O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate → N-(4-Chloro-3-nitrobenzyl)-1-(trifluoromethyl)cyclopropanecarboxamide

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Reaction Steps

TBTU (0.44 g, 1.4 mmol) and TEA (0.43 mL, 3.1 mmol) are added to 1-trifluoromethyl-cyclopropanecarboxylic acid (0.19 g, 1.2 mmol) in THF (5 mL). After 10 min at rt 4-chloro-3-nitro-benzylamine (0.23 g, 1.2 mmol) is added to the reaction mixture and stirring is continued overnight. The mixture is concentrated, the crude is diluted with EtOAc and washed with sat.aq. NaHCO3-solution, water and brine. The organic layer is dried with Na2SO4 and concentrated.

Provenance & Evidence