One-pot cobalt-catalyzed ring-opening of diaziridines for bismuth-promoted Fischer indole synthesis

Abstract

Indoles are privileged scaffolds found in numerous natural products and pharmaceuticals, with the Fischer indole synthesis being the most widely employed synthetic methodology for their construction. In this study, we introduce a cobalt-catalyzed, one-pot strategy for bismuth-promoted Fischer indole synthesis via ring-opening of diaziridines. This approach avoids the use of toxic linear hydrazines and enables the synthesis of diverse indole derivatives under mild conditions using inexpensive reagents, offering a green and practical method for Fischer indole synthesis.