Production of 18F-Labeled Radiopharmaceuticals

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Classical Methods for Radiofluorination • Balz-Schiemann Reaction • Modified Balz-Schiemann Reaction • Wallach-type Reaction Balz-Schiemann Reaction F X N + 2 BF - 4 18 - X N + 2 [ 18 - F]BF 4 Exchange Pyrolysis Δ X 18 F + [ 18 F]BF 3 + N 2 • An [ 18 F]aryldiazonium tetrafluoroborate is prepared by exchange of tetrafluoroborate with [ 18 F]fluoride • This salt is then decomposed pyrolytically
Balz-Schiemann Reaction (cont’d) • The radioactivity is partitioned equally between the F atoms of the desired [ 18 F]fluoroarene and the byproduct, [ 18 F]boron trifluoride • The process is therefore CA with a maximal theoretical yield of 25% • Many compounds have been labeled in this manner, particularly amino acids such as L-phenylalanine, L-tryptophan, L- tyrosine and L-DOPA • Yields are often much lower than theoretical • The method is regiospecific; all isomers of the amino acids can be prepared • The method is quite tolerant of functionality Modified Balz-Schiemann Reaction X N 2 + BCl 4 - 18 F - X N 2 + [ 18 F]BFCl 3 - Exchange Pyrolysis Δ X 18 F + [ 18 F]BFCl 2 + BCl 3 + N 2 + X Cl •An [ 18 F]aryldiazonium fluorotrichloroborate is prepared by exchange of tetrachloroborate salt with [ 18 F]fluoride • This salt is then decomposed pyrolytically • The process is NCA
Page 1 and 2: Production of 18 F-Labeled Radiopha
Page 3 and 4: Some Properties of Fluorine - Bondi
Page 5 and 6: [ 18 F]2-Fluoro-2-deoxy-D-glucose (
Page 7 and 8: Production of CA [ 18 F]Fluorine (1
Page 9 and 10: Production of CA ‘[ 18 F]Hydrogen
Page 11: NCA [ 18 F]Fluoride (2) - By irradi
Page 15 and 16: Some ‘Electrophilic’ Radiofluor
Page 17 and 18: [ 18 F]Xenon Difluoride 18 F-F + Xe
Page 19 and 20: 'Electrophilic' Addition -[ 18 F]Fl
Page 21 and 22: 'Electrophilic' Addition -[ 18 F]Ac
Page 23 and 24: X Y Aromatic Radiofluorination (2)
Page 25 and 26: [ 18 F]Fluorodemetallation - At ary
Page 27: [ 18 F]Fluorodemetallation - At alk

Production of 18F-Labeled Radiopharmaceuticals

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