Development of highly reactive and stereoselective catalytic reaction toward formation and introduction of 4 membered ring

2023 Fiscal Year Final Research Report

• Project/Area Number: 20K06976
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Review Section: Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
• Research Institution: Musashino University
• Principal Investigator: Shigehisa Hiroki 武蔵野大学, 薬学部, 講師 (60612471)
• Project Period (FY): 2020-04-01 – 2024-03-31
• Keywords: 創薬化学 / 有機合成化学

Outline of Final Research Achievements

This research focuses on the development of new methodologies for constructing four-membered ring structures, expanding the promising chemical space for drug discovery. We primarily concentrated on synthesizing oxetanes and azetidines, achieving the capability to construct multiple novel four-membered ring building blocks. Through the optimization of reaction conditions, the yield of oxetane synthesis improved from an initial 42% to 90%. Additionally, we are pursuing research on stereoselective synthesis using chiral cobalt catalysts. If successful, this approach will contribute significantly to the synthesis of optically active compounds in pharmaceutical development, addressing a critical need for more efficient drug production processes.

Free Research Field

有機化学

Academic Significance and Societal Importance of the Research Achievements

本研究による４員環構造の合成法の開発は、医薬品開発における新規化合物の探索と合成の効率化を可能にする。特に、高い収率でのオキセタン合成技術は、溶解性と代謝安定性を兼ね備えた化合物の設計に寄与し、創薬の選択肢を広げることが期待される。また、キラルコバルト触媒を使用した立体制御技術の進展は、光学活性化合物の合成に新たな道を開く可能性があり、これは創薬だけでなく、化学合成の基本的な理解を深める上でも大きな意義がある。