Compounds which have the 2-aminobutene-1,4-dione skeleton can be found in many drugs, bio-active compounds and industrial products. [1][2][3][4] Additionally, these 2-aminobutene-1,4-diones can also serve as useful tools for constructing heterocyclic compounds in organic synthesis containing, for example, pyrrole, hydrazine, furan and cyclopentenone moieties. [5][6][7][8] As a consequence, various methods for their preparation have been reported previously, for example, conjugate addition of diaroylacetylenes or sulfur ylides to aryl azides, 9,10 using α,β-unsaturated γ-dicarbonyl or acetophenones with amines, 11,12 reaction of pyridinium bromides and primary aromatic amines with phenylglyoxal or ethyl glyoxalate 13 and other ways. 14,15 Recently, Wu and co-workers developed an efficient Cu-catalysed tandem reaction to synthesise 2-aminobutene-1,4-diones in good yields, but a long reaction time is needed. 16 Here, we develop a simple and convenient method by a multi-component reaction process to access 2-aminobutene-1,4-diones rapidly.Gold catalysis offers new ways for the efficient construction of complex molecules and has attracted much attention because of the catalyst's soft and carbophilic Lewis acidity in recent years. [17][18][19][20] Furthermore, Au-catalysed reactions generally proceed under very mild conditions with small amounts of catalyst. In 2013 we reported a new gold-catalysed three-component coupling (TCC) reaction of phenylglyoxal derivatives, secondary amines and alkynes under an N 2 atmosphere. 21 This method afforded the efficient synthesis of three-substituted furans in good yields and provided a powerful approach for the preparation of furan derivatives. Meanwhile, Hashmi and co-workers demonstrated a reaction to form 1,2-dicarbonyl-3-enes with the same substrates under AuCl catalysis. 22 Secondary amine mediated alkyne-toallene isomerisation and hydrolysis of the enamine substructure during the work-up delivered the formal hydroacylation products. During our previous work, we found traces of 2-aminobutene-1,4diones formed under aerobic conditions with gold catalysts, so we decided to study this product. Now we wish to introduce a goldcatalysed one-pot, three-component synthesis of 2-aminobutene-1,4-dione derivatives utilising the same substrates (phenylglyoxal derivatives, secondary amine and alkynes) in the presence of H 2 O (Scheme 1).