cis-4-(2-Fluoro-4-nitrophenyl)-1,2,6-trimethylpiperazine → 3-Fluoro-4-(cis-3,4,5-trimethyl-piperazin-1-yl)-phenylamine

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Reaction Steps

Using the method described above for the synthesis of racemic-4-(trans-2,4,5-Trimethyl-piperazin-1-yl)-phenylamine, treatment of cis-4-(2-fluoro-4-nitrophenyl)-1,2,6-trimethylpiperazine (1.39 g, 5.20 mmol) with H2 and 10% Pd/C (120 mg) provided crude 3-fluoro-4-(cis-3,4,5-trimethyl-piperazin-1-yl)-phenylamine (1.04 g, 84% recovery, 96% purity as determined by LC/MS analysis @ UV 254 nm detection,). The crude product is used in the next step without further purification. LCMS-ESI (m/z): calcd for C13H20FN3, 237; [M+H]+ found, 238.

Provenance & Evidence