Direct C-H Amidation of 1,3-Azoles: Light-Mediated, Photosensitiser-Free vs. Thermal

Abstract

We have developed one thermal and one light-mediated method for direct Minisci-type C-H amidation of 1,3-azoles, which are applicable to the four most important 1,3-azoles in medicinal chemistry: thiazoles, benzothiazoles, benzimidazoles, and for the first time, imidazoles. The new visible light-mediated approach can be rendered photosensitiser/photocatalyst-free and likely proceeds via an electron donor-acceptor (EDA) complex, the first direct Minisci-type amidation to do so.