1H-1,2,4-Triazole → HCID 66606898, compound

Participants

Reaction Steps

To a solution of 1,2,4-triazole (0.042 g, 0.61 mmol) in DMF at 0° C. was added sodium hydride (60% in mineral oil; 0.044 g, 1.1 mmol), and the mixture was stirred for 30 minutes. (2′-{[(2-Chloro-acetyl)-ethyl-amino]-methyl}-6-methoxy-4′-trifluoromethyl-biphenyl-3-yl)-acetic acid ethyl ester (0.55 mmol) in DMF was added, followed by tetrabutylammonium iodide (0.1022 g, 0.06 mmol), and the reaction was warmed to room temperature and stirred for 1.5 hours. The mixture was diluted with EtOAc and H2O, and the aqueous layer was extracted twice with EtOAc. The combined organic layers were washed three times with H2O, and then dried and concentrated, and the residue was purified by silica gel chromatography (40-90% EtOAc in hexanes) to give the title compound.

Provenance & Evidence