Catalytic Methods for Rapid Aromatic Derivatization

快速芳香衍生化的催化方法

• 批准号: 9154613
• 负责人: David A Nicewicz
• 金额: $ 27.68万
• 依托单位: UNIV OF NORTH CAROLINA CHAPEL HILL
• 依托单位国家: 美国
• 财政年份: 2016
• 资助国家: 美国
• 起止时间: 2016-09-20 至 2020-07-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/9154613
• 关键词: Air; Alcohols; Aromatic Compounds; Boronic Acids; Catalysis; Chemicals; Complex; Coupling; Dental crowns; Development; Dyes; Evaluation; Fluorides; Goals; Lead; Libraries; Metabolic; Methods; Molecular; Nitrogen; Oxidants; Oxygen; Pharmaceutical Chemistry; Pharmacologic Substance; Play; Protocols documentation; Reaction; Reagent; Reporting; Research; Research Personnel; Research Proposals; Role; Source; Structure; System; Therapeutic; Transition Elements; Visible Radiation; aryl halide; base; catalyst; chemical reaction; design; drug candidate; flexibility; functional group; halogenation; lipophilicity; novel; novel strategies; programs; rapid technique; scaffold; small molecule libraries; small molecule therapeutics; tool

Project Summary The objective of this research proposal is to develop new catalytic protocols for the direct C–H functionalization of aromatic compounds. Aromatic compounds are central motifs in the vast majority of therapeutics and simple methods for their further elaboration are always in demand. The goal of this research program is to generate new synthetic tools for biomedical researchers to be able to derivatize lead aromatic-containing therapeutics in order to assemble libraries of drug candidates for further evaluation. This proposal describes the use of organic dyes as catalysts to enable over a dozen new chemical transformations. The value of the proposed synthetic methods is the ability to utilize aromatics that are not pre-oxidized, allowing for greater flexibility in the types of aromatic structures that can be employed. We predict that this research program will enhance the synthetic capabilities of medicinal chemists to explore greater chemical space in the development of small molecule therapeutics.

项目摘要 本研究方案的目标是开发直接C-H的新的催化方案 芳香族化合物的官能化。芳香化合物是浩瀚宇宙中的中心主题 大多数治疗方法和进一步阐述它们的简单方法一直是需要的。 这项研究计划的目标是为生物医学研究人员产生新的合成工具 能够衍生含铅的芳香族治疗药物，以便组装 供进一步评估的候选药物。该提案将有机染料的使用描述为 催化剂使十几种新的化学变化成为可能。建议的价值 合成方法是利用未预氧化的芳烃的能力，允许更大的 可采用的芳香族结构类型的灵活性。我们预测这项研究 计划将增强药物化学家的综合能力，探索更大的 化学空间在小分子治疗学发展中的作用。