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2010 Fiscal Year Final Research Report

Synthesis of ^<18>F-labeled GABA, amino acids, and lactic acids by using oxazoline precursors

Research Project

  • PDF
Project/Area Number 19790028
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeSingle-year Grants
Research Field Chemical pharmacy
Research InstitutionThe Institute of Physical and Chemical Research

Principal Investigator

DOI Hisashi  The Institute of Physical and Chemical Research, 分子イメージング標識化学研究チーム, チームリーダー (00421818)

Project Period (FY) 2007 – 2010
Keywords合成化学 / 生体分子 / 生理活性 / 脳神経 / 放射線
Research Abstract

In order to realize synthesis of ^<18>F-labeled GABA, amino acid, and lactic acid, we have investigated ^<18>F-labeling reaction using oxazoline precursors under PET radiolabeling conditions. However, we encountered difficulties to conduct the ^<18>F-labeling under anhydrous conditions by remote-controlling radiolabeling system, and unfortunately, oxazoline precursors underwent radiolysis under the conditions, giving many side products due to decomposition. In the circumstances, we have tried to develop Pd^0-mediated rapid C-[^<18>F]fluoromethylation in parallel and have explored other 18F-labeling methods for the target compounds.

  • Research Products

    (12 results)

All 2011 2010 2009 Other

All Journal Article (1 results) (of which Peer Reviewed: 1 results) Presentation (6 results) Book (3 results) Remarks (1 results) Patent(Industrial Property Rights) (1 results)

  • [Journal Article] Palladium(0)-Mediated Rapid Methylation and Fluoromethylation on Carbon Frameworks by Reacting Methyl and Fluoromethyl Iodide with Aryl and Alkenyl Boronic Acid Esters Useful for the Synthesis of [^<11>C]CH_3-C-and [^<18>F]FCH_2-C-Containing PET Tracers2009

    • Author(s)
      Hisashi Doi, Ikuya Ban, Akihito Nonoyama, Kengo Sumi, Chunxiang Kuang, Takamitsu Hosoya, Hideo Tsukada, Masaaki Suzuki
    • Journal Title

      Chem.Eur.J. 15

      Pages: 4165-4171

    • Peer Reviewed
  • [Presentation] [^<18>F]FCH_2基含有PETトレーサーの新規合成法の開発;New Methodology of the Synthesis of [^<18>F]FCH_2-Incorporated PET Tracers2010

    • Author(s)
      後藤美樹、土居久志、鈴木正昭
    • Organizer
      日本ケミカルバイオロジー学会第5回年会
    • Place of Presentation
      慶応義塾大学、横浜
    • Year and Date
      20100518-20100519
  • [Presentation] Pd^0-mediated rapid C-[^<18>F]fluoromethylation by the reaction of a [^<18>F]fluoromethyl halide and an organoboron compound2010

    • Author(s)
      H.Doi, M.Goto, M.Suzuki
    • Organizer
      15th European Symposium On Radiopharmacy And Radiopharmaceuticals, Abstract, Q.J.Nucl.Med.Mol.Imaging, 54, Suppl.1 to No.2, pp 18.19.
    • Place of Presentation
      Edinburgh, Scotland (UK)
    • Year and Date
      20100408-20100411
  • [Presentation] 理研におけるPET標識化学の展開:^<11>Cおよび^<18>F-標識法の現状と将来展望2010

    • Author(s)
      土居久志
    • Organizer
      分子イメージング研究シンポジウム2010-未来を拓く創薬・疾患診断研究-,Molecular Imaging 2010, The Future with Drug Discovery and PET Diagnosis
    • Place of Presentation
      日経ビル3階日経ホール、東京
    • Year and Date
      20100121-20100122
  • [Presentation] Pd^0-mediated rapid C-[^<18>F]fluoromethylation : Coupling reaction of an organoboron compound with a [^<18>F]fluoromethyl halide2010

    • Author(s)
      H.Doi, M.Goto, M.Suzuki
    • Organizer
      2010 International Chemical Congress of Pacific Basin Societies (PACIFICHEM 2010)
    • Place of Presentation
      Hawaii, USA
    • Year and Date
      2010-12-15
  • [Presentation] PETを活用した分子イメージング創薬化学の展開;Molecular imaging medicinal chemistry by PET in RIKEN CMIS2009

    • Author(s)
      土居久志
    • Organizer
      第7回糖鎖科学コンソーシアムシンポジウム~糖鎖研究と他領域との統合
    • Place of Presentation
      千里ライフサイエンスセンター、大阪
    • Year and Date
      20091207-20091208
  • [Presentation] PETプローブの一般的合成法の開発とPETケミカルバイオロジーへの展開;Development of General Synthetic Methodologies of PET Probes and Its Applications to PET Chemical Biology2009

    • Author(s)
      土居久志、橋爪良信、畑中恵子、高島好聖、後藤美樹、長田浩子、斯琴、倉橋正浩、鈴木正昭
    • Organizer
      日本ケミカルバイオロジー学会第4回年会
    • Place of Presentation
      神戸市産業振興センター、神戸
    • Year and Date
      20090518-20090519
  • [Book] 科学と工業(大阪工研協会会誌),85(4)(短寿命PET分子プローブの合成のための高速化学反応の開発)2011

    • Author(s)
      土居久志
    • Total Pages
      154-161
  • [Book] 遺伝子医学MOOK18号 創薬研究への分子イメージング応用,"第1章3.PET分子プローブの合成法"2010

    • Author(s)
      土居久志
    • Total Pages
      47-53
    • Publisher
      メディカルドゥ
  • [Book] 臨床医とコメディカルのための最新クリニカルPET,"第15章2.PET分子プローブの開発研究とその進歩"2010

    • Author(s)
      土居久志
    • Total Pages
      251-257
    • Publisher
      先端医療技術研究所
  • [Remarks] ホームページ等 理化学研究所分子イメージング科学研究センター

    • URL

      http://www.cmis.riken.jp/

  • [Patent(Industrial Property Rights)] 高速フルオロメチル化法及びそれを利用したPETトレーサーの製造方法2010

    • Inventor(s)
      鈴木正昭、土居久志、、後藤美樹
    • Industrial Property Rights Holder
      (独)理化学研究所
    • Industrial Property Number
      PCT出願,PCT/JP2010-17632
    • Filing Date
      2010-12-03

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Published: 2012-02-13   Modified: 2016-04-21  

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