| Project/Area Number |
26460012
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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 | Health Sciences University of Hokkaido |
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Principal Investigator |
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| Co-Investigator(Kenkyū-buntansha) |
山田 康司 北海道医療大学, 薬学部, 准教授 (80272962)
阿部 匠 北海道医療大学, 薬学部, 助教 (80453273)
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| Project Period (FY) |
2014-04-01 – 2017-03-31
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| Project Status |
Completed (Fiscal Year 2016)
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| Budget Amount *help |
¥5,070,000 (Direct Cost: ¥3,900,000、Indirect Cost: ¥1,170,000)
Fiscal Year 2016: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2015: ¥1,040,000 (Direct Cost: ¥800,000、Indirect Cost: ¥240,000)
Fiscal Year 2014: ¥2,990,000 (Direct Cost: ¥2,300,000、Indirect Cost: ¥690,000)
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| Keywords | インドリルボレート / インドールアルカロイド / クロスカップリング / 電子環状反応 / ピリドカルバゾールアルカロイド / インドロキナゾリンアルカロイド / 酸化的カップリング / 銅触媒 / エリプチシン / オリバシン / アルカロイド合成 / 抗腫瘍活性 / ピリドカルバゾール / 酸化的二量化 |
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| Outline of Final Research Achievements |
Cross-coupling reaction of indolylborate was used for concise total syntheses of pyrido[4,3-b]carbazole alkaloids. Unprecedented use of copper(I) triflate toluene complex for electrocyclization of hexatriene intermediate successfully improved the construction of pyridocarbazoles. Evaluation of synthetic alkaloids against HCT-116 and HL-60 cell lines was carried out. Concise syntheses of indoloquinazoline alkaloids were developed. Oxidative dimerization of indole-3-carbaldehyde provided tryptanthrin in a one-pot. Further transformation of tryptanthrin through Baeyer-Villiger oxidation provided cephalanthrin A. Oxidative coupling between indole-3-carboxylate and isatoic anhydride provided phaitanthrin E.
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