High specific activity preparation of f-18 tetrafluoroborate
AssigneeMayo Foundation for Medical Education and Research
InventorsTimothy R. DeGrado, Huailei Jiang
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Abstract
Embodiments of the invention provide methods of synthesizing 18F-tetrafluoroborate (18F-TFB) via direct radiofluorination on boron trifluoride (BF3) to enhance both labeling yield and specific activity. Uses of 18F-TFB are also contemplated.
Claims32
A method of radiolabeling tetrafluoroborate (TFB) with 18F-fluoride, the method comprising direct radiofluorination on boron trifluoride (BF3) by reacting the BF3 directly with 18F-fluoride.
A method of radiolabeling tetrafluoroborate with 18F-fluoride, the method comprising:
- (a) reacting 18F-fluoride with BF3;
- and
- (b) isolating the 18F-TFB from unreacted 18F-fluoride and BF3.
The method of any one of the preceding claims, wherein the 18F-TFB has a specific activity of at least 5 GBq/μmol.
The method of any one of the preceding claims, wherein the 18F-TFB has a specific activity of at least 8 GBq/μmol.
The method of any one of the preceding claims, wherein the 18F-TFB was synthesized in radiochemical yield of 15% with greater than 90% purity.
The method of any one of the preceding claims, wherein the 18F-TFB was synthesized in radiochemical yield of 20% with greater than 90% purity.
The method of any one of the preceding claims, wherein the 18F-TFB was synthesized in radiochemical yield of at least 25%.
The method of any one of the preceding claims, wherein the 18F-TFB was synthesized in radiochemical yield of at least 30%.
The method of any one of the preceding claims, wherein the 18F-TFB was has a purity of at least 95%
The method of any one of the preceding claims, wherein the 18F-TFB was synthesized in radiochemical yield of at least 30%.
A method of radiolabeling tetrafluoroborate with 18F-fluoride, the method consisting essentially of:
- (a) trapping 18F-fluoride on an anion exchange column;
- (b) reacting 18F-fluoride with BF3;
- and
- (b) isolating the 18F-TFB from unreacted 18F-fluoride and BF3 from the anion exchange column, wherein the resultant 18F-TFB has a specific activity of at least 5 GBq/μmol.
Dependencies are inferred from the claim text.