Innovative Asymmetric Synthesis of Pharmaceuticals Through Strategic Development of Multifunctional and Multimetallic Catalysts

2010 Fiscal Year Self-evaluation Report

• Project/Area Number: 20229001
• Research Category: Grant-in-Aid for Scientific Research (S)
• Allocation Type: Single-year Grants
• Research Field: Chemical pharmacy
• Research Institution: Microbial Chemistry Research Foundation (2011-2012); The University of Tokyo (2008-2010)
• Principal Investigator: SHIBASAKI Masakatsu 公益財団法人微生物化学研究会, 微生物化学研究所, 所長 (30112767)
• Project Period (FY): 2008 – 2012
• Keywords: 不斉合成

Research Abstract

医薬品は極めて高度かつ多領域にわたる科学を集約した人類の叡智の結晶であり、全人類の福祉に直結するものである。実際の化合物を最小限の環境負荷でグローバルに供給するには既存の有機合成化学技術に抜本的躍進が必要であり、医薬品開発における最重要課題の一つである。多核不斉触媒の特徴を最大限に活用した新たな多核不斉触媒の創製に加え、触媒の反応促進機構及び立体選択性発現機構を種々の分光学的手法を用いた包括的なメカニズム解析により明らかにし、新たな触媒概念の礎となる新知見を積極的に見出す。さらに、独自に開発した不斉触媒反応を基盤とした医薬の実践的化学合成へと展開する。

Research Products

• [Journal Article] Direct Catalytic Asymmetric Vinylogous Mannich-type and Michael Reactions of an α, β-Unsaturated-Butyrolactam Under Dinuclear Nickel Catalysis (2010)
  • Author(s): N.E.Shepherd, H.Tanabe, Y.Xu, S.Matsunaga, M.Sibasaki
  • Journal Title: J.Am.Chem.Soc. 132 Pages: 5036
  • Peer Reviewed
• [Journal Article] Managing Highly Coordinative Substrates in Asymmetric Catalysis : A Catalytic Asymmetric Amination with a Lanthanum-Based Ternary Catalyst (2009)
  • Author(s): T.Mashiko, N.Kumagai, M.Shibasaki
  • Journal Title: J.Am.Chem.Soc. 131 Pages: 14990-14999
  • Peer Reviewed
• [Journal Article] Recent Progress in Asymmetric Bifunctional Catalysis Using Multimetallic Systems (2009)
  • Author(s): M.Shibasaki, M.Kanai, S.Matsunaga, N.Kumagai
  • Journal Title: Acc.Chem.Res. 42 Pages: 1117-1127
  • Peer Reviewed
• [Journal Article] A Synthesis of Tamiflu Based on a Barium-Catalyzed Asymmetric Diels?Alder-Type Reaction (2009)
  • Author(s): K.Yamatsugu, L.Yin, S.Kamijo, Y.Kimura, M.Kanai
  • Journal Title: Angew.Chem.Int.Ed. 48 Pages: 1070-1076
  • Peer Reviewed
• [Presentation] Practical Catalytic Asymmetric Synthesis of Promising Drug Candidates (2010)
  • Author(s): M.Shibasaki
  • Organizer: 3rd EuCheMS Chemistry Congress
  • Place of Presentation: Nurnberg, Germany
  • Year and Date: 2010-08-31
• [Presentation] Practical Catalytic Asymmetric Synthesis of Promising Drug Candidates (2010)
  • Author(s): M.Shibasaki
  • Organizer: 6th Eurasian Meeting on Heterocyclic Chemistry (6th EAMHC)
  • Place of Presentation: University of Alicante, Alicante, Spain
  • Year and Date: 2010-07-03
• [Presentation] Recent Progress in Asymmetric Two-Center Catalysis (2009)
  • Author(s): M.Shibasaki
  • Organizer: Scientific seminar at WuXi PharmaTech
  • Place of Presentation: WuXi PharmaTech Co., Ltd.Shanghai
  • Year and Date: 2009-02-13
• [Presentation] Recent Progress in Asymmetric Two-Center Catalysis (2009)
  • Author(s): M.Shibasaki
  • Organizer: Abbott lecture
  • Place of Presentation: Chicago, USA
  • Year and Date: 2009-02-03
• [Presentation] Recent Progress in Asymmetric Two-Center Catalysis (2009)
  • Author(s): M.Shibasaki
  • Organizer: Invited lecture
  • Place of Presentation: Univ.of Chicago, USA
  • Year and Date: 2009-02-02
• [Patent(Industrial Property Rights)] チオアミド化合物、チオアミド化合物の製造方法、[(4R,6R)-6-アミノエチル-1,3-ジオキサン-4-イル]アセテート誘導体の製造方法、及びアトルバスタチンの製造方法 (2011)
  • Inventor(s): 柴崎正勝, 熊谷直哉
  • Industrial Property Rights Holder: (財)微生物化学研究会
  • Industrial Property Number: 特願,2011-035006
  • Filing Date: 2011-02-21
• [Patent(Industrial Property Rights)] 立体選択的不斉ニトロアルドール反応用触媒 (2009)
  • Inventor(s): 二田原達也, 熊谷直哉, 柴崎正勝
  • Industrial Property Rights Holder: 東京大学
  • Industrial Property Number: 特願,2009-01394
  • Filing Date: 2009-01-26