| Project/Area Number |
25460026
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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 | Toho University |
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Principal Investigator |
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| Project Period (FY) |
2013-04-01 – 2016-03-31
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| Project Status |
Completed (Fiscal Year 2015)
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| Budget Amount *help |
¥5,200,000 (Direct Cost: ¥4,000,000、Indirect Cost: ¥1,200,000)
Fiscal Year 2015: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2014: ¥910,000 (Direct Cost: ¥700,000、Indirect Cost: ¥210,000)
Fiscal Year 2013: ¥2,990,000 (Direct Cost: ¥2,300,000、Indirect Cost: ¥690,000)
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| Keywords | パラジウム / ベンジル化 / ベンジルアルコール / 水 / 環境負荷低減型 / グリーンケミストリー / スルホンアミド / 炭素－水素結合活性化 |
|---|
| Outline of Final Research Achievements |
A unique strategy for benzylation and C-H activation by the (η3-benzyl)palladium(II) system from a water-soluble palladium(0)/sodium diphenylphosphinobenzene-3-sulfonate (TPPMS) catalyst and benzyl alcohol in water is developed. Notably, water may activate the sp3 C-O bond, then stabilize the Pd(II) cation species by hydration, which can then undergo innovative direct transformation reactions. N-Benzylation/benzylic C-H activation cascade is devised as a novel and efficient synthetic route for N-(1,2-diphenylethyl)anilines or 3-phenyl-3,4-dihydro-(2H)-1,2,4-benzothiadiazine-1,1-dioxides. A direct catalytic substitution of benzylic alcohols, which affords the desired products along with water as the sole co-product, is an efficient and environmentally benign method.
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