Cyclotron Isotopes and Radiopharmaceuticals—xxiii. Novel Anhydrous 18f-Fluorinating Intermediates

Production of Some Medically Important Short-Lived Neutron-Deficient Radioisotopes of Halogens

“…30] and relatively large yields have been reported; the chemical form of 18 F, however, was not always well defined. Extensive studies on the characterization of conditions of I8 F-labelled F 2 production have been carried out at BNL [14,31,32], The target vessel is made of nickel (2.5 cm ψ χ 10 cm) and the interior of the vessel is passivated by F 2 . The vessel is filled with the highest purity Ne (plus F 2 in the range of 0.1 -7.5%) and after irradiation the 18 F-F 2 is purged out.…”

18F-FDG Radiosynthesis: A Landmark in the History of PET (perspective on “Efficient Stereospecific Synthesis of No-Carrier-Added 2-[18F]fluoro-2-Deoxy-D-Glucose Using Aminopolyether Supported Nucleophilic Substitution” J Nucl Med. 1986;27:235–238)

“…Vi rtually all of the brain's energy derives from glucose metabolism. This underpins the development of 18 F-FDG, a radiotracer that was fi rst used to measure regional brain glucose utilization in humans, and has had a profound infl uence on research in the neurosciences (1). The subsequent discovery that 18 F-FDG can be used to assess viable myocardium and also accumulates in tumors in proportion to their degree of malignancy underpins the evolution of PET as a major clinical tool in cancer diagnosis and monitoring of treatment.…”

“…The 1986 landmark paper by Hamacher and colleagues in JNM represents a major milestone in the present use of 18 F-FDG in clinical nuclear medicine worldwide (2).…”

“…The 18 F-FDG molecule was modeled on the 14 C-labeled 2deoxyglucose method, which measures regional brain glucose utilization in animals (3). 2-deoxyglucose is an analog of glucose in which the hydroxyl group on C-2 is replaced by a hydrogen atom.…”

“…A survey of the literature at the time revealed that 2-deoxy-2-fl uoro-D-glucose (in which the hydrogen atom on C-2 was replaced by a fl uorine atom) met these requirements. An electrophilic reaction with 18 F using elemental fl uorine ([ 18 F]F 2 ) produced via the 20 Ne(d, ) 18 F reaction on Brookhaven's 152-cm (60-in) cyclotron ( 4) was developed and used to produce 18 F-FDG in suffi cient yield for transport from Long Island to the University of Pennsylvania for the fi rst human studies in 1976 (1,5).…”