2020 Fiscal Year Final Research Report
Development of novel reagents taking the advantage of the electron deficient nitrogen-containing heterocycles
Project/Area Number |
17H03970
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Research Category |
Grant-in-Aid for Scientific Research (B)
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Allocation Type | Single-year Grants |
Section | 一般 |
Research Field |
Chemical pharmacy
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Research Institution | Kanazawa University |
Principal Investigator |
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Co-Investigator(Kenkyū-buntansha) |
三代 憲司 金沢大学, 新学術創成研究機構, 准教授 (60776079)
藤田 光 金沢大学, 薬学系, 助教 (40782850)
山田 耕平 金沢大学, 薬学系, 助教 (40583232)
北村 正典 金沢大学, 薬学系, 准教授 (80453835)
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Project Period (FY) |
2017-04-01 – 2021-03-31
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Keywords | トリアジン / 含窒素芳香族化合物 / 縮合剤 / アルキル化剤 / エポキシ化剤 |
Outline of Final Research Achievements |
In this project, we aim to develop new reagents by maximizing the potential of π-electron deficient nitrogen-containing heterocyclic compounds such as triazines. This research was carried out based on the knowledge of the preparation methods and the correlation between the structure and the reactivities of these heterocycles, which we have elucidated and accumulated over the years. Specifically, we have developed reagents such as dehydrating condensing agents, alkylating agents, and oxidizing agents, which are composed of second period elements (C, N, O) without the use of heavy metals, and are superior to conventional agents in terms of reactivity, chemoselectivity, safety, stability, and cost.
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Free Research Field |
化学系薬学
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Academic Significance and Societal Importance of the Research Achievements |
リード最適化などの創薬研究においては、短期間に多数の低分子化合物の合成が求められるため、反応条件のチューニングを必要とせず、基質適用性が広く、官能基許容性が高い信頼のおける反応が多用される。報告によれば、アルキル化反応、縮合反応、パラジウムカップリング反応だけで全体の半数を占め、保護基の導入、酸化反応などがそれに続く。本研究課題で開発した反応剤は、こうしたニーズに応えうる優れた特長を有しており、創薬はもちろん生命科学研究の推進などに広く貢献しうる点で学術的、社会的に大きな意義を持つ。
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