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Synthetic investigation of lead compounds possessing antitutor and antiviral activities

Synthetic investigation of lead compounds possessing antitutor and antiviral activities
具有抗肿瘤和抗病毒活性的先导化合物的合成研究
批准号:
13672226
负责人:
ISHIKURA Minoru
金额:
$0.77万
依托单位国家:
日本
项目类别:
Grant-in-Aid for Scientific Research (C)
财政年份:
2001
资助国家:
日本
项目状态:
已结题
起止时间:
2001 至 2003

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中文摘要
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英文摘要
In this project, the development of synthetic appliobilities of indolylborate and 2-azabicyclo[2.2.1]hept-5-en-3-one (ABH) as a valuable synthon of indole alkaloids and carbocyclic nucleoside derivatives was investigated.1. Synthetic study of strychnos and uleine alkaloids through tandem cyclization-cross-coupling reaction with indolylborateConversion of 2-vinylindole derivatives, readily available from the tandem cyclization-cross-coupling reaction of indolylborate wirh (2-bromoprop-2-enyl)pentyl-3-nylamine in a one-pot manner, to strychnos indole alkaloid was investigated.2. Novel approach to the construction of carbazole derivatives through intramolecular alkyl migration reaction.Investigation of intramolecular alkyl migration reaction in indolylborate possessing an electrophilic center was carried out, which provided novel methodology for the construction of carbazole derivatives.3. Synthesis of novel carbocyclic nucleoside derivatives by the use of 2-azabicyclo[2.2.1]hept-5-en-3-one (ABH)Cycloaddition reaction toward the double bond of ABH proceeded stereoselectively to provide the exo-adduct. This reaction was used for the construction of novel carbocyclic nucleoside fused with cyclopropane, aziridine and oxirane rings at the 2',3' position of carbocyclic nucleoside derivatives.
期刊论文(24)
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会议论文
M.Ishikura: "Cycloaddition Reaction of 2-Allenylindoles with Diethyl Acetylenedicarboxylate"J.Heterocyclic Chem.. 38(3). 675-678 (2001)
M.Ishikura:“2-烯基吲哚与乙炔二甲酸二乙酯的环加成反应”J.杂环化​​学.. 38(3)。
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通讯作者:
Minoru Ishikura: "Synthetic studies of novel carbocyclic nucleosides based on bicyclic amide (ABH)"Trends in Heterocyclic Chemistry. (In press).
Minoru Ishikura:“基于双环酰胺(ABH)的新型碳环核苷的合成研究”杂环化学趋势。
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Minoru Ishikura: "Ruthenium-catalyzed ring-opening cross-metathesis reaction of 2-azabicyclo-[2.2.1]hept-5-en-3-one"Heterocycles. 57(2). 241-244 (2002)
Minoru Ishikura:“钌催化的 2-azabicyclo-[2.2.1]hept-5-en-3-one”杂环的开环交叉复分解反应。
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石倉 稔: "身近な素材に活路を探して"有機合成化学協会誌. 59. 422-423 (2001)
Minoru Ishikura:“在熟悉的材料中寻找出路”合成有机化学学会杂志 59. 422-423 (2001)。
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24
    Development of novel synthetic method and its use for synthesis of natural products
    • 批准号:
      22590010
    • 项目类别:
      Grant-in-Aid for Scientific Research (C)
    • 资助金额:
      $3.0万
    • 财政年份:
      2010
    • 负责人:
      ISHIKURA Minoru
    • 依托单位:
    Development of multi-functionalized synthon for the synthesis of bioactive natural products
    • 批准号:
      18590011
    • 项目类别:
      Grant-in-Aid for Scientific Research (C)
    • 资助金额:
      $2.57万
    • 财政年份:
      2006
    • 负责人:
      ISHIKURA Minoru
    • 依托单位:
    Novel synthesis of indole derivatives based on the palladium catalyzed cross-coupling reaction with indolylborates as a key reaction
    • 批准号:
      09672151
    • 项目类别:
      Grant-in-Aid for Scientific Research (C)
    • 资助金额:
      $1.98万
    • 财政年份:
      1997
    • 负责人:
      ISHIKURA Minoru
    • 依托单位:
    海外基金