Safety Profile
Current Drug Safety New Therapies for Patients with Chronic Lymphocytic Leukemia
Current Cancer Therapy Reviews Anti-Inflammatory Activity of Tetracyclines: Applications to Human Disease
Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry Cardiovascular Effects of Green Tea Catechins: Progress and Promise
Recent Patents on Cardiovascular Drug Discovery Endogenous Chemical Mediators in Anti-Inflammation and Pro-Resolution
Current Medicinal Chemistry - Anti-Inflammatory & Anti-Allergy Agents Anti-Diabetic Compounds and their Patent Information: An Update
Recent Patents on Inflammation & Allergy Drug Discovery Adiponectin as a Regulator of Vascular Redox State: Therapeutic Implications
Recent Patents on Cardiovascular Drug Discovery Development of Small Molecule Non-peptide Formyl Peptide Receptor (FPR) Ligands and Molecular Modeling of Their Recognition
Current Medicinal Chemistry Molecular Pharmacology of Non-L-type Calcium Channels
Current Pharmaceutical Design Compositions for Treatment of Cancer and Inflammation
Recent Patents on Anti-Cancer Drug Discovery Cardiovascular Risk and Endothelial Dysfunction: The Preferential Route for Atherosclerosis
Current Pharmaceutical Biotechnology Progress in the Preclinical Discovery and Clinical Development of Class I and Dual Class I/IV Phosphoinositide 3-Kinase (PI3K) Inhibitors
Current Medicinal Chemistry