Metal-Catalyzed C-H Borylation: Design of New Catalysts with New Selectivities

金属催化的 C-H 硼化：具有新选择性的新型催化剂的设计

• 批准号: 9354495
• 负责人: Milton Rudolph Smith
• 金额: $ 31.6万
• 依托单位: MICHIGAN STATE UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 2001
• 资助国家: 美国
• 起止时间: 2001-06-01 至 2020-07-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/9354495
• 关键词: Address; Chemicals; Chemistry; Communities; Data; Development; Drug Costs; Electrostatics; Environment; Family; Funding; Generations; Gifts; Grant; High temperature of physical object; Hydrogen Bonding; Hydrogenation; Inorganic Chemistry; Knowledge; Ligands; Metals; Methodology; Modification; Organic Synthesis; Pharmaceutical Preparations; Pharmacologic Substance; Preparation; Production; Reaction; Reporting; Research; Research Personnel; Route; Safety; Site; Source; Structure; Surface; System; United States Food and Drug Administration; Ursidae Family; analog; base; catalyst; design; drug discovery; enantiomer; experimental study; functional group; improved; interest; molecular recognition; preference; theories

Project Title: Metal-Catalyzed C-H Borylation: Design of New Catalysts with New Selectivities Abstract C–H borylation is a synthetic methodology where C–H bonds in an organic molecule react with B–H or B–B bonds forming a B–C bond. It has been widely applied in the functionalization of sp2 C–H bonds, but examples of sp and sp3 C–H bonds have been reported. The products of these reactions are important intermediates, which leverage the remarkable versatility of B–C bonds for installation of other functional groups under mild conditions. In this renewal application, we propose to advance our understanding of C–H borylations and to orthogonally develop the methodology such that it can offer solutions to synthetic problems faced by the biomedical community. Some of the specific aims build on chemistry that was developed in the previous funding cycle, while other specific aims are entirely new. Specifically, we propose to (1) the design of low- coordination number catalysts for directed sp2 and sp3 C–H borylation; (2) The design of ligand frameworks for meta and para C–H borylations; and (3) Hydrogenation of C–H borylated arenes and heterocycles to achieve formal sp3 C–H borylation. We will pursue these aims through a collaborative multi-investigator venture that bring the power of inorganic chemistry and organic synthesis to bear on the problem.

项目名称：金属催化的C-H硼化：具有新选择性的新型催化剂的设计 抽象的 C-H 硼化是一种合成方法，其中有机分子中的 C-H 键发生反应 与 B-H 或 B-B 键形成 B-C 键。它已被广泛应用在 sp2 C-H 键的官能化，但 sp 和 sp3 C-H 键的例子已 报道称。这些反应的产物是重要的中间体，它们利用 B-C 键具有卓越的多功能性，可在温和条件下安装其他官能团 状况。在此更新申请中，我们建议加深对 C-H 的理解 硼化并正交开发该方法，以便为合成提供解决方案 生物医学界面临的问题。 一些具体目标建立在先前资助中开发的化学基础上 周期，而其他具体目标则是全新的。具体来说，我们建议（1）低设计 用于定向 sp2 和 sp3 C-H 硼化的配位数催化剂； (2)配体的设计 间位和对位C-H硼化的框架； (3) C-H硼化芳烃的氢化和 杂环以实现正式的 sp3 C-H 硼化。我们将通过合作来实现这些目标 多研究者合资企业，将无机化学和有机合成的力量发挥作用 问题。