Issue 3, 2016

Asymmetric 18F-fluorination for applications in positron emission tomography

Abstract

Positron emission tomography (PET) is becoming more frequently used by medicinal chemists to facilitate the selection of the most promising lead compounds for further evaluation. For PET, this entails the preparation of 11C- or 18F-labeled drugs or radioligands. With the importance of chirality and fluorine substitution in drug development, chemists can be faced with the challenge of preparing enantiopure molecules featuring the 18F-tag on a stereogenic carbon. Asymmetric 18F-fluorination is an emerging field of research that provides an alternative to resolution or conventional SN2-based radiochemistry. To date, both transition metal complexes and organomediators have been successfully employed for 18F-incorporation at a stereogenic carbon.

Graphical abstract: Asymmetric 18F-fluorination for applications in positron emission tomography

Article information

Article type
Minireview
Submitted
06 Nov. 2015
Accepted
12 Dec. 2015
First published
17 Dec. 2015
This article is Open Access

All publication charges for this article have been paid for by the Royal Society of Chemistry
Creative Commons BY license

Chem. Sci., 2016,7, 1645-1652

Author version available

Asymmetric 18F-fluorination for applications in positron emission tomography

F. Buckingham and V. Gouverneur, Chem. Sci., 2016, 7, 1645 DOI: 10.1039/C5SC04229A

This article is licensed under a Creative Commons Attribution 3.0 Unported Licence. You can use material from this article in other publications without requesting further permissions from the RSC, provided that the correct acknowledgement is given.

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