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Updated: Sep 14, 2025

A Microwave-Assisted Direct Heteroarylation of Ketones Using Transition Metal Catalysis
Published on: February 16, 2020
Microwave-enhanced additive-free C-H amination of benzoxazoles catalysed by supported copper
Andrei Paraschiv1, Valentina Maruzzo1, Filippo Pettazzi1,2
1Department of Drug Science and Technology, University of Turin, Via Pietro Giuria 9, 10125 Turin, Italy.
Abstract:
The C2-amination of benzoxazole offers wide-ranging potential for substrate expansion and the functionalisation of bioactive compounds. This study presents a green and efficient C-H amination, catalysed by CuCl and CuCl2, in acetonitrile without acidic, basic or oxidant additives that is accelerated by microwave (MW) irradiation and is completed in 1.5-2 h. A solid Cu(I) catalyst supported on aminated silica made the process cost-effective and heterogeneous, thus simplifying work-up and minimising free copper in solution. The catalyst was found to be regeneratable and reusable for up to eight cycles. The optimised method facilitated the synthesis of various benzoxazole derivatives, demonstrating its versatility and practical applicability.
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