Initial and subsequent approach for the synthesis of 18FDG

2-deoxy-2-[F-18] fluoro-D-glucose ((18)FDG) was developed in 1976 in a collaboration between scientists at the National Institutes of Health, the University of Pennsylvania, and Brookhaven National Laboratory. It was developed for the specific purpose of mapping brain glucose metabolism in living humans, thereby serving as a tool in the basic human neurosciences. With (18)FDG it was possible for the first time to measure regional glucose metabolism in the living human brain. Around the same time, the use of (18)FDG for studies of myocardial metabolism and as a tracer for tumor metabolism were reported. After the first synthesis of (18)FDG via an electrophilic fluorination with F-18 gas (produced via the Ne-20(d,alpha)F-18 reaction), small volume enriched water targets were developed that made it possible to produce large quantities of [F-18]fluoride ion via the high-yield O-18(p,n)F-18 reaction. This was followed by a major milestone, the development of a nucleophilic fluorination method that produced (18)FDG in very high yield. These advances and the remarkable properties of (18)FDG have largely overcome the limitations of the 110-minute half-life of F-18 so that (18)FDG is now available to most regions of the United States from a number of central production sites. This avoids the need for an on-site cyclotron and chemistry laboratory and has opened up the use of (18)FDG to institutions that have a positron emission tomography (PET) scanner (or other imaging device) but no cyclotron or chemistry infrastructure. Currently, (18)FDG is used by many hospitals as an off the shelf radiopharmaceutical for clinical diagnosis in heart disease, seizure disorders, and oncology, the area of most rapid growth. However, it remains an important tool in human neuroscience and in drug research and development. Copyright (C) 2002 by WB. Saunders Company.