| Project/Area Number |
25460022
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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 | Showa Pharmaceutical University |
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Principal Investigator |
TAMURA Osamu 昭和薬科大学, 薬学部, 教授 (30257141)
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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 |
¥4,680,000 (Direct Cost: ¥3,600,000、Indirect Cost: ¥1,080,000)
Fiscal Year 2015: ¥1,300,000 (Direct Cost: ¥1,000,000、Indirect Cost: ¥300,000)
Fiscal Year 2014: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
Fiscal Year 2013: ¥1,690,000 (Direct Cost: ¥1,300,000、Indirect Cost: ¥390,000)
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| Keywords | O-シリルオキシム / N-アシルニトロン / チイルラジカル / アルキニルO-シリルオキシム / ラジカル環化 / N-ボラノニトロン / 付加環化 / ω-アルケニルオキシム / N-アシル化 / S-アルコキシカルボニル-２－メルカプトピリジン / N-選択的 / 保護基導入剤 / オキシム / ニトロン / アシル化 / 分子内付加環化 / 分子内付加環化反応 |
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| Outline of Final Research Achievements |
(1) Omega-alkenyl oximes, on heating with Boc2O, underwent N-acylation leading to N-Boc nitrones, which caused intramolecular cycloaddition. Acylating reagent that is more adequate for the present cycloaddition was also explored. (2) A C-amide-substituted O-silylated oxime, on treatment with BF3-OEt2, in situ generated boracyclic nitrone-type intermediate, which underwent cycloaddition with alkenes to give 3,5-cis-isoxazolidines as the major products. (3) ω-Alkynyl O-tert-butyldiphenyl- silyloximes, on treatment with odorless 4-tert-butylbenzenethiol in the presence of AIBN in boiling benzene, underwent addition of thiyl radical followed by radical cyclization of the corresponding vinyl radicals onto the O-silyloxime moieties to give cyclic O-silylhydroxylamines in good yields.
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