Borate esters: Simple catalysts for the sustainable synthesis of complex amides

2017/09/01 by Marco T. Sabatini, Lee T. Boulton, Tom D. Sheppard · 1 citation
Biochemistry, Genetics and Molecular Biology · Chemistry · #Chemical Synthesis and Analysis #Chemical Synthesis and Reactions #Asymmetric Hydrogenation and Catalysis

paper · pdf · doi:10.1126/sciadv.1701028

openalex publication_date 2017/09/01 · openalex created_date 2025/10/10 · openalex updated_date 2026/07/19

Abstract

Chemical reactions for the formation of amide bonds are among the most commonly used transformations in organic chemistry, yet they are often highly inefficient. A novel protocol for amidation using a simple borate ester catalyst is reported. The process presents significant improvements over other catalytic amidation methods in terms of efficiency and safety, with an unprecedented substrate scope including functionalized heterocycles and even unprotected amino acids. The method was used to access a wide range of functionalized amide derivatives, including pharmaceutically relevant targets, important synthetic intermediates, a catalyst, and a natural product.

Citations

• Direct Synthesis of Amides from Alcohols and Amines with Liberation of H 2
• Analysis of the reactions used for the preparation of drug candidate molecules

Cited by

• Amide [wikipedia]