Water → Tert-butyl 4-[4-(methoxycarbonyl)-2-nitrophenyl]piperazine-1-carboxylate

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Reaction Steps

To a solution of methyl 4-fluoro-3-nitrobenzoate (2.50 g, 12.6 mmol) in tetrahydrofuran (75 mL), tert-butyl piperazine-1-carboxylate (4.67 g, 25.2 mmol) and potassium carbonate (4.34 g, 25.2 mmol) were added sequentially under ice-cold conditions, and the mixture was stirred at room temperature for 1 hour. The reaction solution was added water under ice-cold conditions, and extracted with ethyl acetate. The organic layer was washed with brine, dried over anhydrous sodium sulfate, and concentrated in vacuo. The obtained residue was purified by silica-gel column chromatography (ethyl acetate). The title compound (4.83 g (yield 100%)) was obtained as a yellow crystal.

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