Rapid microwave-assisted fluorination yielding novel 5'-deoxy-5'-fluorouridine derivatives.
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.
Le
H Phuoc
HP
Pharmaceutical Sciences Bonn (PSB), Pharmaceutical Chemistry, Institute of Pharmacy, University of Bonn, Kreuzbergweg 26, 53115 Bonn, Germany. H.Le@uea.ac.uk <H.Le@uea.ac.uk>
Müller
Christa E
CE
D005467:Floxuridine / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D005461:Fluorine / Q000737:chemistry*; D008872:Microwaves; D015394:Molecular Structure; D013997:Time Factors
D005467:Floxuridine; D005461:Fluorine; C025034:doxifluridine