A sequential ligation reaction via strained-ring cleavage triggered by Staudinger reaction
| Project/Area Number |
17K17749
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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
Drug development chemistry
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| Research Institution | University of Toyama |
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Principal Investigator |
Kohyama Aki 富山大学, 学術研究部薬学・和漢系, 助教 (40778586)
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| Project Period (FY) |
2017-04-01 – 2020-03-31
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| Project Status |
Completed (Fiscal Year 2019)
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| Budget Amount *help |
¥4,420,000 (Direct Cost: ¥3,400,000、Indirect Cost: ¥1,020,000)
Fiscal Year 2019: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Fiscal Year 2018: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2017: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
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| Keywords | ベンゾシクロブテン / Staudinger反応 / クリック反応 / アジド / オルトキノジメタン / 生体直交型反応 / Diels-Alder反応 / 有機化学 / 薬学 |
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| Outline of Final Research Achievements |
Herein, we developed a novel method to generate highly active species, o-quinodimethanes (OQMs) at room temperature. The reaction involves ring cleavage of the intermediate after a stable substrate was converted to a reactive molecule at room temperature.
The OQMs are so highly reactive that they act as “glue” to bind with partner molecules. Thus, we also developed a novel ligation reaction via OQMs at room temperature.
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| Academic Significance and Societal Importance of the Research Achievements |
我々の方法が開発されるまで，オルトキノジメタンの発生法は，加熱や強アルカリ条件が必要とされてきた。今回開発した方法は，そのような過酷な反応条件を必要としない世界で初めての方法である。今までにないオルトキノジメタン利用法の開拓に大きく貢献する方法と位置付けられる。
具体的には，生体分子の修飾反応や，ステロイド等の医薬分子合成といった生命化学・創薬分野への応用展開が今後期待される。
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Report
(4 results)
Research Products
(18 results)
