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Development of a Target Box for the production of 18F and its Conversion into reactive reaguents for Clinical Use

Research Project

Project/Area Number 60870037
Research Category

Grant-in-Aid for Developmental Scientific Research

Allocation TypeSingle-year Grants
Research Field Radiation science
Research InstitutionKyushu Nuversity

Principal Investigator

KOJIMA Masaharu  Kyushu University, Faculty of pharmaceutical Sceinces, Provessor, 薬学部, 教授 (90037565)

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)
Project Period (FY) 1985 – 1987
Project Status Completed (Fiscal Year 1987)
Budget Amount *help
¥9,000,000 (Direct Cost: ¥9,000,000)
Fiscal Year 1987: ¥1,000,000 (Direct Cost: ¥1,000,000)
Fiscal Year 1986: ¥3,500,000 (Direct Cost: ¥3,500,000)
Fiscal Year 1985: ¥4,500,000 (Direct Cost: ¥4,500,000)
KeywordsFloutring-18 / Target box / Fluoride ion / Deoxyfluorogrlucose / Deoxyluorogalattose / Labeling reagent / 求核置換反応 / 酸素-18 / 陽子 / サイクロトロン / チタンホイル
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 … More 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

Report

(3 results)
  • 1987 Final Research Report Summary
  • 1986 Annual Research Report
  • 1985 Annual Research Report
  • Research Products

    (13 results)

All Other

All Publications (13 results)

  • [Publications] M.Maeda: Chem.Pharm.Bull.33. 1301-1303 (1985)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1987 Final Research Report Summary
  • [Publications] M.Maeda: J.Labelled Compds. Radiopharm.23. 1104-1105 (1986)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1987 Final Research Report Summary
  • [Publications] M.Maeda: Radiat,Isot.38. 307-310 (1987)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1987 Final Research Report Summary
  • [Publications] T.Haradahira: J.Labelled Compds.Radiopharm.25. (1988)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1987 Final Research Report Summary
  • [Publications] T.Haradahira: J.Labelled Compds.Radiopharm.25. (1988)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1987 Final Research Report Summary
  • [Publications] M. MAEDA: "Dimethylsuflonium Salts as Substrate in Aromatic %nucvleophilic Substitution with Fluoride Ion" Chem. Pharm. Bull.33. 1301-1303 (1985)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1987 Final Research Report Summary
  • [Publications] M. MAEDA: "Nucleophilic Displacement of activated Aromatic Dimethylsufonium Group by (F-18)Fluoride Ion" J. Labelled Compds. Rafiopharm.23. 1104-1105 (1986)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1987 Final Research Report Summary
  • [Publications] M. MAEDA: "Dimethylsufonium Moiety as a Leaving Group in Atomatic Radiofluorination using Trtra-n-butylammonium (F-18)Fuloride" Radiat. Iso.38. 307-310 (1987)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1987 Final Research Report Summary
  • [Publications] T. HARADAHIRA: "Alternative Synthesis of No-carrier-added 2-Deoxy-2-(^<18>F)fluoroD-flucoss Uins (F-18)Fluoride Ion" J. Labelled Compds. Rafiopharm.25. (1988)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1987 Final Research Report Summary
  • [Publications] T. HARADAHIRA: "A New Synthesis of 2-Deoxy-2-(^<18>F)fluoro-D-galactose Using (F-18)Fluotide Ion" J. Lavelled Compds. Radiopharm.25. (1988)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1987 Final Research Report Summary
  • [Publications] M.Maeda: Chem.Pharm.Bull.33. 1301-1303 (1985)

    • Related Report
      1986 Annual Research Report
  • [Publications] M.Maeda: J.Label.Compds.Radiopharm.23. 1104-1105 (1986)

    • Related Report
      1986 Annual Research Report
  • [Publications] M.Maeda: Radiat.Isot.(Int.J.Radiat.Appl.Instrum.Part A). 38. (1987)

    • Related Report
      1986 Annual Research Report

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Published: 1987-03-31   Modified: 2016-04-21  

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