New Directions in Palladium/Norbornene Cooperative - Instrument Supplement

钯/降冰片烯合作的新方向 - 仪器补充

• 批准号: 10382974
• 负责人: Guangbin Dong
• 金额: $ 10.25万
• 依托单位: UNIVERSITY OF CHICAGO
• 依托单位国家: 美国
• 财政年份: 2018
• 资助国家: 美国
• 起止时间: 2018-06-01 至 2022-04-30
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/10382974
• 关键词: Acylation; Address; Amination; Biological; Catalysis; Complex; Epoxy Compounds; Funding; Ligands; Palladium; Positioning Attribute; Research; Site; functional group; instrument; scaffold

Abstract: We are engaged in the systematic efforts to exploit new, efficient, and broadly useful palladium/norbornene (Pd/NBE) catalysis for site-specific arene mono- and di-functionalization. Our objective in the proposed funding period includes: first to develop new classes of vicinal di- functionalization, e.g. ortho amination, acylation, thiolation and annulation with epoxides by discovering new classes of electrophiles; and second to address the “ortho effect” limitation (requirement of a pre-existing ortho substituent) by developing new NBE-type ligands. The proposed research is expected to vastly expand the toolbox for arene functionalization via site- specifically installing functional groups at unactivated positions, which in turn would streamline synthesis of complex biologically important molecules containing multi-substituted aromatic scaffolds.

摘要：我们正在系统地努力开发新的、高效的和广泛有用的 钯/降冰片烯 (Pd/NBE) 催化位点特异性芳烃单官能化和双官能化。 我们在拟议资助期内的目标包括：首先开发新类别的邻里迪 官能化，例如邻位胺化、酰化、硫醇化和与环氧化物的环化 发现新类别的亲电子试剂；其次解决“邻位效应”的限制 （需要预先存在的邻位取代基）通过开发新的 NBE 型配体。 拟议的研究预计将通过位点极大地扩展芳烃功能化的工具箱 在未激活的位置专门安装功能组，从而简化 含有多取代芳族化合物的复杂生物学重要分子的合成 脚手架。