反应详情

A solution of 0.1 g (0.2 mmole) 4-(4-benzyl-piperazin-1-yl)-1-(3,5-dichloro-benzenesulfonyl)-1H-indole and 0.05 mL (0.46 mmole) 1-chloroethyl chloroformate in 10 mL 1,2-dichloroethane was heated under reflux for 0.5 hour. The solution was concentrated under reduced pressure and the residue was dissolved in 6 mL methanol. The solution was heated under reflux for 1 hour, then it was concentrated. 1-(3,5-Dichloro-benzenesulfonyl)-4-piperazin-1-yl-1H-indole (2) was isolated as the hydrochloride salt from methanol/ethyl ether, 74 mg, M+H=410, m.p. 156-157° C.

1. temperatureunder reflux for 0.5 hour
2. concentrationThe solution was concentrated under reduced pressure
3. dissolutionthe residue was dissolved in 6 mL methanol
4. temperatureThe solution was heated
5. temperatureunder reflux for 1 hour
6. concentrationit was concentrated