Development of new transformation of polycyclic aromatic compounds utilizing reactive carbon-iodine(III) bond
| Project/Area Number |
16K18854
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| Research Category |
Grant-in-Aid for Young Scientists (B)
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| Allocation Type | Multi-year Fund |
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| Research Field |
Chemical pharmacy
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| Research Institution | Meijo University |
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Principal Investigator |
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| Project Period (FY) |
2016-04-01 – 2019-03-31
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| Project Status |
Completed (Fiscal Year 2018)
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| Budget Amount *help |
¥3,900,000 (Direct Cost: ¥3,000,000、Indirect Cost: ¥900,000)
Fiscal Year 2018: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2017: ¥1,170,000 (Direct Cost: ¥900,000、Indirect Cost: ¥270,000)
Fiscal Year 2016: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
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| Keywords | ヨウ素 / 芳香環 / 複素環 / 多環式 / 核酸塩基 / 有機ヨウ素 |
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| Outline of Final Research Achievements |
We have developed the new metal-free coupling method of nucleobase derivatives such as purines toward nucleophiles (i.e. electron-rich arenes or amines), and facile synthesis of uracil-iodonium(III) salts as new attractive synthetic modules of these nucleobases. We have investigated in detail the optimized conditions for generating highly strained heterocyclic alkyne species from uracil-iodonium(III) salts with basic activation, which have led to development of the new vicinal functionalization of the uracil ring in a single synthetic operation.
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| Academic Significance and Societal Importance of the Research Achievements |
核酸塩基のなかでも、ウラシル骨格は抗がん活性や抗ウイルス活性等を示す医薬品のファーマコアとして重要な機能を有しており、ウラシルのふたつの二重結合炭素を官能基化する手法を開発することは、創薬化学分野において重要である。本研究で開発したウラシルのビシナル官能基化法を用いると、合成難易度の高い複雑な芳香環化合物の骨格構築を高効率に行うことが可能であり、医薬品関連分子や機能性分子の創生研究への寄与につながりうる。
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Report
(4 results)
Research Products
(25 results)
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[Journal Article] Atropisomeric chiral diiododienes, (Z,Z)-2,3-di(1-iodoalkylidene)tetralins: Synthesis, enantiomeric resolution, and application in asymmetric catalysis2017
Author(s)
M. Ogasawara, H. Sasa, H. Hu, Y. Amano, H. Nakajima, N. Takenaga, K. Nakajima, Y. Kita, T. Takahashi, T. Dohi
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Journal Title
Org. Lett.
Volume: 19
Issue: 15
Pages: 4102-4105
DOI
NAID
Related Report
Peer Reviewed / Open Access
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