New routes to the activation of organic molecules

有机分子活化的新途径

• 批准号: 1949401
• 金额: --
• 依托单位: University of Nottingham
• 依托单位国家: 英国
• 项目类别: Studentship
• 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=studentship-1949401
• 关键词: New; routes; activation; organic; molecules

Phosphorus compounds are widely used in Chemistry. They are often used in agriculture, materials, medicines and for the activation of organic molecules (such as carboxylic acids). Often the synthesis of these useful compounds uses, toxic, hazardous and/or energy intensive processes and reagents, examples include: PCl5, PCl3, POCl3, phosgene, Cl2 etc. In order to move to a more sustainable future, chemists must develop alternative reagents and methods that are, safer, more stable and therefore easier to use.The most common transformation used by the pharmaceutical industry is amide bond synthesis, representing 1 in 7 reactions performed. As a result, a wide range of coupling (activating) reagents have been developed to couple carboxylic acids with amine nucleophiles. Phosphorus (V) activating reagents are popular (e.g. T3P, DPPA, BOP etc.) as these reagents produce water soluble by-products that can easily be removed by aqueous washing. However, the synthesis of these compounds requires the use of PCl5. Other issues are also presented with the use of phosphorous activating reagents, such as toxicity, water sensitivity and the production of high molecular weight by-products (this applies to BOP), which leads to poor atom economy. This project aims to address these problems by using other non-toxic, low molecular weight phosphorus reagents as coupling partners, which can be sourced without the need to use chlorine gas and/or other toxic and moisture sensitive reagents. Proposed solution and methodologyWithheld due to confidentiality reasons.

磷化合物在化学中有着广泛的应用。它们通常用于农业，材料，医药和有机分子（如羧酸）的活化。这些有用化合物的合成通常使用有毒、危险和/或能量密集的方法和试剂，实例包括：PCl 5，PCl 3，POCl 3，光气，Cl 2等。为了走向更可持续的未来，化学家必须开发更安全，更稳定，因此更容易使用的替代试剂和方法。制药行业最常见的转化是酰胺键合成，代表进行的7个反应中的1个。因此，已经开发了各种各样的偶联（活化）试剂以使羧酸与胺亲核试剂偶联。磷（V）活化剂是流行的（例如T3 P、DPPA、BOP等）。因为这些试剂产生水溶性副产物，其可容易地通过水洗涤除去。然而，这些化合物的合成需要使用PCl 5。使用磷活化剂还存在其它问题，例如毒性、水敏感性和产生高分子量副产物（这适用于BOP），这导致原子经济性差。该项目旨在通过使用其他无毒、低分子量磷试剂作为偶联伙伴来解决这些问题，这些试剂可以在不需要使用氯气和/或其他有毒和潮湿敏感试剂的情况下获得。提议的解决办法和方法由于保密原因而搁置。