课题基金 / 基金详情

ACYCLIC STEREOSELECTION IN NATURAL PRODUCT SYNTHESIS

ACYCLIC STEREOSELECTION IN NATURAL PRODUCT SYNTHESIS
天然产物合成中的无环立体选择
批准号：
2842627
负责人：
CLAYTON H HEATHCOCK
金额：
$29.54万
依托单位：
UNIVERSITY OF CALIFORNIA BERKELEY
依托单位国家：
美国
项目类别：
财政年份：
1978
资助国家：
美国
项目状态：
已结题
起止时间：
1978-09-01 至 2002-02-28
来源：
https://reporter.nih.gov/project-details/2842627
关键词：
antifungal antibiotics antineoplastic antibiotics biological products chemical models computer simulation conformation drug design /synthesis /production macrolide antibiotics molecular dynamics nuclear magnetic resonance spectroscopy stereochemistry

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英文摘要
DESCRIPTION: (Verbatim from the Applicant's Abstract) Plans are presented to complete a total synthesis of spongistatin 1 (altohrytin A), a potent antifungal and cytotoxic agent of marine origin. Because of its potent bioactivity, spongistatin is a promising drug candidate, but it would be virtually impossible to obtain sufficient quantities from natural sources. The goal of this project is to develop a synthesis that is sufficiently practical that it can be used to prepare approximately five grams of the material, which would be sufficient for a phase I clinical trial. Plans are also presented to complete a total synthesis of the 14- membered macrolide antibiotic lankamycin. Although an efficient and convenient synthetic route to the aglycone seco-acid has been developed in previous work, the macrolactonization reaction has not yet been achieved. In fact, this common transformation is often a limiting step in macrolide total synthesis. The goal of the coming project period is to apply modern methods of computer modelling, NMR conformational analysis, and synthesis to identify a suitable substrate for the macrolactonization.
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TOTAL SYNTHESIS OF POLYCYCLIC NATURAL PRODUCTS
  • 批准号：
    2183631
  • 项目类别：
  • 资助金额：
    $18.63万
  • 财政年份：
    1992
  • 负责人：
    CLAYTON H HEATHCOCK
  • 依托单位：
    UNIVERSITY OF CALIFORNIA BERKELEY
TOTAL SYNTHESIS OF POLYCYCLIC NATURAL PRODUCTS
  • 批准号：
    3305528
  • 项目类别：
  • 资助金额：
    $16.13万
  • 财政年份：
    1992
  • 负责人：
    CLAYTON H HEATHCOCK
  • 依托单位：
    UNIVERSITY OF CALIFORNIA BERKELEY
TOTAL SYNTHESIS OF POLYCYCLIC NATURAL PRODUCTS
  • 批准号：
    6636030
  • 项目类别：
  • 资助金额：
    $25.34万
  • 财政年份：
    1992
  • 负责人：
    CLAYTON H HEATHCOCK
  • 依托单位：
    UNIVERSITY OF CALIFORNIA BERKELEY
TOTAL SYNTHESIS OF POLYCYCLIC NATURAL PRODUCTS
  • 批准号：
    2444788
  • 项目类别：
  • 资助金额：
    $19.79万
  • 财政年份：
    1992
  • 负责人：
    CLAYTON H HEATHCOCK
  • 依托单位：
    UNIVERSITY OF CALIFORNIA BERKELEY