| Project/Area Number |
16K18857
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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
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| Research Institution | Microbial Chemistry Research Foundation |
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Principal Investigator |
SAITO Akira 公益財団法人微生物化学研究会, 微生物化学研究所, 研究員 (10772866)
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| Project Period (FY) |
2016-04-01 – 2018-03-31
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| Project Status |
Completed (Fiscal Year 2017)
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| Budget Amount *help |
¥3,640,000 (Direct Cost: ¥2,800,000、Indirect Cost: ¥840,000)
Fiscal Year 2017: ¥1,430,000 (Direct Cost: ¥1,100,000、Indirect Cost: ¥330,000)
Fiscal Year 2016: ¥2,210,000 (Direct Cost: ¥1,700,000、Indirect Cost: ¥510,000)
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| Keywords | アリル化 / 不斉合成 / アミド / 含フッ素化合物 / 協奏機能触媒 / 協奏機能型触媒 / 触媒的不斉合成 / アリル化反応 / エノラート / パラジウム触媒 |
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| Outline of Final Research Achievements |
Catalytic asymmetric a-allylation of a-CF3 amide was developed by the design of novel synergistic catalyst system, which nucleophilic 7-azaindoline amide enolate by chiral Cu/hard Bronsted base and electrophilic pi-allyl Pd species can be independently generated and coexist. The novel methodology of enantioselective C-C bond formation at a-position of amides, whose alpha-deprotonation is regarded difficult in general, could be successfully presented. The chiral alpha-CF3-gamma,delta-unsaturated amides obtained by the reaction can be transformed to corresponding CF3-substituted cyclopropane derivatives, which are promising building block for drug candidate in the field of medicinal chemistry.
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