Development of novel polyol synthesis using unprotected alcohols

2023 Fiscal Year Final Research Report

• Project/Area Number: 21K15220
• Research Category: Grant-in-Aid for Early-Career Scientists
• Allocation Type: Multi-year Fund
• Review Section: Basic Section 47010:Pharmaceutical chemistry and drug development sciences-related
• Research Institution: The University of Tokyo
• Principal Investigator: Harunobu Mitsunuma 東京大学, 大学院薬学系研究科(薬学部), 助教 (20823818)
• Project Period (FY): 2021-04-01 – 2024-03-31
• Keywords: 医薬品合成 / 原子効率 / 短工程 / 保護基フリー / 触媒

Outline of Final Research Achievements

The polyol skeleton is a critical structure frequently encountered in numerous bioactive molecules, pharmaceuticals, and functional materials. Historically, various methodologies have been developed for the construction of this skeleton, yet challenges related to reaction efficiency, the number of steps, and atom economy often persist, and an ideal synthetic method has not yet been established. I discovered that using readily accessible simple alkenes as nucleophiles, and employing a consecutive catalytic allylation reaction to aldehydes, which does not require the protection of hydroxyl groups, leads to an efficient synthesis of 1,3-polyols.

Free Research Field

薬学

Academic Significance and Societal Importance of the Research Achievements

本研究成果では1，3ポリオール合成を無保護にて行う炭素伸長法を開発した。これは今までに前例がなく学術的に価値がある。これにより余計な工程数やごみの排出を抑え、医薬品や生物活性分子の迅速合成が可能になることが予想される。ひいては新規医薬シーズの発見や合成コストの低下による薬価削減につながるものだと考えている。