[18F]Fluorine-Labeled Pharmaceuticals: Direct Aromatic Fluorination Compared to Multi-Step Strategies

Krüll J, Heinrich M (2019)


Publication Type: Journal article, Review article

Publication year: 2019

Journal

Book Volume: 8

Pages Range: 576-590

Journal Issue: 5

DOI: 10.1002/ajoc.201800494

Abstract

Positron emission tomography (PET) presents an important tool for medicinal and pharmaceutical investigations, with applications ranging from fundamental research to the diagnosis of a broad variety of diseases. Crucial for the use of this technique is, however, a robust labeling strategy for the preparation of the required radiolabeled compound. For 18-fluorine-labeling, which represents the most widely applied method in this field, it is interesting to note that a kind of paradigm change occurred over the last years. While multi-step labeling strategies were the preferred approach for many decades, mainly due to the lack of suitable leaving groups for direct [ 18 F]fluorination reactions, the synthetic tools to achieve the highly attractive direct 18-fluorine-labeling rapidly increased recently. This focus review points out a comparison between the multi-step approaches and the newly developed direct fluorination strategies available for nucleophilic 18-fluorination of carbocyclic aromatic systems, including a discussion of advantages and limitations.

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How to cite

APA:

Krüll, J., & Heinrich, M. (2019). [18F]Fluorine-Labeled Pharmaceuticals: Direct Aromatic Fluorination Compared to Multi-Step Strategies. Asian Journal of Organic Chemistry, 8(5), 576-590. https://dx.doi.org/10.1002/ajoc.201800494

MLA:

Krüll, Jasmin, and Markus Heinrich. "[18F]Fluorine-Labeled Pharmaceuticals: Direct Aromatic Fluorination Compared to Multi-Step Strategies." Asian Journal of Organic Chemistry 8.5 (2019): 576-590.

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