反应详情

Methyl 2-(4-(pyrrolidin-1-ylmethyl)-2-(trifluoromethyl)phenyl)-1H-benzo[d]imidazole-4-carboxylate (544 mg) and LiOH (95 mg, 4 mmol) were dissolved in THF/H2O (1:1, 24 mL). The reaction was stirred overnight at room temperature, then heated at 50° C. overnight. The solvents were removed in vacuo. The residue was taken up in water and the pH was adjusted to 7-8 with 1N HCl. After allowing the mixture to stirred for 1 hour, the solids were collected by filtration to afford 2-(4-(pyrrolidin-1-ylmethyl)-2-(trifluoromethyl)phenyl)-1H-benzo[d]imidazole-4-carboxylic acid 159 as a pale solid (170 mg, 2-step yield: 40%). MS (ESI) calcd for C20H18F3N3O2: 389.14; found: 390 [M+H].

1. temperatureheated at 50° C. overnight
2. customThe solvents were removed in vacuo
3. stirringto stirred for 1 hour
4. filtrationthe solids were collected by filtration