Synthesis of Indoles by Intermolecular Cyclization of Unfunctionalized Nitroarenes and Alkynes: OneStep Synthesis of the Skeleton of Fluvastatin

The addition of Ru3CO12, dimethyl carbonate, or both to the reaction mixture improves the selectivity of the palladiumphenanthrolinecatalyzed reaction of nitroarenes, arylalkynes, and CO to give 3arylindoles. When 4fluorophenylacetylene and nitrobenzene are used as substrates, the indole skeleton of Fluvastatin and other pharmaceutically active compounds is obtained in one step.© WileyVCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2009