Methyl iodide → Methyl 4-[(5-chloro-2-{[4-(trifluoromethoxy)-phenyl]amino}-1H-benzimid-azol-1-yl)methyl]benzoate

関与物質

反応条件

反応手順

The title compound of Example 12, Step B (0.5 mmol, 145 mg) and 4-trifluoromethoxyphenyl isothiocyanate (0.5 mmol, 81 μL) were heated in DCM (1 mL) for 1 h, then allowed to stand at ambient temperature for 16 h. MeI (1.0 mmol, 62 μL), DIEA (1.0 mmol, 174 μL) and DMF (0.5 mL) were added and the solution was heated at 40° C. for 2 h. The reaction mixture was partitioned between EtOAc/brine and the organic phase was dried with Na2SO4 and concentrated in vacuo. Flash chromatography on silica eluting with 18% EtOAc in hexanes afforded the product as a beige solid. LC-MS (ESI, Method C): 3.85 min, m/z 476.1 (M+1).

情報源と証拠