Catalyst-Free Photooxidative N-Acylation of Azoles with Aldehydes

Chemistry. 2025 Jan 1:e202404225. doi: 10.1002/chem.202404225. Online ahead of print.

Abstract

A catalyst-free photochemical N-acylation of azoles with aldehydes has been developed using inexpensive BrCCl3 as the oxidant. This transition-metal- and photocatalyst-free amidation proceeded efficiently with a wide variety of substrates to give the corresponding N-acylazoles, including for the late modification of pharmaceutically active molecules, and on a gram-scale.

Keywords: Aldehydes; BrCCl3; N-acylazoles; oxidative amidation; photocatalyst-free.