Triethylamine → N-tert-butyl-3-((4-(4-nitro-2(trifluoromethyl)benzoyl)piperazin-1-yl)methyl)benzamide

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Reaction Steps

To a stirred solution of N-tert-butyl-3-(piperazin-1-ylmethyl)benzamide (3.99 mmol, 1.1 g), 4-nitro-2-(trifluoromethyl)benzoic acid (3.83 mmol. 0.9 g) and triethylamine (28.7 mmol, 4 mL. 2.90 g) in dichloromethane (20 mL) was added 1-propanephosphonic acid cyclic anhydride (8.94 mmol, 5.3 mL, 5.69 g, 50% solution in ethyl acetate) dropwise. After 1 hour stirring, ethyl acetate was added and the organic mixture was washed with saturated sodium hydrogen carbonate (×2), water (×2) and finally brine. The organic mixture was dried with sodium sulfate and concentrated under vacuum to give the intermediate N-tert-butyl-3-((4-(4-nitro-2(trifluoromethyl)benzoyl)piperazin-1-yl)methyl)benzamide.

Provenance & Evidence