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Boron: Beyond the Reagent

硼：超越试剂

基本信息

批准号：
EP/W007517/1
负责人：
Guy Lloyd-Jones
金额：
$ 638.74万
依托单位：
University of Edinburgh
依托单位国家：
英国
项目类别：
Research Grant
财政年份：
2023
资助国家：
英国
起止时间：
2023 至无数据
项目状态：
未结题

来源：
https://gtr.ukri.org/projects?ref=EP%2FW007517%2F1
关键词：
Boron Beyond Reagent

项目摘要

Boron is Earth-abundant, and present in its 'mineral form' in everyday objects, such as glass, detergents, flame-retardants, preservatives, and eye-drops. Boron is also found in 'organic form' in nature, including plant enzymes, and is an essential element in the diets of numerous living species, including ourselves. Inclusion of boron in man-made ('synthetic') organic compounds, often in place of one carbon atom in a chain of carbon atoms, can impart tremendous changes in the properties of a molecule. When these 'borylated' molecules are correctly 'tuned' by having the boron in the 'right place' together with other elements such as nitrogen and oxygen - their new properties can be harnessed to provide compounds with diverse applications. These range from 'smart' materials (e.g., in thin-film displays) through to safe, 'green' and economically advantageous reagents in the production of agrochemicals and pharmaceuticals, and, in another very recently emerging application, in the drug molecules themselves.Whilst there is no doubt that boron will continue to be a critical element in molecules and materials that are essential to our 21st century existence, the tools to install boron in, and to release boron from, such 'borylated' species have lagged behind the growth of the applications. The carbon-boron bond in borylated molecules can be fickle: on occasion it is fragile and keeping the assembly in place is the challenge. On other occasions it is too robust, resisting release of its organic molecule cargo, except under harsh conditions, where it is impossible to control the outcome. This research programme will tame these molecules to eliminate these gaps. We have assembled a world-class team that combines deep insight from experts in the design, preparation and analysis of borylated molecules, with end-user specialists who will help steer our investigations. Together, we will identify key opportunities and exploit the breakthroughs. With the market for borylated molecules expected to reach $1.7 Billion by 2025, this work will enable multi-scale applications across chemical, materials, and biological sciences, and provide a gateway to future technologies.Three divergent, expertise-related, and cross-fertilising research areas will be tackled, directly contributing to EPSRC themes of Healthcare Technologies, Manufacturing the Future, and the Productive and Resilient Nation.1. In developing borylated medicines, we will discover how to tune the instability of the carbon-boron bond to develop new boron-containing pharmaceuticals. These will resist carbon-boron bond cleavage until they have delivered the borylated pro-drug to the correct location, e.g., a specific organ, and then undergo cleavage to release the active drug in the right place at the right time. This will ensure the optimum concentration at the target, avoiding undesired side-effects, and requiring lower and safer doses.2. In chemical manufacturing, we will design borylated reagents with switchable (arm/disarm) reactivity. These robust species will be easily prepared, stored and transported, on large scales if required. Yet, when ready for use, on addition of small amount of a 'release' component, the borylated reagent will rapidly switch to its reactive armed form, delivering the organic molecule payload, primed for the manufacturing process. This will reduce waste, increase safety, and allow new processes to be developed.3. Smart boron-containing materials, used in devices such as OLEDs, need to be able to deliver efficient function and stability over long device lifetimes. This necessitates very high stability in the carbon-boron bond for these applications. We will design and test new borylated building blocks that are immune to 'release' of the organic fragment, under a wide range of operating conditions. This will broaden the conditions that the devices will tolerate and increase their application scope.

硼在地球上含量丰富，以“矿物形式”存在于日常用品中，如玻璃、洗涤剂、阻燃剂、防腐剂和眼药水。硼也以“有机形式”存在于自然界中，包括植物酶，并且是许多生物物种（包括我们自己）饮食中的重要元素。在人造（“合成”）有机化合物中包含硼，通常代替碳原子链中的一个碳原子，可以使分子的性质发生巨大变化。当这些“硼化”分子通过将硼与氮和氧等其他元素一起放在“正确的位置”而正确地“调整”时，它们的新特性可以被利用来提供具有不同应用的化合物。这些范围从“智能”材料（例如，薄膜显示器中）到农用化学品和药物生产中安全、“绿色”和经济上有利的试剂，以及在另一个最近新兴的应用中，药物分子本身。毫无疑问，硼将继续成为分子和材料中的关键元素，这些分子和材料对我们21世纪的存在至关重要，是安装硼和释放硼的工具，这种“硼基化”物质已经落后于应用的增长。硼化分子中的碳硼键可能是变化无常的：有时它是脆弱的，保持组装到位是一个挑战。在其他情况下，它过于强大，抵抗其有机分子货物的释放，除非在苛刻的条件下，在那里不可能控制结果。这项研究计划将驯服这些分子，以消除这些差距。我们组建了一个世界级的团队，将硼化分子设计、制备和分析专家的深刻见解与最终用户专家结合起来，他们将帮助指导我们的研究。我们将共同确定关键机遇并利用这些突破。预计到2025年，硼化分子的市场将达到17亿美元，这项工作将使化学，材料和生物科学的多尺度应用成为可能，并为未来技术提供一个门户。三个不同的，专业相关的和交叉的研究领域将得到解决，直接有助于EPSRC的医疗保健技术，制造未来，和富有生产力和韧性的国家。在开发硼化药物的过程中，我们将发现如何调整碳-硼键的不稳定性，以开发新的含硼药物。这些将抵抗碳-硼键断裂，直到它们将硼基化前药递送到正确的位置，例如，特定的器官，然后进行裂解，在正确的时间在正确的位置释放活性药物。这将确保目标的最佳浓度，避免不希望的副作用，并需要更低和更安全的剂量。2.在化学制造中，我们将设计具有可切换（arm/disarm）反应性的硼化试剂。如果需要，这些健壮的物种将易于大规模制备、储存和运输。然而，当准备使用时，在添加少量的“释放”组分时，硼基化试剂将迅速转变为其反应性武装形式，递送有机分子有效载荷，为制造过程做好准备。这将减少浪费，提高安全性，并允许开发新的工艺。3.用于OLED等器件的智能含硼材料需要能够在较长的器件寿命内提供有效的功能和稳定性。对于这些应用，这需要碳-硼键的非常高的稳定性。我们将设计和测试新的硼基化结构单元，这些单元在广泛的操作条件下对有机片段的“释放”免疫。这将拓宽设备所能容忍的条件并扩大其应用范围。