2‐Bromo‐6‐[18F]fluoropyridine: two‐step fluorine‐18 radiolabelling via transition metal‐mediated chemistry†. (18th December 2013)

• Record Type: Journal Article
• Authors: Betts, Helen M.; Robins, Edward G.; Dilworth, Jonathan R.; Pascu, Sofia I.
• Is Part Of: Journal of labelled compounds & radiopharmaceuticals. Volume 57:Number 4(2014)
• Page Start: 215
• Page End: 218
• Publication Date: 2013-12-18
• Subjects: Tracers (Chemistry) -- Periodicals; Radiopharmaceuticals -- Periodicals; 615.8424
• DOI: 10.1002/jlcr.3147
• Languages: English
• ISSNs: 0362-4803

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <p>Novel radiolabelling methods are important for the development of new tracers for positron emission tomography. Direct nucleophilic fluorination of aromatic rings with [¹⁸F]fluoride is limited to activated substrates, restricting the application of this approach. Inspired by transition metal‐mediated transformations, a fluorine‐18 synthon was prepared to supplement the radiolabelling methods available for molecules unsuitable for direct labelling. 2‐Bromo‐6‐[¹⁸F]fluoropyridine (denoted [¹⁸F]1) was prepared in high yield, and palladium‐mediated cross‐coupling reactions were exemplified. High incorporation of fluoride and efficient cross‐coupling reactions demonstrate that compound [¹⁸F]1 holds promise as a new synthon for construction of fluorine‐18‐labelled molecules via transition metal‐mediated reactions.</p> </abstract>