9-oxo-9H-indeno(1,2-b)pyrazine-2,3-dicarbonitrile → 3-(4,4-difluoro-piperidin-1-yl)-9-oxo-9H-indeno[1,2-b]-pyrazine-2-carbonitrile

Participants

Reaction Steps

4,4-Difluoropiperidine hydrochloride (249 mg, 1.58 mmol) was dissolved in 1N NaOH (5 ml) and extracted with CH2Cl2 (2×5 ml). Organic phase was dried over Na2SO4, filtered and evaporated. The residue was dissolved in THF (2 ml) and this solution was added to a solution of 1 (185 mg, 0.79 mmol) in THF (2 ml); the mixture was stirred at room temperature for 48 hours. The solvent was evaporated, the crude solid washed with EtOH and dried under vacuum, affording 8 (245 mg, 95%) as yellow-brown solid.

Provenance & Evidence