Iodonium Ylide-Mediated Radiofluorination of ^sup 18^F-FPEB and Validation for Human Use
Translation of new methodologies for labeling nonactivated aromatic molecules with ...F remains a challenge. Here, we report a one-step, regioselective, metal-free ...F-labeling method that uses a hypervalent iodonium(III) ylide precursor, to prepare the radiopharmaceutical ...F-3-fluoro-5-[(pyridin...
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| Veröffentlicht in: | The Journal of nuclear medicine (1978) 2015-03, Vol.56 (3), p.489 |
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| container_issue | 3 |
| container_start_page | 489 |
| container_title | The Journal of nuclear medicine (1978) |
| container_volume | 56 |
| creator | Stephenson, Nickeisha A Holland, Jason P Kassenbrock, Alina Yokell, Daniel L Livni, Eli Liang, Steven H Vasdev, Neil |
| description | Translation of new methodologies for labeling nonactivated aromatic molecules with ...F remains a challenge. Here, we report a one-step, regioselective, metal-free ...F-labeling method that uses a hypervalent iodonium(III) ylide precursor, to prepare the radiopharmaceutical ...F-3-fluoro-5-[(pyridin-3-yl)ethynyl]benzonitrile (...F-FPEB). Automated radiosynthesis of ...F-FPEB was achieved by reaction of the ylide precursor (4 mg) with ...F-Et...NF in dimethylformamide at 80°C for 5 min and formulated for injection within 1 h. ...F-FPEB was synthesized in 20% ± 5% (n = 3) uncorrected radiochemical yields relative to ...F-fluoride, with specific activities of 666 ± 51.8 GBq (18 ± 1.4 Ci)/μmol at the end of synthesis and was validated for human use. Radiofluorination of iodonium (III) ylides proved to be an efficient radiosynthetic strategy for synthesis of ...F-labeled radiopharmaceuticals. (ProQuest: ... denotes formulae/symbols omitted.) |
| format | Article |
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Here, we report a one-step, regioselective, metal-free ...F-labeling method that uses a hypervalent iodonium(III) ylide precursor, to prepare the radiopharmaceutical ...F-3-fluoro-5-[(pyridin-3-yl)ethynyl]benzonitrile (...F-FPEB). Automated radiosynthesis of ...F-FPEB was achieved by reaction of the ylide precursor (4 mg) with ...F-Et...NF in dimethylformamide at 80°C for 5 min and formulated for injection within 1 h. ...F-FPEB was synthesized in 20% ± 5% (n = 3) uncorrected radiochemical yields relative to ...F-fluoride, with specific activities of 666 ± 51.8 GBq (18 ± 1.4 Ci)/μmol at the end of synthesis and was validated for human use. Radiofluorination of iodonium (III) ylides proved to be an efficient radiosynthetic strategy for synthesis of ...F-labeled radiopharmaceuticals. 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Here, we report a one-step, regioselective, metal-free ...F-labeling method that uses a hypervalent iodonium(III) ylide precursor, to prepare the radiopharmaceutical ...F-3-fluoro-5-[(pyridin-3-yl)ethynyl]benzonitrile (...F-FPEB). Automated radiosynthesis of ...F-FPEB was achieved by reaction of the ylide precursor (4 mg) with ...F-Et...NF in dimethylformamide at 80°C for 5 min and formulated for injection within 1 h. ...F-FPEB was synthesized in 20% ± 5% (n = 3) uncorrected radiochemical yields relative to ...F-fluoride, with specific activities of 666 ± 51.8 GBq (18 ± 1.4 Ci)/μmol at the end of synthesis and was validated for human use. Radiofluorination of iodonium (III) ylides proved to be an efficient radiosynthetic strategy for synthesis of ...F-labeled radiopharmaceuticals. (ProQuest: ... denotes formulae/symbols omitted.)</abstract><cop>New York</cop><pub>Society of Nuclear Medicine</pub></addata></record> |
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| ispartof | The Journal of nuclear medicine (1978), 2015-03, Vol.56 (3), p.489 |
| issn | 0161-5505 1535-5667 |
| language | eng |
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| source | Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals |
| subjects | Chemical reactions Fluorine Molecules Nuclear medicine Validation studies |
| title | Iodonium Ylide-Mediated Radiofluorination of ^sup 18^F-FPEB and Validation for Human Use |
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