Development of Divergent Cascade Annulation Reactions for the Synthesis of Malagashanine and Akuamilline Alkaloids

合成 Malagashanine 和 Akuamilline 生物碱的发散级联环化反应的发展

基本信息

  • 批准号:
    1362502
  • 负责人:
  • 金额:
    $ 37.5万
  • 依托单位:
  • 依托单位国家:
    美国
  • 项目类别:
    Continuing Grant
  • 财政年份:
    2014
  • 资助国家:
    美国
  • 起止时间:
    2014-07-15 至 2018-06-30
  • 项目状态:
    已结题

项目摘要

In this project funded by the Chemical Synthesis program of the Chemistry Division, Professor Simon Blakey of Emory University is developing new reactions that will allow the synthesis of two novel families of bioactive molecules. The development of new methodology, and the demonstrated ability to access multiple classes of natural products that were previously inaccessible, will set the stage for further understanding of the basic biological activities of these molecules. This fundamental research will pave the way for the development of the therapeutic properties implied in ethnomedicine studies that serve as the inspiration for this project, furthering our understanding of malarial resistance to common drug treatments, and potentially providing a road map to new clinical entities.An outreach program is exploring the narrative of the malagashanine story through a collaboration between the sciences and the arts. The combination illustrates the interplay between disciplines to inform a public audience on cutting edge science and ethical questions arising from the discoveries. Professor Blakey will deliver public lectures at the Atlanta Botanical Garden, and ultimately to broad audiences as part of the Atlanta Science Festival.The unusual structures of these molecules render them difficult to synthesize with existing methods. To date, no members of either family have been synthesized. To meet the challenge posed by these molecules, and provide significant quantities for further biological study, new reactions and new catalysts to control these reactions are under development. Specifically, a series of stereospecific iminium ion initiated cascade reactions, and novel chiral disulfonamide catalysts will be developed and studied, providing solutions to the synthetic problem posed by the malagashanine and akuamma alkaloids. These studies are expected to culminate in the syntheses of representative molecules from both families.
在这个由化学系化学合成项目资助的项目中,埃默里大学的Simon Blakey教授正在开发新的反应,这将允许合成两种新型生物活性分子家族。新方法的开发,以及获得以前无法获得的多种天然产物的能力,将为进一步了解这些分子的基本生物活性奠定基础。这项基础研究将为民族医学研究中隐含的治疗特性的发展铺平道路,这些研究是该项目的灵感来源,进一步加深了我们对疟疾对常见药物治疗的耐药性的理解,并可能为新的临床实体提供路线图。一个外展计划正在通过科学和艺术之间的合作探索马拉加沙宁故事的叙述。这种结合说明了学科之间的相互作用,以向公众介绍这些发现所产生的前沿科学和伦理问题。布莱基教授将在亚特兰大植物园发表公开演讲,并最终作为亚特兰大科学节的一部分向广大观众发表演讲。这些分子的不寻常结构使其难以用现有方法合成。迄今为止,这两个家族的成员都没有被合成。为了应对这些分子带来的挑战,并为进一步的生物学研究提供大量的物质,正在开发新的反应和控制这些反应的新催化剂。具体而言,一系列的立体定向亚胺离子引发的级联反应,和新的手性二磺酰胺催化剂将被开发和研究,提供解决的合成问题所带来的malagashanine和akuamma生物碱。这些研究预计最终在两个家庭的代表性分子的合成。

项目成果

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Simon Blakey其他文献

Prediction of growth of jet fuel autoxidative deposits at inner surface of a replicated jet engine burner feed arm
  • DOI:
    10.1016/j.fuel.2017.10.006
  • 发表时间:
    2018-02-15
  • 期刊:
  • 影响因子:
  • 作者:
    Ehsan Alborzi;Simon Blakey;Hassan Ghadbeigi;Christophe Pinna
  • 通讯作者:
    Christophe Pinna

Simon Blakey的其他文献

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{{ truncateString('Simon Blakey', 18)}}的其他基金

NewJet Network+
新捷网络
  • 批准号:
    EP/S032118/1
  • 财政年份:
    2019
  • 资助金额:
    $ 37.5万
  • 项目类别:
    Research Grant
CAREER: Metallonitrene/Alkyne Metathesis and Beyond: Transition Metal Catalyzed Oxidative Amination For Organic Synthesis
职业:金属氮/炔复分解及其他:过渡金属催化的有机合成氧化胺化
  • 批准号:
    0847258
  • 财政年份:
    2009
  • 资助金额:
    $ 37.5万
  • 项目类别:
    Continuing Grant

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