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Practical protocol of preparation of [18F]CF3 labelled probe for diagnostic agents

Research Project

Project/Area Number 26713041
Research Category

Grant-in-Aid for Young Scientists (A)

Allocation TypePartial Multi-year Fund
Research Field Radiation science
Research InstitutionNagasaki University

Principal Investigator

MIZUTA Satoshi  長崎大学, 医歯薬学総合研究科(医学系), 助教 (50717618)

Research Collaborator OTAKI Hiroki  長崎大学, 医歯薬学総合研究科(医学系), 助教
WATANABE Ken  長崎大学, 医歯薬学総合研究科(医学系), 助教
ISHIKAWA Takeshi  長崎大学, 医歯薬学総合研究科(医学系), 准教授
Project Period (FY) 2014-04-01 – 2017-03-31
Project Status Completed (Fiscal Year 2016)
Budget Amount *help
¥23,920,000 (Direct Cost: ¥18,400,000、Indirect Cost: ¥5,520,000)
Fiscal Year 2015: ¥5,460,000 (Direct Cost: ¥4,200,000、Indirect Cost: ¥1,260,000)
Fiscal Year 2014: ¥18,460,000 (Direct Cost: ¥14,200,000、Indirect Cost: ¥4,260,000)
Keywordsフッ素含有ヘテロ環 / フッ素化反応 / イミダゾリウム塩 / イオン性液体 / 生理活性物質 / 核医学 / PET / トリフルオロメチル / フッ化物イオン / [18F] / 放射線科学
Outline of Final Research Achievements

Our group addressed to development of new methods for synthesis of trifluoromethyl compounds via a fluorination reaction as a key step. Reactions of dibromofluoromethylthio substrates with KF and silver(I) salt were performed affording the trifluoromethylthio products. The F-CF2S bond forming reaction might be available for the hot fluorination reaction with radio isotope. Alternatively, we have developed methods for synthesis of new trifluoromethyl compounds. As one examples, phase transfer catalysts, trifluoromethylthio substituted imidazolium salts from thiourea and electrophilic trifluoromethylating reagents have been synthesized.In addition, dibromo-2-trifluoromethyl acrylic acid ethyl ester found to be a versatile platform for the stereoselective preparation of functionalized-α-trifluoromethyl α,β-unsaturated lactones and trifluoromethyl pyrazolinones. Ionic liquid-mediated hydrofluorination of 3-bromooxindoles also have been achieved.

Report

(4 results)
  • 2016 Annual Research Report   Final Research Report ( PDF )
  • 2015 Annual Research Report
  • 2014 Annual Research Report
  • Research Products

    (12 results)

All 2017 2016 2015 2014

All Journal Article (7 results) (of which Peer Reviewed: 6 results,  Acknowledgement Compliant: 4 results,  Open Access: 2 results) Presentation (3 results) Patent(Industrial Property Rights) (2 results)

  • [Journal Article] Identification of Small Molecule Inhibitors for Influenza A Virus Using In Silico and In Vitro Approaches,2017

    • Author(s)
      Makau JN, Watanabe K, Ishikawa T, Mizuta S, Hamada T, Kobayashi N, Nishida N
    • Journal Title

      PLoS ONE

      Volume: 12 Issue: 3 Pages: e0173582-e0173582

    • DOI

      10.1371/journal.pone.0173582

    • NAID

      120006987539

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Open Access
  • [Journal Article] Computational study of the competitive binding of valproic acid glucuronide and carbapenem antibiotics to acylpeptide hydrolase2017

    • Author(s)
      Takeshi Ishikawa, Hiroki Otaki, Satoshi Mizuta, Masami Kuriyama, Osamu Onomura, Norihide Higuchi, Mihoko N. Nakashima, Mikiro Nakashima and Kaname Ohyama
    • Journal Title

      Drug Metabolism and Pharmacokinetics

      Volume: 印刷中 Issue: 4 Pages: 201-207

    • DOI

      10.1016/j.dmpk.2017.04.002

    • NAID

      210000159704

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Ionic Liquid-Mediated Hydrofluorination of o-Azaxylylenes Derived From 3-Bromo-oxindoles2017

    • Author(s)
      Satoshi Mizuta, Hiroki Otaki, Ayako Kitagawa , Kanami Kitamura, Yuki Morii, Jun Ishihara, Kodai Nishi, Ryo Hashimoto, Toshiya Usui, and Kenya Chiba
    • Journal Title

      Organic Letters

      Volume: 印刷中 Issue: 10 Pages: 2572-2575

    • DOI

      10.1021/acs.orglett.7b00887

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Activity of N,N'-dialkyl-2-trifluoromethylthioimidazolium salts as phase-transfer catalyst for the alkylation of active methylene compounds2016

    • Author(s)
      Satoshi Mizuta, Kanami Kitamura, Kodai Nishi, Ryo Hashimoto, Toshiya Usui, and Kenya Chiba
    • Journal Title

      RSC Advances

      Volume: 6 Issue: 49 Pages: 43159-43162

    • DOI

      10.1039/c6ra06870g

    • Related Report
      2016 Annual Research Report 2015 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] 3,3-Dibromo-2-trifluoromethyl Acrylic Acid Ethyl Ester: A Versatile Platform for the Stereoselective Preparation of Functionalized- α-Trifluoromethyl α,β-Unsaturated Lactones and Trifluoromethyl Pyrazolinones2016

    • Author(s)
      Mizuta S, Otaki H. Kitamura, K, Nishi K, Watanabe K, Makau J. N, Hashimoto R, Usui T, Chiba K
    • Journal Title

      Org. Chem. Front.

      Volume: 3 Issue: 12 Pages: 1661-1667

    • DOI

      10.1039/c6qo00360e

    • NAID

      120006987602

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Acknowledgement Compliant
  • [Journal Article] Neutrophils and the S100A9 protein critically regulate granuloma formation2016

    • Author(s)
      Yuya Yoshioka, Tatsuaki Mizutani, Satoshi Mizuta, Ayumi Miyamoto, Satoru Murata, Toshiaki Ano, Hiroshi Ichise, Daisuke Morita, Hiroyuki Yamada, Yoshihiko Hoshino, Tatsuaki Tsuruyama and Masahiko Sugita
    • Journal Title

      Blood Advances

      Volume: 1 Issue: 3 Pages: 184-192

    • DOI

      10.1182/bloodadvances.2016000497

    • Related Report
      2016 Annual Research Report
    • Peer Reviewed / Open Access / Acknowledgement Compliant
  • [Journal Article] ピリジン、ジアジン類の位置選択的C-Hフッ素化反応2014

    • Author(s)
      水田賢志
    • Journal Title

      ファルマシア;トピックス

      Volume: 50 Pages: 1032-1032

    • NAID

      130005265890

    • Related Report
      2014 Annual Research Report
  • [Presentation] イオン性液体を媒体とした求核的フッ素化反応2017

    • Author(s)
      森井優樹、石原淳、畑山範、水田賢志
    • Organizer
      第137年回日本薬学会
    • Place of Presentation
      東北大学(宮城県、仙台市)
    • Year and Date
      2017-03-24
    • Related Report
      2016 Annual Research Report
  • [Presentation] 有機合成を基盤とした創薬研究支援2016

    • Author(s)
      水田賢志
    • Organizer
      分子標的医学研究センターシンポジウム
    • Place of Presentation
      長崎大学グローバルヘルス研究棟1階 (長崎県・長崎市)
    • Year and Date
      2016-01-07
    • Related Report
      2015 Annual Research Report
  • [Presentation] New advances in radiosynthesis of [18F]trifluoromethylarenes2015

    • Author(s)
      Satoshi Mizuta, Veronique Gouverneur
    • Organizer
      第10回日本分子イメージング学会総会
    • Place of Presentation
      タワーホール船堀 (東京都・江戸川区船堀4)
    • Year and Date
      2015-05-20
    • Related Report
      2015 Annual Research Report
  • [Patent(Industrial Property Rights)] キノリノン化合物および抗RNAウイルス治療薬2017

    • Inventor(s)
      水田賢志、渡邊健、西田教行、濱田剛、石川岳志、田中義正、大滝大樹
    • Industrial Property Rights Holder
      水田賢志、渡邊健、西田教行、濱田剛、石川岳志、田中義正、大滝大樹
    • Industrial Property Rights Type
      特許
    • Industrial Property Number
      2017-072230
    • Filing Date
      2017-03-31
    • Related Report
      2016 Annual Research Report
  • [Patent(Industrial Property Rights)] 新規放射線防護剤2016

    • Inventor(s)
      植田弘師、出口雄一、永井潤、水田賢志、鈴木啓司、松下洋輔、酒井
    • Industrial Property Rights Holder
      植田弘師、出口雄一、永井潤、水田賢志、鈴木啓司、松下洋輔、酒井
    • Industrial Property Rights Type
      特許
    • Industrial Property Number
      2016-142646
    • Filing Date
      2016-07-20
    • Related Report
      2016 Annual Research Report

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Published: 2014-04-04   Modified: 2018-03-22  

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