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A General Intermolecular Benzylic C-H Amination Employing an Earth Abundant Metal

A General Intermolecular Benzylic C-H Amination Employing an Earth Abundant Metal
采用地球储量丰富的金属进行一般分子间苯甲基 C-H 胺化
批准号:
9192732
负责人:
Joseph Clark
金额:
$5.61万
依托单位国家:
美国
项目类别:
财政年份:
2016
资助国家:
美国
项目状态:
已结题
起止时间:
2016-09-16 至 2017-09-15

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英文摘要
Abstract Benzylic amines are commonly found in current drug candidates and FDA approved drugs. The direct installation of a nitrogen into a benzylic C–H bond, generating a benzylic amine, would be significant as aromatics are ubiquitous in bioactive molecules. Additionally, direct functionalization of a prevalent C–H bond eliminates the need for pre-installed functionalities, eliminating synthetic overhead and accelerating drug-diversification. A highly site- and chemoselective, inexpensive first row transition metal-catalyzed benzylic C–H amination is proposed for the rapid diversification of topologically complex and functionally diverse molecules. The method will be optimized and the catalyst reactivity will be evaluated in a variety of common organic scaffolds used in drug design. Selectivity trends will be elaborated in more complex commercially available pharmaceuticals. Once reactivity and selectivity trends are established, the method will be used to diversify complex drug scaffolds and natural products. Nitrogen is abundant in pharmaceuticals and natural products, making nitrogen tolerance under the reaction conditions necessary to significantly broaden the applications of the proposed method. Bioactive molecules containing a tertiary amine or pyridine will undergo complexation to the quaternary salt, to quell unwanted side reactions from detrimental nitrogen binding to reaction intermediates in the benzylic C–H amination reaction. If the proposed research is achieved, many new small molecule drug candidates will be accessible in only one step from existing small molecules, pharmaceuticals, and natural products. Such a method would broadly impact human health and the field of medicine as rapid and inexpensive access to new drug candidates will be possible with an earth-abundant, non-toxic, first-row transition metal catalyst.
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Molecular Rotational Resonance Spectroscopy Instrumentation for the Quantification and Characterization of Enantioisotopomers
  • 批准号:
    10797702
  • 项目类别:
  • 资助金额:
    $25.0万
  • 财政年份:
    2022
  • 负责人:
    Joseph Clark
  • 依托单位:
Highly Selective Cu-Catalyzed Reactions for Precision Deuteration and Alkyne Hydrofunctionalization
  • 批准号:
    10661088
  • 项目类别:
  • 资助金额:
    $37.02万
  • 财政年份:
    2022
  • 负责人:
    Joseph Clark
  • 依托单位:
Highly Selective Cu-Catalyzed Reactions for Precision Deuteration and Alkyne Hydrofunctionalization
  • 批准号:
    10501457
  • 项目类别:
  • 资助金额:
    $37.05万
  • 财政年份:
    2022
  • 负责人:
    Joseph Clark
  • 依托单位:
海外基金