Abstract
The isolation of the cis-[ 18F]5-fluoro-6-acetoxy diastereomers 2 and 3, products from the reaction of [ 18F]acetyl hypofluorite with 2′-deoxyuridine ( 1a), undine ( 1b) and arabinofuranosyluracil ( 1c) in acetic acid, and the corresponding [ 18F]5-fluoro-5′,O 6-anhydro-6-hydroxy-cyclouracil derivatives 4 and 5 is described. As an evaluation of their possible use as prodrugs for the toxic 5-fluorouracil (5-FU) the in, vitro behaviour of these two new classes of 18F-labelled pyrimidines in water was determined. In addition, the in vivo behaviour of some of these compounds was studied in nude mice bearing either 5-FU sensitive or 5-FU resistant tumours.
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