Water → 5-(Benzoxazol-2-yl)-1-(tetrahydropyran-4-yl)-2-trichloromethylbenzimidazole

Participants

Reaction Steps

To a solution of 5-(benzoxazol-2-yl)-2-(tetrahydropyran-4-yl)aminoaniline (see Working Example 20-2) (150 mg, 0.485 mmol) in acetic acid (3 mL) was added methyl 2,2,2-trichloroacetimidate hydrochloride (94.1 mg, 0.533 mmol), and this was stirred at room temperature for 4 hours. After the reaction was complete, water was added, and the precipitated crystals were filtered, and after being washed with water were dried to yield the title compound (196 mg, 93% yield) as gray crystals.

Provenance & Evidence