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Development of practical organic synthetic methods contributing to drug discovery by using toxic gas surrogates

Research Project

Project/Area Number 18K06584
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeMulti-year Fund
Section一般
Review Section Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
Research InstitutionUniversity of Shizuoka

Principal Investigator

Konishi Hideyuki  静岡県立大学, 薬学部, 准教授 (20565618)

Project Period (FY) 2018-04-01 – 2021-03-31
Project Status Completed (Fiscal Year 2020)
Budget Amount *help
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2020: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2019: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2018: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Keywords毒性ガス / 等価体 / 一酸化炭素 / 二酸化硫黄 / 安全 / 実用的 / 実用 / 触媒
Outline of Final Research Achievements

Using "toxic gas surrogates" that can generate toxic gases such as carbon monoxide and sulfur dioxide by chemical reactions, we have established novel synthetic methods with high safety, simplicity, and reliability. We have also expanded their potential applications in drug discovery research. We have developed the synthetic method for unsymmetric ketones using novel carbon monoxide surrogates, symmetric sulfones and sulfides using sulfur dioxide surrogates, and the development of an insane open-air carbonylation, demonstrating the further utility of toxic gas surrogates in synthetic organic chemistry.

Academic Significance and Societal Importance of the Research Achievements

化学反応により毒性ガスを生成できる「毒性ガス等価体」の開発およびそれを用いる新規反応の開発を行い、モノづくりの根幹を成す有機合成化学において高い安全性と効率性、実用性を有する新たな合成手法を見出すことができた。これにより、互いに混じりにくい気体と溶液が関与する反応を、溶液中のみで行う反応へと転換して化学反応を行う、という新たな概念を実証した。さらに、非常識とも言える開放系カルボニル化反応などの開発を通して、この概念が創薬化学においても即戦力で利用できることを示した。本研究の成果は、毒性ガス等価体のさらなる有用性を示すとともに、有機合成化学や創薬研究の発展に新たな指針を与えるものである。

Report

(4 results)
  • 2020 Annual Research Report   Final Research Report ( PDF )
  • 2019 Research-status Report
  • 2018 Research-status Report
  • Research Products

    (19 results)

All 2020 2019 2018 Other

All Journal Article (6 results) (of which Peer Reviewed: 6 results) Presentation (11 results) (of which Int'l Joint Research: 4 results,  Invited: 3 results) Remarks (2 results)

  • [Journal Article] Synthesis of 2,3-disubstituted indoles from alkynylanilines and 2-chlorophenols using palladium-dihydroxyterphenylphosphine catalyst2020

    • Author(s)
      Yamaguchi, Miyuki; Ogihara, Kota; Konishi, Hideyuki; Manabe, Kei
    • Journal Title

      Tetrahedron Letters

      Volume: - Issue: 21 Pages: 151896-151896

    • DOI

      10.1016/j.tetlet.2020.151896

    • Related Report
      2020 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Discussion Addendum for: Pd-Catalyzed External-CO-Free Carbonylation: Preparation of 2,4,6-Trichlorophenyl 3,4- Dihydronaphthalene-2-Carboxylate2020

    • Author(s)
      Hideyuki Konishi, Kei Manabe
    • Journal Title

      Organic Syntheses

      Volume: 97 Pages: 125-138

    • DOI

      10.15227/orgsyn.097.0125

    • Related Report
      2020 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Direct C3-Selective Arylation of N-Unsubstituted Indoles with Aryl Chlorides, Triflates, and Nonaflates Using a Palladium-Dihydroxyterphenylphosphine Catalyst2020

    • Author(s)
      Miyuki Yamaguchi, Ryoya Hagiwara, Kanami Gayama, Kohei Suzuki, Yusuke Sato, Hideyuki Konishi, Kei Manabe
    • Journal Title

      The Journal of Organic Chemistry

      Volume: 85 Issue: 16 Pages: 10902-10912

    • DOI

      10.1021/acs.joc.0c01494

    • Related Report
      2020 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Palladium-catalyzed external-CO-free reductive carbonylation of aryl sulfonates2020

    • Author(s)
      Hideyuki Konishi, Minoru Kumon, Miyuki Yamaguchi, Kei Manabe
    • Journal Title

      Tetrahedron

      Volume: 76 Issue: 48 Pages: 131639-131639

    • DOI

      10.1016/j.tet.2020.131639

    • Related Report
      2020 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Palladium-catalyzed One-step Synthesis of Symmetrical Diaryl Sulfones from Aryl Halides and a Sulfur Dioxide Surrogate2019

    • Author(s)
      Hiromichi Tanaka, Hideyuki Konishi, Kei Manabe
    • Journal Title

      Chemistry Letters

      Volume: 48 Issue: 8 Pages: 760-763

    • DOI

      10.1246/cl.190300

    • NAID

      130007687708

    • Related Report
      2019 Research-status Report
    • Peer Reviewed
  • [Journal Article] Recent Progress on Catalytic Heck Carbonylations Using Carbon Monoxide Surrogates2019

    • Author(s)
      Hideyuki Konishi, Kei Manabe
    • Journal Title

      Tetrahedron Letters

      Volume: 60 Issue: 42 Pages: 151147-151147

    • DOI

      10.1016/j.tetlet.2019.151147

    • Related Report
      2019 Research-status Report
    • Peer Reviewed
  • [Presentation] 二酸化硫黄等価体を用いる新規4H-thiochromen-4-one類合成法の開発2020

    • Author(s)
      杉田あすか、小西英之、眞鍋敬
    • Organizer
      日本病院薬剤師会東海ブロック・日本薬学会東海支部合同学術大会2020
    • Related Report
      2020 Annual Research Report
  • [Presentation] 二酸化硫黄等価体を用いる新規4H-thiochromen-4-one類合成法の開発2020

    • Author(s)
      杉田 あすか、小西 英之、眞鍋 敬
    • Organizer
      日本薬学会第140年会
    • Related Report
      2019 Research-status Report
  • [Presentation] Rapid and Practical Synthesis of Fluoren-9-ones Using a Carbon Monoxide Surrogate2019

    • Author(s)
      Hideyuki Konishi, Suguru Futamata, Xi Wang, Kei Manabe
    • Organizer
      The 4th International Symposium on Process Chemistry (selected as oral presentation)
    • Related Report
      2019 Research-status Report
    • Int'l Joint Research
  • [Presentation] CO等価体を用いる開放系におけるカルボニル化反応の開発2019

    • Author(s)
      坂本紅星、松原美香、小西英之、眞鍋敬
    • Organizer
      日本薬学会第139年会
    • Related Report
      2018 Research-status Report
  • [Presentation] Toxic Gas Surrogates for Safe and Practical Reactions2019

    • Author(s)
      Hideyuki Konishi
    • Organizer
      The 4th International Symposium on Catalysis toward Green Sustainable Chemistry (CAT-GSC-4)
    • Related Report
      2018 Research-status Report
    • Int'l Joint Research / Invited
  • [Presentation] 一酸化炭素等価体を用いる安全かつ実用的な触媒的カルボニル化反応2018

    • Author(s)
      小西英之、福田匡貴、関野智行、上田剛、眞鍋敬
    • Organizer
      日本プロセス化学会2018サマーシンポジウム
    • Related Report
      2018 Research-status Report
  • [Presentation] Carbon Monoxide Surrogates for Safe, Practical, and Catalytic Reactions2018

    • Author(s)
      Hideyuki Konishi
    • Organizer
      The 1st International Symposium of Soft Molecular Activation Research Center (SMARC)
    • Related Report
      2018 Research-status Report
    • Int'l Joint Research / Invited
  • [Presentation] Carbon Monoxide Surrogates for Safe, Practical, and Catalytic Reactions2018

    • Author(s)
      Hideyuki Konishi
    • Organizer
      The International Congress on Pure & Applied Chemistry (ICPAC) Langkawi 2018
    • Related Report
      2018 Research-status Report
    • Int'l Joint Research / Invited
  • [Presentation] SO2等価体を用いる一段階対称ジアリールスルホン合成法の開発2018

    • Author(s)
      田中寛康、小西英之、眞鍋敬
    • Organizer
      日本病院薬剤師会東海ブロック・日本薬学会東海支部 合同学術大会2018
    • Related Report
      2018 Research-status Report
  • [Presentation] 新規CO等価体を用いるCO挿入を伴う還元的クロスカップリングによる非対称ケトン合成法の開発2018

    • Author(s)
      上原尚也、小西英之、眞鍋敬
    • Organizer
      日本病院薬剤師会東海ブロック・日本薬学会東海支部 合同学術大会2018
    • Related Report
      2018 Research-status Report
  • [Presentation] 一酸化炭素等価体を用いる フルオレノン類の触媒的迅速合成法の開発2018

    • Author(s)
      小西英之、二俣傑、王晰、眞鍋敬
    • Organizer
      第44回反応と合成の進歩シンポジウム
    • Related Report
      2018 Research-status Report
  • [Remarks] 静岡県立大学薬学部 医薬品化学分野・薬化学講座 ホームページ

    • URL

      https://w3pharm.u-shizuoka-ken.ac.jp/yakka/

    • Related Report
      2020 Annual Research Report 2019 Research-status Report 2018 Research-status Report
  • [Remarks] 静岡県立大学薬学部 医薬品化学分野・薬化学講座 発表論文

    • URL

      https://w3pharm.u-shizuoka-ken.ac.jp/yakka/paper.html

    • Related Report
      2020 Annual Research Report 2019 Research-status Report 2018 Research-status Report

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Published: 2018-04-23   Modified: 2022-01-27  

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