反应详情

1-(2-Chlorobenzyl)-6-chlorocarbonyl-2-cyclopropylbenzimidazole hydrochloride (140 mg) is added at room temperature to a solution which has been prepared by adding morpholine (298 mg, a 30% methanol solution) to methylene chloride (10 ml) . After the reaction mixture is stirred for one hour at the same temperature, it is washed with water, dried and concentrated under reduced pressure. The residue is recrystallized using ether and thus, 1-(2-chlorobenzyl)-2-cyclopropyl-6-morpholino-carbonylbenzimidazole (20 mg) is obtained. (Colorless crystal). 1H-NMR (CDCl3,): 1.04-1.12 (2H, m), 1.25-1.32 (2H, m), 1.82-1.96 (1H, m), 3.68 (8H, bs), 5.56 (2H, s), 6.55 (1H, dd, J=1, 8 Hz), 7.13 (1H, dt, J=1, 8 Hz), 7.22-7.29 (2H, m), 7.30 (1H, d, J=1 Hz), 7.46 (1H, dd, J=1, 8 Hz), 7.77 (1H, d, J=8 Hz).

1. customhas been prepared
2. washis washed with water
3. customdried
4. concentrationconcentrated under reduced pressure
5. customThe residue is recrystallized