Preparation of fluorine-18 labelled sugars and derivatives and their application as tracer for positron-emission-tomography

The usefulness of F-18-labelled carbohydrates, especially 2-deoxy-2-[F-18]fluoro-D-gluco se, to study pathophysiological processes in man non-invasively using positron-emission-tomography (PET) led to a widespread investigation of different F-18-labelled sugars and sugar derivatives. In consideration of the short half-life of fluorine-18 (T-1/2 = 110 min) synthetic strategies concerning precursor design, labelling conditions and deprotection of the intermediate compounds were developed to guarantee an efficient high radiochemical yield synthesis for diagnostic purposes. Besides some aspects of medical application of 2-deoxy-2-[F-18]fluoro-D-glucose, a few synthetic strategies are described reflecting development work on promising F-18-labelled sugars for diagnostic purposes during the last two decades. (C) 2000 Elsevier Science Ltd. All rights reserved.