1987 Fiscal Year Final Research Report Summary
Development of a Target Box for the production of 18F and its Conversion into reactive reaguents for Clinical Use
| Project/Area Number |
60870037
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| Research Category |
Grant-in-Aid for Developmental Scientific Research
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| Allocation Type | Single-year Grants |
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| Research Field |
Radiation science
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| Research Institution | Kyushu Nuversity |
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Principal Investigator |
KOJIMA Masaharu Kyushu University, Faculty of pharmaceutical Sceinces, Provessor, 薬学部, 教授 (90037565)
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| Co-Investigator(Kenkyū-buntansha) |
MAEDA Miyoru Kyushu Univeristy, Faculty of pharmaceutical Sciences, Associate Professor, 薬学部, 助教授 (70101178)
YOSHIMURA Astushi Kyushu Unversity, Radioisotope Center, Associate Professor, アイソトープ総合センター病院地区実験室, 助教授 (50013371)
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| Project Period (FY) |
1985 – 1987
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| Keywords | Floutring-18 / Target box / Fluoride ion / Deoxyfluorogrlucose / Deoxyluorogalattose / Labeling reagent / 求核置換反応 |
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| Research Abstract |
A simple titanuim target box has been constucted for the profuction of^<18>F via^<18>O(P,n)^<18>F reaction. A 6-8% enriched sample of (^8OJH_2O was used as target meterial. The^<18>F activety of 10-12 mci was obtained by a 20 min irradation with a beam current of 15 <micru>A after waiting 2 hr to alloe^<13>N produced concomitantly ot decay. Ion chromatographic analsys showed that carrier fluoride is present at the level of 0.1-0.2 ppm. The conversion of the aq. (^<18>Flfuoride into reactive nucleophilic reagents and the subsequent reaction was pwrformed in the same vassel. Resolubilization in a Polymewthlpentene(TPX) vessel resulted in a higher resolubilization yield for the^<18>F when compared to a pyrex vessel. We have found that phenyldimathylsulfonium methylsulfactes activeted by electron-withdrawing substituents undergo nuclecophilic substitutuon with (Bu)_4N+^<+18>F^- to give^<18>F-labeled aryl fluorides. This dimethylsulfonium group allows reasonable yeilds only in very activate
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d compounds using a TPC vessel. We have also been successful in the use of^<18>F-fluorinating agents from this water target to aliphatic nucleophilic substitution reactions. A syntrhetic route to NCA 2-deoxy-2(^<18>Fjfluoro-glucose (2-^<18>FDG) involving (^<18>Flfuoride ion displacement on methyl 3-0-benzyl-4,6-3-benzylidene-2-3-trifluoromethanusulfonyl<beta>-D-mannopyranoside in a TPX vessel followed by hydrolysis with 6N HCl produces a 34-43% overall rediochemaicl yiels without corretion for decay. This methodology constitutes an alternative route to NCA 2-^<18>FDG using (^<18>Flfluoride ion. A nucleophilic rafiofulorination of methyl 3,4-0isopropylidene-2-3-trifluoromethanesulfonyl-6-3-teiryl-<beta>-D-talopyranoside with (k/2.2.2.)^<+18> F^- followed by hydrolysis with 6N HCl afforded 2-deoxy-2-(^<18>Fjfluoro-D-galactose (2-^<18>FDGal) in 36-39* overall radiochemical yield without correction fot decay, proveding the first successful synyhesis of NCA 2-^<18>FDGal using (^<18>Fjfluoride ion. Less
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Research Products
(10 results)
