反应详情

A solution of 8.8 g of 3-(2-bromoethyl)-5-methoxy indole in 100 ml of dimethylformamide is added to a stirring mixture of 4-(4-toluyl)piperidine hydrochloride [Example 5(a)] and 10.1 g of potassium carbonate in 400 ml of dimethylformamide and the reaction mixture is stirred at ambient temperature for 80 hours and then at 50° C. for 10 additional hours. It is cooled to ambient temperature, filtered, and 2 liters of water are added dropwise to produce a precipitate. The precipitate is triturated with ether and eluted with a 5% methanol in benzene solution through a silica gel column. The precipitate is recrystallized from an ethanol-water mixture to give off-white crystals, mp 131°-133° C., 5-methoxy-3-{2-[4-(4-toluyl)piperidyl]ethyl}indole.

1. customat 50° C.
2. temperatureIt is cooled to ambient temperature
3. filtrationfiltered
4. addition2 liters of water are added dropwise
5. customto produce a precipitate
6. customThe precipitate is triturated with ether
7. washeluted with a 5% methanol in benzene solution through a silica gel column
8. customThe precipitate is recrystallized from an ethanol-water mixture