Mechanochemistry, solvent-free and scale-up: Application toward coupling of acids and amines to amides

Abstract

Amide is one of the most important molecules in chemistry and biology. Seeking a green and efficient synthesis method for obtaining amide compounds has always been the main research direction. In this paper, it was proposed to use acid and amine as raw materials to synthesize amides under green, fast and mechanochemical conditions, the purification of the product only requires water washing and filtration. This method avoids using a large amount of organic solvents and pollutant generation in the reaction process, the yield of amide is up to 96%. Even when scaled up to 50 mmol for the preparation of moclobemide, the yield of moclobemide is higher than that of traditional methods, and the purification is simple. This green, fast and simple protocol is one of the ideal alternatives to obtain amide.

Keywords

• Amide
• Mechanochemistry
• Coupling
• Acid