Free radical strategies for bioactive molecule synthesis

生物活性分子合成的自由基策略

• 批准号: 10330824
• 负责人: Corey Stephenson
• 金额: $ 35.95万
• 依托单位: UNIVERSITY OF MICHIGAN AT ANN ARBOR
• 依托单位国家: 美国
• 财政年份: 2022
• 资助国家: 美国
• 起止时间: 2022-01-01 至 2026-12-31
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/10330824
• 关键词: Amines; Chemicals; Companions; Electrons; Free Radicals; Generations; Imines; Investigation; Methodology; Methods; Modernization; Molecular; Photochemistry; Reaction; Transition Elements; Vertebral column; Work; drug discovery; innovation; interest; novel; scaffold; small molecule therapeutics

Project Summary Through our expertise in photo- and electrochemical methodology, the proposed work will afford novel molecular scaffolds relevant and of interest to modern drug discovery. Through the utilization of single-electron methodologies described herein, we can generate previously inaccessible saturated carbocylces that have the potential to advance long standing challenges within drug discovery. Through companion photochemical methodologies, novel access to 1- aminonobornanes (1-aminoNBs), aminocyclopentanes, and bicyclo[3.1.1]heptan-1-amines has established a robust platform from which to explore new carbocyclic frameworks as diverse, sp3- rich chemical building blocks. Fundamental investigations of the imine photochemistry underlying these transformations will yield further applications beyond carbocycle formation. The intersection of our photochemical methods with transition metal catalyzed reactions provides a practical means of introducing desirable functionality (i.e. saturated motifs) onto ubiquitous aromatic backbones. Ultimately, we will utilize the power of single-electron transformations to gain access to new chemical space which we are confident will afford translational opportunities in drug discovery and beyond.

项目概要 通过我们在光和电化学方法方面的专业知识，拟议的工作将提供 与现代药物发现相关且令人感兴趣的新型分子支架。通过 利用本文描述的单电子方法，我们可以先前生成 难以接近的饱和碳环有可能推进长期存在的挑战 在药物发现中。通过配套的光化学方法，新颖地获得 1- 氨基降冰片烷 (1-aminoNBs)、氨基环戊烷和双环[3.1.1]庚烷-1-胺 建立了一个强大的平台，从中探索新的碳环框架，如多样化的、sp3- 丰富的化学构件。亚胺光化学的基础研究 这些转化将产生碳环形成之外的进一步应用。十字路口 我们的光化学方法与过渡金属催化反应提供了实用的 将所需功能（即饱和基序）引入到普遍存在的芳香族化合物上的方法 骨干。最终，我们将利用单电子变换的力量来获得访问权 我们相信新的化学领域将提供药物转化机会 发现及超越。