2020 Fiscal Year Final Research Report
Development of cleavable linker using third-period elements and azides
| Project/Area Number |
19K15711
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| Research Category |
Grant-in-Aid for Early-Career Scientists
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| Allocation Type | Multi-year Fund |
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| Review Section |
Basic Section 37030:Chemical biology-related
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| Research Institution | Nagoya University |
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Principal Investigator |
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| Project Period (FY) |
2019-04-01 – 2021-03-31
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| Keywords | 第三周期元素 / 有機硫黄化合物 / スルホンアミド / 有機リン化合物 / ホスフィン / アジド / 切断可能リンカー / ケミカルバイオロジー |
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| Outline of Final Research Achievements |
Cleavable linkers, that is, spacers which can be broken at the appropriate time and place, have important roles in chemical biology. However, it is difficult to achieve both stability and mild cleavage conditions, and the development of an ideal linker that is easier to use is required. In this context, in this study, we focused on the third period elements such as phosphorus or sulfur, which have characteristic properties, and by introduction of the azido group at the α position, we succeeded in development of a linker that can be selectively cleaved under mild conditions such as treatment of phosphines. We also found that the third period element can be replaced by treatment of a thiol and a base.
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| Free Research Field |
ケミカルバイオロジー
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| Academic Significance and Societal Importance of the Research Achievements |
今回開発した切断可能リンカーは、多くの条件では安定な一方で、穏和な条件では切断できることから、生物系も含めた幅広い状況で、適切な時に適切な場所で機能性分子を切断できることが期待される。このリンカーを用いて生命現象を化学的な観点から明らかにすることができれば、医学の発展に貢献できるものと考えられる。また、第三周期元素とアジドを組み合わせた新規化合物を取り扱う中で、今までに見られない置換反応を見いだすことができ、有機合成化学の領域からも興味深い地検を得ることができた。
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