Rapid microwave-assisted fluorination yielding novel 5′-deoxy-5′-fluorouridine derivatives

The preparation of 18F-labeled ligands for positron emission tomography (PET) and the subsequent imaging have to be completed within a half-life of the neutron-deficient isotope (18F = 110 min). In this paper, we report a rapid fluorination approach to obtain 5′-deoxy-5′-fluoro-substituted uracil nucleoside analogues. Nucleophilic substitution at the 5′-position of the nucleosides was achieved within 45 min providing excellent yields of 75–92% by application of microwaves.

Graphical abstractA rapid fluorination at the 5′-position of nucleosides derivatives is achieved within 45 min providing yields of 75–92% by application of microwave.Figure optionsDownload full-size imageDownload as PowerPoint slide