New array strategies using C-H borylation chemistry

使用 C-H 硼化化学的新阵列策略

• 批准号: EP/F068158/1
• 负责人: Patrick Steel
• 金额: $ 64.25万
• 依托单位: Durham University
• 依托单位国家: 英国
• 项目类别: Research Grant
• 财政年份: 2008
• 资助国家: 英国
• 起止时间: 2008 至 无数据
• 项目状态: 已结题
• 来源: https://gtr.ukri.org/projects?ref=EP%2FF068158%2F1
• 关键词: New; array; strategies; using; borylation

In order to evaluate and optimise (small) molecules for a particular function, e.g. as a drug molecule, it is necessary to prepare a range of analogues that differ in structure. This is known as an array and the efficient synthesis of such arrays requires reactions that can be used on multiple samples simultaneously. The variety of chemical reactions currently used in array preparation is limited and the research in this project is designed to address this need based on chemistry of the boronic acid functional group. In particular we will develop new array synthetic strategies using direct catalytic C-H borylation chemistry. This requires evaluation of new substrate classes and an optimisation of the catalysts to give better selectivity and reactivity. This will provide sets of new boronic acids from unfunctionalised aromatic and heteroaromatic precursors. In addition, the boronic acids are themselves used in many synthetic transformations and we will explore using the arrays of boronic acids as starting points for a further generation of array synthesis.

为了评估和优化具有特定功能的（小）分子，例如作为药物分子，有必要制备一系列结构不同的类似物。这就是所谓的阵列，这种阵列的有效合成需要可以同时在多个样品上使用的反应。目前用于阵列制备的化学反应种类有限，本项目的研究旨在解决基于硼酸官能团化学的这一需求。特别是我们将开发新的阵列合成策略使用直接催化C-H硼化化学。这需要评估新的底物类别和优化催化剂，以提供更好的选择性和反应性。这将从未官能化的芳香和杂芳香前体中提供一系列新的硼酸。此外，硼酸本身在许多合成转化中使用，我们将探索使用硼酸阵列作为进一步一代阵列合成的起点。

项目成果

"One-pot" tandem C-H borylation/1,4-conjugate addition/reduction sequence.

• DOI: 10.1021/ol102518v
• 发表时间: 2010-11
• 期刊: Organic letters
• 影响因子: 5.2
• 作者: Hazmi Tajuddin;Lena Shukla;A. Maxwell;T. Marder;P. Steel