1,2-Dimethylindole is a versatile building block for the preparation of carboxyindoles, 3-functionalized indoles, cyanoindoles, carbazoles, and trifluoromethylindoles. 1,2-Dimethylindole is also used as a reagent in Nazarov cyclizations, and in the preparation of plant growth promoters, tryptophan derivatives, and antihyperlipidemic agents.