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中文摘要
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描述(由申请人提供):光化学反应对药物发现很有吸引力,因为它们可以合成其他方法无法合成的不寻常的、紧张的分子框架。然而,制药公司很少利用光化学合成,因为需要专门的光化学设备是不切实际的障碍,因为很少有方法来控制光化学反应的立体化学存在。因此,光化学合成产生的分子结构基本上没有作为可能的候选药物进行检查。我们的实验室开创了一种光化学合成的新方法,该方法使用方便,容易获得的可见光(例如,家用灯泡,环境阳光),以便首次使药物化学家可以进行光化学合成。这项建议有两个平行的目标:目标1。光化学反应立体化学控制策略的发展。目标2。可见光光化学活化新机制的研究进展。这些方法功能强大,健壮,并且易于在大型工业相关规模上执行。因此,本提案中描述的研究将对学术化学社区和更广泛的药物化学家社区产生重大影响,他们需要新的分子构建方法来发现下一代救命药物。
英文摘要
DESCRIPTION (provided by applicant): Photochemical reactions are attractive for drug discovery because they enable the synthesis of unusual, strained molecular frameworks that cannot be synthesized by other methods. Nevertheless, pharmaceutical companies rarely take advantage of photochemical synthesis because the need for specialized photochemical equipment is an impractical impediment and because very few methods to control the stereochemistry of photochemical reactions exist. Therefore, the structures of the molecules that are produced by photochemical synthesis have essentially not been examined as possible drug candidates. Our laboratory has pioneered a new approach to photochemical synthesis that uses convenient, readily available sources of visible light (e.g., household lightbulbs, ambient sunlight) in order to make photochemical synthesis accessible to medicinal chemists for the first time. This Proposal has two parallel objectives: Aim 1. The development of strategies to control the stereochemistry of photochemical reactions. Aim 2. The development of a novel mechanism of photochemical activation with visible light. These methods are powerful, robust, and simple to perform on large, industrially relevant scales. Thus, the research described in this proposal will significantly impact both the academic chemistry community and the broader community of medicinal chemists who require new methods of molecule construction to discover the next generation of life-saving drugs.
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SYNTHETIC PHOTOCHEMISTRY
  • 批准号:
    10543475
  • 项目类别:
  • 资助金额:
    $57.64万
  • 财政年份:
    2022
  • 负责人:
    TEHSHIK P YOON
  • 依托单位:
SYNTHETIC PHOTOCHEMISTRY
  • 批准号:
    10330629
  • 项目类别:
  • 资助金额:
    $22.27万
  • 财政年份:
    2022
  • 负责人:
    TEHSHIK P YOON
  • 依托单位:
SYNTHETIC PHOTOCHEMISTRY
  • 批准号:
    10798418
  • 项目类别:
  • 资助金额:
    $5.14万
  • 财政年份:
    2022
  • 负责人:
    TEHSHIK P YOON
  • 依托单位:
Visible Light Photocatalysis
  • 批准号:
    10380452
  • 项目类别:
  • 资助金额:
    $3.76万
  • 财政年份:
    2020
  • 负责人:
    TEHSHIK P YOON
  • 依托单位:
海外基金