Title:Continuous Flow Synthesis of Amides in Bio-Derived Solvent GVL
Volume: 22
Issue: 3
Author(s): Xu-Yang Mu, Rui Zhu, Li-Jie Yu and Wen-Long Wang*
Affiliation:
- School of Life Sciences and Health Engineering, Jiangnan University, Jiangsu, 214122, China
Keywords:
γ-Valerolactone, amide condensation, continuous flow chemistry, bio-derived solvent, 2-bromo-1-ethylpyridinium tetrafluoroborate, green solvents.
Abstract: The amide group is one of the most ubiquitous chemical motifs in the pharmaceutical
field. An efficient continuous flow synthesis of amides was achieved by coupling acids with amines
using 2-bromo-1-ethylpyridinium tetrafluoroborate (BEP) in the bio-derived “green” solvent γ-
valerolactone (GVL). The reaction proceeded under mild reaction conditions (ambient temperature,
1 min) with simple filtration without the need for extensive purification, allowing a safe and ondemand
generation of procainamide and VH032-Boc with a productivity of 0.44 g day,-1 and 0.99 g
day-1. The finding of our work aligned with green chemistry principles should result in its adoption
by the chemistry community.
