Ti-catalyzed cascading hydroaminoalkylation as a route to complex functionalized amines

Ti 催化级联氢氨基烷基化作为制备复杂官能化胺的途径

• 批准号: 10750347
• 负责人: Zoua Pa Vang
• 金额: $ 6.87万
• 依托单位: UNIVERSITY OF MINNESOTA
• 依托单位国家: 美国
• 财政年份: 2023
• 资助国家: 美国
• 起止时间: 2023-08-18 至 2025-08-17
• 项目状态: 未结题
• 来源: https://reporter.nih.gov/project-details/10750347
• 关键词: Alkenes; Amines; Aniline; Biological; Catalysis; Complex; Development; Electrons; Kinetics; Ligands; Medicine; Methodology; Methods; Modern Medicine; Muscarinic Antagonists; Nitrogen; Organic Chemistry; Pharmacologic Substance; Play; Preparation; Productivity; Reaction; Reporting; Role; Route; Structure; Time; Titanium; Transition Elements; catalyst; density; diene; drug candidate; improved; innovation; method development; phosphoramidate; scaffold; theories; tool

Project Summary/Abstract Central to the development of medicine is organic chemistry and catalysis as it has permitted the discovery of new reactions and methods for the synthesis of key pharmaceutical components that will play a critical role in continuing the advancement of modern medicine. With the high presence of nitrogen atoms in drug candidates due to their high biological activity, it is crucial to develop new and innovative methods to synthesize and functionalize nitrogen-containing molecules. Recently, reactive titanium intermediates were used to explore second insertions of unsaturated species yielding useful nitrogen heterocycles. This proposal will focus on developing an efficient and one-step atom- economical Ti-catalyzed multicomponent, cascading hydroaminoalkylation reaction to produce β- cycloalkyl amines from dienes and amine/aniline substrates. This methodology has potential to be a valuable synthetic tool because β-cycloalkyl amines products are scaffolds present in pharmaceutical compounds such as cyclopentamine and propylhexedrine and in M3 muscarinic antagonist. Additionally, this method will provide a fundamental understanding of this new reaction class that can be extended into other cascading reactions to rapidly build molecule complexity.

项目总结/文摘