Gold(I)-catalyzed one-pot reaction between 2-alkynylanilines and alkynols leading to the formation of C-3-substituted indoles: a case of formal carboamination of alkynes
A process involving gold(I)-catalyzed formal carboamination of alkynes for the synthesis of C-3-substituted indoles has been developed. The procedure utilizes easily accessible starting materials such as 2-alkynylanilines and alkynols. A series of C-3-functionalized indoles are accessible by using this one-pot strategy. Mechanistically, the reaction involves three catalytic cycles and each of them is essentially catalyzed by a single metal catalyst, that is, Ph3PAuOTf.
Gold(III)-catalyzed annulation of 2-alkynylanilines: A mild and efficient synthesis of indoles and 3-haloindoles
Gold(III)-catalyzed annulation of 2-alkynylanilines in EtOH or EtOH-water mixtures at room temperature gives indoles derivatives in good yields. One-flask protocol for the gold-catalyzed conversion of 2-alkynylanilines to 3-bromo and 3-iodoindoles is also reported.