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Control of axial chirality and development of novel bioactive compounds with asymmetric axes.

Research Project

Project/Area Number 21790025
Research Category

Grant-in-Aid for Young Scientists (B)

Allocation TypeSingle-year Grants
Research Field Chemical pharmacy
Research InstitutionTeikyo University

Principal Investigator

TABATA Hidetsugu  Teikyo University, 薬学部, 助手 (80445634)

Project Period (FY) 2009 – 2010
Project Status Completed (Fiscal Year 2010)
Budget Amount *help
¥4,290,000 (Direct Cost: ¥3,300,000、Indirect Cost: ¥990,000)
Fiscal Year 2010: ¥2,080,000 (Direct Cost: ¥1,600,000、Indirect Cost: ¥480,000)
Fiscal Year 2009: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
Keywords動的キラリティー / 軸不斉 / ビアリール骨格 / アトロプ異性体 / カップリング反応
Research Abstract

The dibenzo[b,d]azepin-6-one nucleus, which constitutes the scaffold of the γ-secretase inhibitors LY-411575 and its analogs, has two sp^2-sp^2 asymmetric axes. We are interested in stereochemistry of the two asymmetric axes, and have reported the atropisomeric properties of dibenzo[b,d]azepin-6-one derivatives. Herein, we present a study on the stereochemistry of the eight-membered analog, dibenzo[b,d]azocin-6-one derivatives.

Report

(3 results)
  • 2010 Annual Research Report   Final Research Report ( PDF )
  • 2009 Annual Research Report
  • Research Products

    (15 results)

All 2011 2010 2009

All Journal Article (5 results) (of which Peer Reviewed: 5 results) Presentation (10 results)

  • [Journal Article] Atropisomerism in the Vaptan Class of Vasopressin Receptor Ligands : The Active Conformation Recognized by the Receptor.2011

    • Author(s)
      Hidetsugu Tabata, Jun Nakagomi, Daisuke Morizono, Tetsuta Oshitari, Hideyo Takahashi, Hideaki Natsugari.
    • Journal Title

      Angewwandte Chemie International Edition 50

      Pages: 3075-3079

    • Related Report
      2010 Final Research Report
    • Peer Reviewed
  • [Journal Article] Atropisomerism Ovserved in Indometacin Derivatives.2011

    • Author(s)
      Hideyo Takahashi, Shintaro Wakamatsu, Hidetsugu Tabata, Tetsuta Oshitari, Ayako Harada, Keizo Inoue, Hideaki Natsugari.
    • Journal Title

      Organic Letters 13

      Pages: 760-763

    • Related Report
      2010 Final Research Report
    • Peer Reviewed
  • [Journal Article] Atropisomerism in the Vaptan Class of Vasopressin Receptor Ligands : The Active Conformation Recognized by the Receptor2011

    • Author(s)
      田畑英嗣
    • Journal Title

      Angewandte Chemie International Edition

      Volume: 50 Pages: 3075-3079

    • Related Report
      2010 Annual Research Report
    • Peer Reviewed
  • [Journal Article] Atropisomeric Properties of 7-, 8-, and 9-Membered-Ring Dibenzolactams : Conformation, Thermal stability, and Chemical Reactivity.2010

    • Author(s)
      Tabata Hidetsugu, Suzuki Hiroyuki, Akiba Kumi, Takahashi Hideyo, Natsugari Hideaki.
    • Journal Title

      Journal of Organic Chemistry 75

      Pages: 5984-5993

    • Related Report
      2010 Final Research Report
    • Peer Reviewed
  • [Journal Article] Atropisomeric Properties of 7-, 8-, 9-Membered-Ring Dibenzolactams : Conformation, Thermal Stability, and Chemical Reactivity2010

    • Author(s)
      田畑英嗣
    • Journal Title

      Journal of Organic Chemistry

      Volume: 75 Pages: 5984-5993

    • Related Report
      2010 Annual Research Report
    • Peer Reviewed
  • [Presentation] ベンズアゼピノン誘導体の軸不斉とACAT阻害作用2011

    • Author(s)
      田畑英嗣
    • Organizer
      日本薬学会131年会
    • Place of Presentation
      静岡
    • Year and Date
      2011-03-31
    • Related Report
      2010 Final Research Report
  • [Presentation] ベンゾジアゼピノン誘導体の軸性キラリティーとACAT阻害活性2010

    • Author(s)
      田畑英嗣
    • Organizer
      第29回メディシナルケミストリーシンポジウム
    • Place of Presentation
      京都
    • Year and Date
      2010-11-28
    • Related Report
      2010 Final Research Report
  • [Presentation] ベンズアゼピノン誘導体の軸性キラリティーとACAT阻害活性-CDスペクトルは絶対配置の決め手になるか-2010

    • Author(s)
      田畑英嗣
    • Organizer
      第29回メディシナルケミストリーシンポジウム
    • Place of Presentation
      京都テルサ(京都府)
    • Year and Date
      2010-11-17
    • Related Report
      2010 Annual Research Report
  • [Presentation] 7/8/9員環ジベンゾラクタム類の軸性キラリティと立体化学2010

    • Author(s)
      田畑英嗣
    • Organizer
      第40回複素環化学討論会
    • Place of Presentation
      仙台
    • Year and Date
      2010-10-14
    • Related Report
      2010 Final Research Report
  • [Presentation] 7/8/9員環ジベンゾラクタム類の軸性キラリティと立体化学2010

    • Author(s)
      田畑英嗣
    • Organizer
      第40回複素環化学討論会
    • Place of Presentation
      仙台市民会館(宮城県)
    • Year and Date
      2010-10-14
    • Related Report
      2010 Annual Research Report
  • [Presentation] 軸性キラリティを有するビフェニルラクタム類の立体化学の解明2010

    • Author(s)
      田畑英嗣
    • Organizer
      日本薬学会第130年会
    • Place of Presentation
      岡山
    • Year and Date
      2010-03-30
    • Related Report
      2010 Final Research Report
  • [Presentation] ビフェニルラクタム類の軸性キラリティの解明2009

    • Author(s)
      田畑英嗣
    • Organizer
      第56回日本薬学会関東支部大会
    • Place of Presentation
      埼玉
    • Year and Date
      2009-10-03
    • Related Report
      2010 Final Research Report
  • [Presentation] ビフェニルラクタム類の軸性キラリティの解明2009

    • Author(s)
      田畑英嗣
    • Organizer
      第53回日本薬学会関東支部大会
    • Place of Presentation
      城西大学(埼玉県)
    • Year and Date
      2009-10-03
    • Related Report
      2009 Annual Research Report
  • [Presentation] ジベンゾ[b,d]アゼピン-6-オン誘導体の軸性キラリティーと立体化学2009

    • Author(s)
      田畑英嗣
    • Organizer
      第56回有機合成化学協会関東支部シンポジウム
    • Place of Presentation
      東京
    • Year and Date
      2009-05-09
    • Related Report
      2010 Final Research Report
  • [Presentation] ジベンゾ[b,d]アゼピン-6-オン誘導体の軸性キラリティーと立体化学2009

    • Author(s)
      田畑英嗣
    • Organizer
      第57回有機合成化学協会関東支部シンポジウム
    • Place of Presentation
      早稲田大学(東京都)
    • Year and Date
      2009-05-09
    • Related Report
      2009 Annual Research Report

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Published: 2009-04-01   Modified: 2016-04-21  

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