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Catalytic Synthesis and Functionalisation of a Universal Aryl-Sulfur Intermediate

通用芳基硫中间体的催化合成和官能化

基本信息

批准号：
EP/R002452/1
负责人：
Liam Thomas Ball
金额：
$ 12.84万
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：
2017
资助国家：
英国
起止时间：
2017 至无数据
项目状态：
已结题

来源：
https://gtr.ukri.org/projects?ref=EP%2FR002452%2F1
关键词：
Catalytic Synthesis Functionalisation Universal Aryl

项目摘要

The ability of chemists to produce specific organic molecules on demand, at low cost and on scales ranging from milligrams to multi-tonnes, has been central to many of the advances on which our quality of life now relies. The UK's fine chemical industry - particularly within the pharmaceutical and agrochemical sectors - continually faces new synthetic challenges, and is under increasing pressure to reduce the environmental impact of its operations. As such, there is constant demand for new synthetic methods that either provide more efficient access to known classes of compounds, or that open up previously unexplored areas of chemical space. Aryl-sulfur motifs feature in many societally-important molecules, including the sulfa drugs, anti-infectives that paved the way towards the modern healthcare we enjoy today. Formation of the C(aryl)-S linkage is often critical to the assembly of new aryl-sulfur-containing therapies, agrochemicals and materials, but - in many cases - is challenging to achieve in a mild and convenient fashion. Our research seeks to address these challenges through development of a robust and scalable method for C-S bond formation that avoids the malodorous, toxic and air sensitive intermediates that pervade organosulfur chemistry. The initial reaction products will then be exploited as a branching point from which to access all of the most important aryl-sulfur architectures, thereby demonstrating the ability of our methodology to deliver diverse, drug- and agrochemical-like scaffolds rapidly and under mild conditions. We will support this new methodology with detailed insight into how the system operates, and which variables are most critical for its successful application. Ultimately, this project will provide new tools to aid synthetic chemists in the preparation of a more diverse range of sulfur-containing molecules, in a more efficient manner. Given the contribution of pharmaceutical and agrochemical companies to the UK economy, this increased capability will be of benefit to UK plc. In addition, this project will provide a wealth of useful information and fundamental academic understanding that could guide the future development of new synthetic methods.

化学家按需生产特定有机分子的能力，以低成本和从毫克到数吨的规模生产，一直是我们现在生活质量所依赖的许多进步的核心。英国的精细化学工业--尤其是制药和农用化学品行业--不断面临新的合成挑战，并面临着越来越大的压力，要求减少其运营对环境的影响。因此，对新的合成方法的需求不断增加，这些方法要么提供更有效的途径来获取已知类别的化合物，要么开辟以前未探索的化学空间领域。芳基硫基序在许多具有重要社会意义的分子中具有特色，包括磺胺类药物，这些抗感染药物为我们今天享受的现代医疗保健铺平了道路。C(芳基)-S键的形成对组装新的芳基硫疗法、农用化学品和材料往往至关重要，但在许多情况下，以温和和方便的方式实现C(芳基)-S键具有挑战性。我们的研究试图通过开发一种健壮且可扩展的C-S键形成方法来应对这些挑战，该方法避免了有机硫化学中弥漫的恶臭、有毒和对空气敏感的中间体。然后，将利用初始反应产物作为分支点，从该分支点访问所有最重要的芳基硫结构，从而展示我们的方法能够在温和的条件下快速提供各种药物和农用化学品类支架。我们将通过对系统如何运行以及哪些变量对其成功应用最关键的详细了解来支持这一新方法。最终，该项目将提供新的工具，帮助合成化学家以更有效的方式制备范围更广的含硫分子。鉴于制药和农用化学品公司对英国经济的贡献，这种增强的能力将有利于英国公司。此外，该项目将提供丰富的有用信息和基本的学术理解，可以指导未来新的合成方法的发展。