Water → 1-(2-Methoxyphenyl)piperazine

Participants

Reaction Conditions

Reaction Steps

To a solution of 1-bromo-2-methoxybenzene (0.623 mL, 5.0 mmol) and piperazine (1722.8 mg, 20.0 mmol) in diglyme (5 mL) was added t-BuONa. The resulting mixture was stirred at rt for a few minutes before the addition of dichlorobis(tri-β-tolyphosphine)palladium (235.8 mg, 0.3 mmol). The resulting mixture was then stirred at 170° C. under microwave irradiation for 30 min. Water was added and the mixture was extracted with EtOAc. The combined organic layers were dried, concentrated, and purified by ISCO to give 1-(2-methoxyphenyl)piperazine (intermediate 65) (758 mg, 79%) as an off-white solid. HPLC: 95%, RT 2.641 min. MS (ESI) m/z 193.10 [M+H]+.

Provenance & Evidence