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

羧酸的新型直接胺将使用易于使用的，无毒的基于硅的试剂开发。预计该方案将适用于具有一级，环状和无环的继发胺和苯胺伴侣的多种脂肪型和芳香族羧酸。将选择基于硅的试剂，以便通过提供水溶性硅副产品的工作状态消灭它们，并允许以纯形式隔离酰胺产物，而无需进一步（色谱）纯化。预计该协议可以随着竞争过程质量强度而扩大规模。此外，将展示自动酰胺耦合 - 作为同质反应，然后是简单的自动化工作 - 将证明纯酰胺产物。关键词：酰胺，直接胺化，有机硅，自动酰胺合成