Indole → 6-cyano-4-methyl-1H-indole-3-carboxylic acid

Participants

Reaction Conditions

Reaction Steps

A mixture of compound 1 (10.0 g, 50.0 mmol), CuCN (9.0 g, 100 mmol) and NMP (60 mL) was heated at 180° C. for 6 h. The mixture was cooled to room temperature, diluted with EA, then washed with H2O, brine, dried and concentrated. The residue was purified by silica gel chromatography (petroleum ether/EtOAc=10/1) to give the desired product (3.30 g, 22.8 mmol, 45.6%) as a yellow solid.

Provenance & Evidence