Catalytic Synthesis and Functionalisation of a Universal Aryl-Sulfur Intermediate

化学家能够以低成本、从毫克到数吨的规模按需生产特定的有机分子，这是我们现在生活质量所依赖的许多进步的核心。英国的精细化工行业——尤其是制药和农用化工行业——不断面临着新的合成挑战，并面临着越来越大的压力，以减少其运营对环境的影响。正因为如此，人们对新的合成方法的需求不断增加，这些方法要么能更有效地获得已知种类的化合物，要么能开辟以前未开发的化学领域。芳基硫基在许多重要的社会分子中都具有重要的特征，包括磺胺药物、抗感染药物，这些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键的形成通常对新的芳基含硫疗法、农用化学品和材料的组装至关重要，但在许多情况下，以温和和方便的方式实现是具有挑战性的。我们的研究旨在通过开发一种强大且可扩展的C-S键形成方法来解决这些挑战，该方法避免了有机硫化学中普遍存在的恶臭，有毒和空气敏感的中间体。然后，初始反应产物将被利用为分支点，从中获取所有最重要的芳基硫结构，从而证明我们的方法能够在温和的条件下快速提供多种药物和农用化学品样支架。我们将通过详细了解系统如何运作以及哪些变量对其成功应用最为关键来支持这种新方法。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更多样化的含硫分子。鉴于制药和农用化学品公司对英国经济的贡献，这种增加的能力将有利于英国plc。此外，该项目将提供丰富的有用信息和基本的学术认识，可以指导新的合成方法的未来发展。

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.