反应详情

To a solution of (R)-N-(3-((2,2-dimethyl-1,3-dioxolan-4-yl)methoxy)phenyl)-2-(2-(trifluoromethyl)phenyl)-1H-benzo[d]imidazole-4-carboxamide (134; 51.5 mg, 0.1 mmol) in 3 mL of THF was added 4 N HCl dropwise until observe color change, solution darkens, at which point an additional 1 mL of HCL is added and the solution is allowed to stir at room temperature for 18 h. The reaction mixture was diluted with MeOH and then concentrated under reduced pressure. The resulting yellowish suspension is purified by preparatory HPLC. The desired product (Compound 725) was obtained as a white solid (32.5 mg, 64%). MS (ESI) calcd for C24H20F3N3O4: 471.14; found: 472 [M+H].

1. additionat which point an additional 1 mL of HCL is added
2. concentrationconcentrated under reduced pressure
3. customThe resulting yellowish suspension is purified by preparatory HPLC