反应详情

A mixture of 2-[4-(2,6-difluoro-benzoylamino)-1H-pyrazol-3-yl]-1H-benzimidazole-4-carboxylic acid (50 mg, 0.13 mmol), N-methylpiperazine (20 μl, 0.18 mmol), EDC (30 mg, 0.15 mmol) and HOBt (22 mg, 0.15 mmol) in DMF (5 ml) was stirred at ambient temperature for 18 h. The mixture was reduced in vacuo and the residue purified by flash column chromatography [SiO2, CH2Cl2/MeOH (95:5, 90:10)] to give 2,6-difluoro-N-{3-[4-(4-methyl-piperazine-1-carbonyl)-1H-benzimidazol-2-yl]-1H-pyrazol-4-yl}-benzamide (14 mg) as a cream solid. (LC/MS: Rt 2.21, [M+H]+ 466).

1. customthe residue purified by flash column chromatography [SiO2, CH2Cl2/MeOH (95:5, 90:10)]