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The transition metal-catalysed direct functionalisation of C–H bonds is an increasingly viable alternative to the multi-step strategies traditionally adopted. The use of powerful and environmentally benign gold(I) and gold(III) catalysts in such transformations has highlighted their remarkable reactivity and led to a significant increase in their utilisation. This tutorial review provides an overview of gold-catalysed C–H functionalisation, looking at transformations which rely on the ability of gold to perform C–H activation, as well as those exploiting its potent π-acidity.

Graphical abstract: Gold-mediated C–H bond functionalisation

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