反应详情

To a suspension of 4-(2-bromoethyl-2(1H)-quinolinone (II-2) (30 g, 119 mmol) and 3-(4-piperidinyl)-1H-indole (23.8 g, 119 mmol) in dry dimethylformamide 300 ml was added triethylamine (33 ml, 238 mmol) at room temperature and the mixture was allowed to react under the same conditions for 48 hours. Water (600 ml) was poured into the reaction mixture and the mixture was stirred for 15 minutes at room temperature. The separated solid was filtered off by aspiration. The solid was washed with water, dried under reduced pressure and recrystallized with methanol/tetrahydrofuran/water to give the desired product (103 g) (III-2) as white solid (mp 259°-259.5 ° C. (methanol/tetrahydrofuran/water), yield 70.9 %).

1. customto react under the same conditions for 48 hours
2. filtrationThe separated solid was filtered off by aspiration
3. washThe solid was washed with water
4. customdried under reduced pressure
5. customrecrystallized with methanol/tetrahydrofuran/water