Rapid microwave-assisted fluorination yielding novel 5'-deoxy-5'-fluorouridine derivatives |
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Authors: | Le H Phuoc Müller Christa E |
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Institution: | Pharmaceutical Sciences Bonn (PSB), Pharmaceutical Chemistry, Institute of Pharmacy, University of Bonn, Kreuzbergweg 26, 53115 Bonn, Germany. H.Le@uea.ac.uk |
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Abstract: | The preparation of (18)F-labeled ligands for positron emission tomography (PET) and the subsequent imaging have to be completed within a half-life of the neutron-deficient isotope ((18)F=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. |
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