1,2-Difluoro-4-nitrobenzene → (3R,5S)-1-(2-Fluoro-4-nitrophenyl)-3,5-dimethylpiperazine

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Reaction Steps

Crude 1-(2-fluoro-4-nitrophenyl)-cis-3,5-dimethylpiperazine (5.71 g, 103% recovery) is prepared according to the method described above for the synthesis of racemic-1-(2-fluoro-4-nitrophenyl)-trans-2,5-dimethylpiperazine by treatment of 1,2-difluoro-4-nitrobenzene (3.48 g, 21.8 mmol) with cis-2,6-dimethylpiperazine (2.50 g, 21.8 mmol). The crude product is used in the next step without chromatographic purification. LCMS-ESI (m/z): calcd for C12H16FN3O2, 253; [M+H]+ found, 254.

Provenance & Evidence