Indole-3-carbonitrile is used as a synthesis reagent for preparation of 4-substituted β-lactams, biologically active indoles, inhibitors of glycogen synthase kinase 3β (GSK-3), indole fragments as inosine monophosphate dehydrogenase (IMPDH) inhibitors and HIV-1 integrase inhibitors. It is also used as a reactant for intramolecular oxidative C-H coupling reactions with applications in medium-ring synthesis techniques and for preparation of tryptophan dioxygenase inhibitors pyridyl-ethenyl-indoles as potential anticancer immunomodulators.