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 通过我们在光和电化学方法学方面的专业知识，拟议的工作将负担得起 与现代药物发现相关并感兴趣的新型分子支架。通过 利用本文所述的单电子方法，我们可以预先生成 难以接近的饱和碳环，有可能推动长期存在的挑战 在药物发现中。通过伴随的光化学方法， 氨基硼烷（1-氨基NB）、氨基环戊烷和双环[3.1.1]庚烷-1-胺具有 建立了一个强大的平台，从探索新的碳环框架作为不同的，sp3- 丰富的化学成分亚胺光化学基础研究 这些转化将产生碳环形成以外的进一步应用。路口 我们的光化学方法与过渡金属催化反应提供了一个实用的 将期望的官能度（即饱和基序）引入普遍存在的芳族化合物上的方法 骨干最终，我们将利用单电子转换的力量， 我们有信心将提供药物转化的机会， 发现及超越。