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A Radical Amination Approach to Aliphatic Amines

脂肪胺的自由基胺化方法

基本信息

批准号：
EP/V050176/1
负责人：
James Cuthbertson
金额：
$ 51.83万
依托单位：
University of Nottingham
依托单位国家：
英国
项目类别：
Research Grant
财政年份：
2022
资助国家：
英国
起止时间：
2022 至无数据
项目状态：
未结题

来源：
https://gtr.ukri.org/projects?ref=EP%2FV050176%2F1
关键词：
Radical Amination Approach Aliphatic Amines

项目摘要

The synthesis of novel molecules underpins diverse academic fields and industries vital to the UK economy. Amines, in particular beta-functionalised amines, are prevalent in molecules essential to everyday life ranging from pharmaceuticals such as Pregabalin and Januvia, to agrochemicals, such as Fenpropimorph, which are used to safeguard global food supplies. Despite their importance, current methods for amine synthesis are often reliant upon toxic reagents (alkyl halides), unstable precursors (aldehydes), or stoichiometric organometallic reagents. There is therefore significant demand for mild and efficient approaches to amine-containing molecules.Recently, the use of nitrogen centred radicals in the synthesis of amines has been reported, providing a mild alternative to conventional synthetic methods. However, despite their potential, radical aminofunctionalisation reactions have not been comprehensively investigated, and the true potential of this approach remains to be realised.In this project we will investigate the use of nitrogen centred radicals, reductively generated in a single electron transfer process, in the synthesis of synthetically valuable beta-aryl amines. The addition of a nitrogen centred radical to an alkene, will generate a versatile alkyl radical intermediate that can be functionalised through a diverse range of pathways. The proposed aminoarylation processes will enable rapid access to a range of amine building blocks. This modular approach to amine synthesis, in which two new bonds (C-N and C-C) are constructed in a single step, will open up previously unexplored areas of chemical space, facilitating the development of new pharmaceuticals, agrochemicals, and materials.We will apply the chemistry to the synthesis of bioactive natural products and pharmaceutical analogues to highlight the potential applications of the research in academia and industry.

新分子的合成支撑着对英国经济至关重要的各种学术领域和行业。胺，尤其是β功能化胺，普遍存在于日常生活必不可少的分子中，从普瑞巴林（Pregabalin）和Januvia等药物，到苯丙咪唑（fenpropromorph）等用于保障全球粮食供应的农用化学品。尽管它们很重要，但目前的胺合成方法往往依赖于有毒试剂（烷基卤化物）、不稳定前体（醛）或化学计量有机金属试剂。因此，对温和和有效的含胺分子的方法有很大的需求。最近，氮中心自由基在胺合成中的应用已被报道，为传统的合成方法提供了一种温和的替代方法。然而，尽管它们具有潜力，但自由基氨基功能化反应尚未得到全面研究，这种方法的真正潜力仍有待实现。在这个项目中，我们将研究在单电子转移过程中还原生成的氮中心自由基在合成有合成价值的-芳基胺中的使用。在烯烃上加入以氮为中心的自由基，会生成一个多功能的烷基自由基中间体，它可以通过多种途径被功能化。提出的氨基化过程将使快速获得一系列胺构建块。这种模块化的胺合成方法，在一个步骤中构建两个新的键（C-N和C-C），将开辟以前未开发的化学空间领域，促进新药物，农用化学品和材料的开发。我们将把化学应用于生物活性天然产物和药物类似物的合成，以突出该研究在学术界和工业界的潜在应用。