反应详情

A solution of boron tribromide (6.3 ml) in chloroform (16 ml) is added dropwise to a solution of 5-methoxy-3-[(1-methylpiperidin-4-yl)thio]-1H-indole (8 g, prepared in Example 41) in chloroform (105 ml) at 0° C. After 3 hours at room temperature, the reaction mixture is poured onto ice and rendered basic with aqueous ammonia. The organic phase is dried over sodium sulfate and concentrated. The oily residue is chromatographed on silica gel (eluent: CH2Cl2 /EtOH/iPrNH2 79/20/1) to give 3-[(1-methylpiperidin-4-yl)thio]-1H-indol-5-ol (0.8 g), which is recrystallized from xylene.

1. additionthe reaction mixture is poured onto ice
2. dry with materialThe organic phase is dried over sodium sulfate
3. concentrationconcentrated
4. customThe oily residue is chromatographed on silica gel (eluent: CH2Cl2 /EtOH/iPrNH2 79/20/1)