Synthesis of Heterocycles Making Use of Transition-Metal Catalyzed C-H Functionalization
| Project/Area Number |
16K08187
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Multi-year Fund |
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| Section | 一般 |
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| Research Field |
Chemical pharmacy
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| Research Institution | Mukogawa Women's 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 |
¥4,810,000 (Direct Cost: ¥3,700,000、Indirect Cost: ¥1,110,000)
Fiscal Year 2018: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2017: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2016: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
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| Keywords | 炭素－水素結合官能基化 / 銅触媒 / アミノ化 / 複素環化合物 / キサンチン / 触媒・化学プロセス / 有機化学 / 遷移金属 / C-H官能基化 |
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| Outline of Final Research Achievements |
In recent years, substantial progress has been made in the development of new transformations via the transition-metal-catalyzed functionalization of unreactive C-H bonds, which can provide more efficient and straightforward alternatives to conventional cross-coupling methods. Herein, the author found a novel catalytic method for synthesizing xanthins via C-H functionalization. The process involves copper-catalyzed intramolecular C-H amination of benzamidines that possess a uracil moiety and produces variously substituted xanthines generally in good to high yields. This work introduces a new, facile approach to polysubstituted xanthine compounds.
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| Academic Significance and Societal Importance of the Research Achievements |
複素環骨格を有する化合物は，医薬品や生理活性天然物などの母核として広く存在している，極めて重要な化合物群の１つである．それゆえ，複素環化合物の合成および修飾に関しては，古くから多くの研究がおこなわれてきた．しかしながら既存の手法においては，反応条件が過酷であるため基質適用範囲が狭い，毒性の高い試薬を過剰量用いる必要がある，などといった問題点も残されており，より効率的な複素環合成・修飾法の開発は，非常に意義深い．本研究における C-H 閉環による複素環構築法は，効率性および実用性の観点から，既存の手法に比べて優位性を大きくアピールできる．基礎・応用化学いずれの分野にも大きな波及効果が予想される．
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Report
(4 results)
Research Products
(24 results)
