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.

项目摘要 通过我们在照片和电化学方法论方面的专业知识，拟议的工作将负担 与现代药物发现相关的新型分子支架。通过 利用本文所述的单电子方法，我们可以先前生成 难以访问的饱和碳纤维有可能提高长期挑战 在药物发现中。通过伴侣光化学方法，新的访问1- Aminonobornanes（1-氨基盐），氨基细胞和bicyclo [3.1.1] Heptan-1-胺具有 建立了一个强大的平台，从该平台探索新的碳环框架，如SP3- 丰富的化学构建块。亚胺光化学的基本调查 这些转换将产生超出碳循环形成以外的进一步应用。十字路口 通过过渡金属催化反应的光化学方法提供了一种实用的 将所需功能（即饱和基序）引入无处不在的芳族的手段 骨干。最终，我们将利用单电子转换的力量来获得访问 到我们有信心的新化学空间，可以为药物提供转化机会 发现及以后。