Seminars in Nuclear Medicine
Volume 32, Issue 1 , Pages 6-12, January 2002

Initial and subsequent approach for the synthesis of 18FDG+

This article is dedicated to the memory of Alfred P. Wolf, whose vision and contributions to the development of 18FDG, to the advancement of radiotracer chemistry, and to the training of scientists have had an enormous, worldwide impact on the field of nuclear medicine.

  • Joanna S. Fowler

      Affiliations

    • Corresponding Author InformationAddress reprint requests to Joanna S. Fowler, PhD, Chemistry Department, Brookhaven National Laboratory, Upton, NY 11973.
    • ,
  • Tatsuo Ido

2-deoxy-2-[18F] fluoro-d-glucose (18FDG) 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 18FDG it was possible for the first time to measure regional glucose metabolism in the living human brain. Around the same time, the use of 18FDG for studies of myocardial metabolism and as a tracer for tumor metabolism were reported. After the first synthesis of 18FDG via an electrophilic fluorination with 18F gas (produced via the 20Ne(d,α)18F reaction), small volume enriched water targets were developed that made it possible to produce large quantities of [18F]fluoride ion via the high-yield 18O(p,n)18F reaction. This was followed by a major milestone, the development of a nucleophilic fluorination method that produced 18FDG in very high yield. These advances and the remarkable properties of 18FDG have largely overcome the limitations of the 110-minute half-life of 18F so that 18FDG 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 18FDG to institutions that have a positron emission tomography (PET) scanner (or other imaging device) but no cyclotron or chemistry infrastructure. Currently, 18FDG 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.

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+ This research was performed in part at Brookhaven National Laboratory under contract DE-AC02-98CH10886 with the US Department of Energy and was supported by its Office of Biological and Environmental Research and by the National Institutes of Health (NS-15380).

PII: S0001-2998(02)80036-8

doi:10.1053/snuc.2002.29270

Seminars in Nuclear Medicine
Volume 32, Issue 1 , Pages 6-12, January 2002

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