β-Nitroacrylates: New Key Precursors of Indole-2-Carboxylates via Fischer Indole Synthesis

Abstract

Indole 2-carboxylates are very important scaffolds that are widely investigated for their activities and are used as key intermediates of biologically active molecules. Herein, we report a new procedure for the preparation of this class of derivatives, via Fischer indole synthesis, starting from β-nitroacrylates and arylhydrazines. The protocol permits the production of the title targets in satisfactory overall yields, avoids any wasteful aqueous work-up, and has with evident advantages from a sustainability point of view.