C–N Bond formation by C–H functionalization via metal-catalyzed nitrene insertion

Simon Blakey and Nina Mace Weldy

Science of Synthesis,
2015, Section 12: C–H Activation, 2.9, p249-286


One of the core programs within the CCHF is the development of catalysts based upon earth-abundant elements that can be employed in C–H functionalization systems. A recent section of that program that has seen much success is the work being done by the Yu group in collaboration with the Dai group at Shanghai University.

This program has explored the use of copper-(II) salts for the directed activation of aromatic C–H bonds. Employing a sophisticated directing group strategy directed C–H activation and subsequent reaction with a series of nucleophiles has been found to be straightforward.

This report describes reaction with malonates, furnishing directly the protected heterocycles.

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