2-Chloro-4-nitrobenzoic acid → N-tert-Butyl-3-((4-(2-chloro-4-nitrobenzoyl)piperazin-1-yl)methyl)benzamide

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Reaction Steps

1-Propanephosphonic acid cyclic anhydride (3.16 g, 92 mmol, 2.95 mL) was added dropwise to a solution of 2-chloro-4-nitrobenzoic acid (1 g, 4.9 mmol), N-tert-butyl-3-(piperazin-1-ylmethyl)benzamide (1.4169 g, 5.1 mmol) and triethylamine (1.4979 g, 14.7 mmol, 2 mL) in dichloromethane. The reaction was concentrated under reduced pressure and the residue was taken up in ethyl acetate, washed with water, sodium hydrogen carbonate and brine. The organic phase was concentrated under vacuum to afford the title compound (2.06 g).

Provenance & Evidence