1-Methylpiperazine → 1-(4-Chloro-2-methoxyphenyl)-4-methylpiperazine

Participants

Reaction Conditions

Reaction Steps

Palladium II acetate (25.09 mg, 0.11 mmol) was added to 4-chloro-1-iodo-2-methoxybenzene (300 mg, 1.12 mmol), 1-methylpiperazine (0.124 ml, 1.12 mmol), sodium 2-methylpropan-2-olate (215 mg, 2.23 mmol) and 9,9-Dimethyl-4,5-bis(diphenylphosphino)xanthene (323 mg, 0.56 mmol) in toluene (4 ml) at room temperture under nitrogen. The resulting mixture was stirred at 100oC overnight. The reaction mixture was filtered through celite and then concentrated under reduced pressure. The crude product was then taken up in DCM and washed with water. The crude product was purified by chromatography in DCM:MeOH 0-->10% to afford 1-(4-chloro-2-methoxyphenyl)-4-methylpiperazine (171 mg, 63.6 %) as yellow oil. This was carried through to the next reaction immediately as it is a controlled substance.

Provenance & Evidence