Gold(III) chloride catalyzed direct amination of arenes with azodicarboxylates was developed. The new catalytic system was active to a broad range of substrates, and the reaction was carried out under mild conditions. It represents the first catalytic system for the direct amination of electron-deficient arenes with azodicarboxylates to the best of our knowledge. This reaction provides an important approach for the synthesis of heterocyclic compounds in pharmaceutical and chemical industries.

Many functional groups and sterically hindered arenes are tolerated.