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 beta-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.

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

Serena Gabrielli;Roberto Ballini;Alessandro Palmieri
2019-01-01

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 beta-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.
2019
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Descrizione: Appl. Sci. 2019, 9, 5168
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11581/432625
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