Gold(I)-Catalyzed Rearrangement of N-Aryl 2-Alkynylazetidines to Pyrrolo[1,2-a]indoles

Various N-aryl-2-alkynylazetidines were very efficiently converted to pyrrolo[1,2-a]indoles with gold catalysts, especially the 2-biphenyl-dicyclohexylphosphino-gold(I) hexafluoroantimonate, in dichloromethane at room temperature. Additionally, two formal syntheses of bioactive non-natural compounds, i.e. 7-methoxymitosene and an 5-HT2c receptor agonist, have been achieved.