1-Hydroxybenzotriazole → HCID 178451022, compound

Participants

Reaction Steps

To 2.2 g of (S)-4-Amino-5-oxo-5-[4-(3-trifluoromethyl-phenyl)-piperazin-1-yl]-pentanoic acid tert-butyl ester in 30 ml of DMF, 892 mg of HOBT, 1.08 g of 5-Hydroxy-1-phenyl-1H-pyrazole-3-carboxylic acid 1.12 g EDC Hydrochlorid and 1.90 ml DIPEA was added. After 3 h at RT the mixture was diluted with ethyl acetate and washed with saturated sodium hydrogen carbonate solution. Drying of the organic layer over sodium sulfate and evaporation under reduced pressure afforded a brownish powder that was purified by chromatography over silica gel eluting with ethyl acetate/heptane 1:1 to 100% ethyl acetate to give 2.7 g of the desired product. Yield: 2.7 g MS (ES+): m/e=416.

Provenance & Evidence