Application of Chiral Nucleophilic Catalysts for Highly Difficult Molecular Transformations

2021 Fiscal Year Final Research Report

• Project/Area Number: 19K05456
• Research Category: Grant-in-Aid for Scientific Research (C)
• Allocation Type: Multi-year Fund
• Section: 一般
• Review Section: Basic Section 33020:Synthetic organic chemistry-related
• Research Institution: Gihu University of Medical Science
• Principal Investigator: Mandai Hiroki 岐阜医療科学大学, 薬学部, 准教授 (60534427)
• Co-Investigator(Kenkyū-buntansha): 菅 誠治 岡山大学, 自然科学研究科, 教授 (50291430)
• Project Period (FY): 2019-04-01 – 2022-03-31
• Keywords: 求核触媒 / アシル化 / 有機分子触媒

Outline of Final Research Achievements

In order to further exploration of difficult molecular transformations reactions using binaphthyl-based DMAP derivatives, we worked on (1) structural elucidation of N-acylpyridinium salts important for enantioselectivity, (2) development of enantioselective (or regioselective) acylation of polyols, and (3) development of simple immobilized catalysts for acylation. In each research field, In each of these research items, we were able to obtain unprecedented knowledge. In particular, we obtained various the acylation of polyols yielded results that exceeded our initial expectations.

Free Research Field

有機合成化学

Academic Significance and Societal Importance of the Research Achievements

本研究成果は，医薬品，農薬，天然物などの生物活性化合物合成に利用できるキラルビルディング（キラル合成素子）を迅速かつ効率的に合成できる方法であり，従来の触媒ではなし得なかった高選択的な分子変換を実現できた。将来的には医薬品や農薬などのファインケミカルの分野に大きく波及するものと期待している。