反应详情

To a mixture of 2,3-diamino-5-morpholin-4-yl-benzoic acid methyl ester (73; 600 mg, 2.39 mmol) in EtOH (60 ml) was added sodium metabisulfite (373 mg, 1.96 mmol), H2O (2 ml) and 2-trifluoromethylbenzaldehyde (74; 990 mg, 5.69 mmol). The resulting reaction mixture was stirred under reflux for 3 h. It was then cooled to room temperature and concentrated under reduced pressure. Purification by chromatography afforded 6-morpholin-4-yl-2-(2-trifluoromethyl-phenyl)-1H-benzoimidazole-4-carboxylic acid methyl ester 75 (670 mg, 69.2%) as a yellow solid.

1. customThe resulting reaction mixture
2. temperatureunder reflux for 3 h
3. concentrationconcentrated under reduced pressure
4. customPurification by chromatography