反应详情

A solution of 2-[4-(2,6-difluoro-benzoylamino)-1H-pyrazol-3-yl]-1H-benzimidazole-4-carboxylic acid methyl ester (220 mg, 0.55 mmol) in THF/water (1:1, 10 ml) was treated with lithium hydroxide hydrate (70 mg, 1.66 mmol) and the mixture stirred at ambient temperature for 18 h. The volatiles were removed in vacuo, the mixture acidified to pH5 by the addition of 2M aqueous hydrochloric acid and the solid formed collected by filtration, washed with water then dried under vacuum to give 2-[4-(2,6-difluoro-benzoylamino)-1H-pyrazol-3-yl]-1H-benzimidazole-4-carboxylic acid (165 mg) as a brown solid. (LC/MS: Rt 3.28, [M+H]+ 384).

1. customThe volatiles were removed in vacuo
2. additionthe mixture acidified to pH5 by the addition of 2M aqueous hydrochloric acid
3. customthe solid formed
4. filtrationcollected by filtration
5. washwashed with water
6. customthen dried under vacuum