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2011 Fiscal Year Final Research Report

Development of versatile 1, 2-Diamine synthetic methodology and its application for preparation of drug candidates.

Research Project

  • PDF
Project/Area Number 21590013
Research Category

Grant-in-Aid for Scientific Research (C)

Allocation TypeSingle-year Grants
Section一般
Research Field Chemical pharmacy
Research InstitutionKumamoto University

Principal Investigator

ISHIZUKA Tadao  熊本大学, 大学院・生命科学研究部, 教授 (60176203)

Project Period (FY) 2009 – 2011
Keywords有機化学 / ジアミン
Research Abstract

Synthetic strategy for chiral 1, 2-diamines, which are included in many kind of bioactive compounds, has been successfully developed.
The versatile chiral synthon, 4, 5-dimethoxy-2-imidazolidinone, has been prepared by FeCl_3 catalized epoxidation-ring cleavage with H_2O or t-BuOH process followed by optical resolution. Diastereomeric methodology with camphor-derived chiral carboxylic acid has also successed with 93% de.

  • Research Products

    (5 results)

All 2012 2011 2010 Other

All Journal Article (2 results) (of which Peer Reviewed: 2 results) Presentation (2 results) Remarks (1 results)

  • [Journal Article] A Simple, Iron-catalyzed, Pyridineassisted Hydrogen Peroxide Epoxidation System2011

    • Author(s)
      Mingyu, J., Matsunaga, H., Ishizuka, T.
    • Journal Title

      Chemical & Pharmaceutical Bulletin

      Volume: vol.59 Pages: 799-801

    • Peer Reviewed
  • [Journal Article] Sterically congested,"roofed"υ-iminodisulfides as new chiral ligands for palladium-catalyzed, asymmetric allylic alkylation2010

    • Author(s)
      Matsunaga, H., Tokuda, R., Nakajima, M., Ishizuka, T.
    • Journal Title

      Chemical & Pharmaceutical Bulletin

      Volume: vol.58 Pages: 1419-1421

    • Peer Reviewed
  • [Presentation] 鉄触媒酸化反応を利用した1, 2-ジアミンキラルシントン合成法の開発2012

    • Author(s)
      江下伊織、松永浩文、石塚忠男
    • Organizer
      日本薬学会第132年会
    • Place of Presentation
      北海道大学
    • Year and Date
      2012-03-30
  • [Presentation] 不斉酸化反応を用いた1, 2-ジアミン類キラルシントン効率合成法の開発と応用2011

    • Author(s)
      江下伊織、松永浩文、石塚忠男
    • Organizer
      第41回複素環化学討論会
    • Place of Presentation
      崇城大学市民ホール
    • Year and Date
      2011-10-20
  • [Remarks]

    • URL

      http://yakko.pharm.kumamoto-u.ac.jp/

URL: 

Published: 2013-07-31  

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