Automated Direct Amidation of Carboxylic Acids using Silicon-Based Reagents

点击翻译按钮获取中文摘要

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