Automated Direct Amidation of Carboxylic Acids using Silicon-Based Reagents

新的羧酸直接酰胺化将被开发，使用现成的，无毒的，硅基试剂。该方案预计将适用于广泛的脂肪族和芳香族羧酸与伯胺、环胺和无环仲胺和苯胺伙伴。硅基试剂的选择将使它们被提供水溶性硅副产物的预处理机制所湮灭，并允许以纯形式分离酰胺产物，而无需进一步（色谱）纯化。预计该协议将适应竞争过程质量强度的扩大。此外，自动化酰胺偶联-作为均相反应，随后是简单的自动化工作-将演示提供纯酰胺产品。关键词：酰胺，直接酰胺化，有机硅，自动化酰胺合成

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