| Project/Area Number |
17K05870
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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 |
Synthetic chemistry
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| Research Institution | Doshisha University |
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Principal Investigator |
OE Yohei 同志社大学, 生命医科学部, 教授 (20512734)
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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 |
¥4,680,000 (Direct Cost: ¥3,600,000、Indirect Cost: ¥1,080,000)
Fiscal Year 2019: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2018: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2017: ¥1,820,000 (Direct Cost: ¥1,400,000、Indirect Cost: ¥420,000)
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| Keywords | ルテニウム / アルキル化反応 / 触媒反応 / Borrowing Hydrogen法 / 遷移金属錯体触媒 / 水素移動 / アルキル化 / 均一系触媒反応 / アトムエコノミー |
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| Outline of Final Research Achievements |
Aromatic rings and heteroaromatic rings are often found as frameworks in pharmaceuticals. Therefore, modifications of these side chains are important organic transformation to synthesize various drag candidates. In general, alkylations of side chains of these compounds are carried out by use of stoichiometric amount of strong base and alkyl halides. However, the use of alkyl halides and stoichiometric amount of strong base should be avoided from the viewpoint of green chemistry. Under such social demands, the author investigated the development of a new heterocyclic side chain modification method using the catalytic "Borrowing Hydrogen" methodology (BH method), where alcohols were used as alkylating agents. As a result, several useful findings have been obtained, including the development of a new alkylation method for the side chain of the heteroaromatic ring using the Ru/In concerted catalysis.
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| Academic Significance and Societal Importance of the Research Achievements |
現代の有機合成化学では、触媒を利用した精密な分子変換反応を効率的に行うことで多段階合成を短縮化することが求めらる．本研究は、従来、アルコールをハロアルカンやその誘導体へと導いた後に求核剤と反応させることで対応するアルキル化体を得るという段階的な反応を、ルテニウム触媒を用いるこことで一段階で行うBorrowing Hydrogen法に関するものである．得られた研究成果は、この手法の新たな一面を切り拓く学術的に重要な知見であるとともに、それらがさらに高度化されることによって環境への付加を低減し、持続可能な社会を目指すグリーンケミストリー領域に貢献できるものであるといえる．
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