Base-Catalysed F-18-Labelling Of Trifluoromethyl Ketones. Application To The Synthesis Of F-18-Labelled Neutrophil Elastase Inhibitors

A new method for the fluorine-18 labelling of trifluoromethyl ketones has been developed. This method is based on the conversion of a-COCF3 functional group to a difluoro enol silyl ether followed by halogenation and fluorine-18 labelling. The utility of this new method was demonstrated by the synthesis of fluorine-18 labelled neutrophil elastase inhibitors, which are potentially useful for detection of inflammatory disorders.