Automated Direct Amidation of Carboxylic Acids using Silicon-Based Reagents

使用硅基试剂自动直接酰胺化羧酸

• 批准号: 2279368
• 金额: --
• 依托单位: Imperial College London
• 依托单位国家: 英国
• 项目类别: Studentship
• 财政年份: 2019
• 资助国家: 英国
• 起止时间: 2019 至 无数据
• 项目状态: 已结题
• 来源: https://gtr.ukri.org/projects?ref=studentship-2279368
• 关键词: Automated; Direct; Amidation; Carboxylic; Acids

Novel direct amidations of carboxylic acids will be developed using readily available, non-toxic, siliconbased reagents. The protocols are expected to be applicable to a wide range of aliphatic and aromatic carboxylic acids with primary, cyclic, and acyclic secondary amines and aniline partners. The siliconbased reagents will be selected such that they are annihilated by the work-up regime providing watersoluble silicon byproducts and allowing for the isolation of the amide products in pure form without the need for further (chromatographic) purification. The protocols are expected to be amenable to scale-up with competitive process mass intensities. Moreover, automated amide couplings - as homogenous reactions, followed by simple automated work-ups - to provide pure amides product will be demonstrated. Key words: Amides, Direct Amidation, Organosilicon, Automated Amide Synthesis

将使用现成的、无毒的硅基试剂开发新型的羧酸直接酰胺化方法。该方案预计适用于各种具有伯胺、环状和无环仲胺以及苯胺伙伴的脂肪族和芳香族羧酸。选择硅基试剂，使得它们通过后处理方案消除，提供水溶性硅副产物，并允许以纯形式分离酰胺产物，而不需要进一步（色谱）纯化。这些协议预计能够以具有竞争力的工艺质量强度进行扩展。此外，还将演示自动化酰胺偶联——作为均相反应，然后进行简单的自动化后处理——以提供纯酰胺产品。关键词: 酰胺, 直接酰胺化, 有机硅, 酰胺自动化合成