Abstract

A series of unsymmetrical arylureas was obtained by the one-pot method for reacting isatins with indoles incorporating primary amino moieties, a significant heterocyclic skeleton for diverse pharmaceutically active structures. The reaction proceeds through Cu(I)-catalyzed C2C3 bond of the ring-opening isatins and then expands the substrates in the optimum conditions. Furthermore, selected compounds 4b and 4k exhibit moderate to good anti-schistosomicidal activities.

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