Practical Syntheses of 5-Trifluoromethyl-1H-indoles

Abstract

Short and convenient syntheses of 5-trifluoromethyltryptamine and 5-trifluoromethyltryptophole have been realized via a regioselective, palladium catalyzed, coupling/annulation method involving functionalized alkynes and 2iodo-4-trifluoromethylaniline.A new and improved approach for the preparation of 5-trifluoromethyl-1H-indole is also described.