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2020 Fiscal Year Final Research Report

Radical-initiated C-H functionalization of cubane for medicinal chemistry

Research Project

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Project/Area Number 19K23792
Research Category

Grant-in-Aid for Research Activity Start-up

Allocation TypeMulti-year Fund
Review Section 0801:Pharmaceutical sciences and related fields
Research InstitutionTohoku University

Principal Investigator

Nagasawa Shota  東北大学, 薬学研究科, 助教 (50846425)

Project Period (FY) 2019-08-30 – 2021-03-31
Keywordsキュバン / CーH官能基化 / 創薬化学
Outline of Final Research Achievements

Unfortunately, an appropriate directing groups and conditions for radical-initiated C-H functionalization have not been found. On the other hand, introduction of an acetoxy group into cubane skeleton have been achieved by applying reaction conditions for transition-metal catalyzed C-H functionalization. Furthermore, the obtained acetoxylated compound could be converted into a cubane analog of pharmaceutically important aromatics. Preparation of manuscript including these result is underway.

Free Research Field

有機合成化学

Academic Significance and Societal Importance of the Research Achievements

有機化合物に遍在するC-H結合を直接変換する手法は世界中の研究者が鎬を削って研究を行っている分野であるが,キュバンのような「特殊系」における方法論はほとんど研究されておらず,特にC-H結合活性化を経るものは皆無である.この結果は,有機合成化学的に挑戦的とされる分子変換を,これまでとは異なるアプローチで達成したという学術的意義に加えて,未開拓ケミカルスペースへのアクセスを可能にし,これまで考えられなかった分子設計による新たな機能性分子・医薬品の創生を促しうるという社会的意義を有する.

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Published: 2022-01-27  

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