Microwave-Enhanced, Additive-Free C-H Amination of Benzoxazoles Catalysed by supported Copper

• DOI: 10.3762/bxiv.2025.14.v1
• Publication Date: 2025-03-04T15:43:36Z
• Authors: Andrei Paraschiv; Valentina Maruzzo; Filippo Pettazzi; Stefano Magliocco; Paolo Inaudi; Daria Brambilla; Gloria Berlier; Giancarlo Cravotto; Katia Martina

The C2 amination of benzoxazole offers wide-ranging potential for substrate expansion and the functionalisation bioactive compounds. This study presents a green efficient C-H amination, catalysed by CuCl CuCl₂, in acetonitrile without acidic, basic or oxidant additives that is accelerated Microwave (MW) irradiation completed 1.5–2 h. A solid Cu(I) catalyst supported on aminated silica made process cost-effective heterogeneous, thus simplifying work-up minimising free copper solution. was found to be regenerable reusable up eight cycles. optimised method facilitated synthesis various derivatives, demonstrating its versatility practical applicability.