Cesium carbonate → 6-bromo-1-cyclobutyl-5-fluoro-1H-indole-3-carbonitrile

Participants

Reaction Conditions

Reaction Steps

To 6-bromo-5-fluoro-1H-indole-3-carbonitrile (49.2 g, 206 mmol) [prepared as in Example 6, Step B] was added cesium carbonate (133 g, 408 mmol), DMF (200 mL), and cyclobutylbromide (30 mL, 311 mmol). This mixture was stirred at 90° C. for three days, cooled to room temperature and poured into ice water. The precipitate was collected, washed with water and dried to give 6-bromo-1-cyclobutyl-5-fluoro-1H-indole-3-carbonitrile as a light grey solid (55 g, 90%).

Provenance & Evidence