SYNTHESIS OF 18F FLUOROMETHYL BENZENE USING BENZYL PENTAFLUOROBENZENESULFONATE

摘要

The present invention discloses the reactivity of ponytail ('PT') sulfonates as leaving groups in nucleophilic fluorination reactions. The results showed that using a pentafluorobenzenesulfonate precursor is a suitable leaving group for n. c. a. nucleophilic 18F-fluorination in synthesis of [18F]fluoromethyl benzene, wherein this is a suitable leaving group for 18F-labeling with moderate reactivity. The PT-precursor seems to be quite stable. In an attempt to purify the crude 18F-labeled product using fluorous solid phase extraction (F-SPE), the radio labeled impurities decreased significantly. This provides an opportunity for utilizing PT methodology in both simple and fast purification methods.