Synthesis
Procedure for the synthesis of 1-(4-bromophenyl)-4-methylpiperazine (PZ959-2): 4-bromostyrene (PZ959-1, 22 g, 0.13 mol), 2-chloro-N-(2-chloroethyl)-N-methylethylamine (25.9 g, 0.17 mol), and triethylamine (353.5 mL, 0.38 mol) were dissolved in ethanol (300 mL). The reaction was refluxed for 80 hours. After completion of the reaction, the solvent was removed by distillation under reduced pressure, and the obtained residue was purified by high efficiency rapid column chromatography (DCM:EtOH=10:1) to obtain the target product PZ959-2 (20.3 g, 61% yield). LC-MS showed that [M+H]+ m/z=255.1.
