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Radiochemical Synthesis of Alkyl Geminal 18F-Difluoroalkyl Motifs Mediated by Silver(I) Oxide

Year: 2025

Type: article

Abstract: High Resolution Image Download MS PowerPoint Slide 18 F radiotracers are used in positron emission tomography imaging for medical diagnosis and drug development. Current methods to synthesize 18 F-polyfluorinated functional groups are limited in substrate scope and result in radiotracers with low molar activities ( A m ). We disclose the synthesis of a range of 18 F-difluoroalkyl groups by nucleophilic substitution of geminal bromofluoroalkyl electrophiles with [ 18 F]fluoride mediated by Ag 2 O. The utility of this transformation to support (pre)clinical imaging is demonstrated by translation to an automated synthesizer.

Source: Organic Letters

DOI: 10.1021/acs.orglett.5c00187

Authors: Pawan Mishra, Jasmine Hind, Ian A. Fallis, Matthew Tredwell

Institutions: Cardiff University, University Hospital of Wales

Language: English

Topic: Radiopharmaceutical Chemistry and Applications

Subfield: Radiology, Nuclear Medicine and Imaging

Field: Medicine

Domain: Health Sciences

Open Access status: hybrid

Estimated APC paid: $4,500

Funder: Engineering and Physical Sciences Research Council