反应详情

Aq. 4M NaOH (3 mL) was added to a stirring mixture of 4-bromo-3-methyl-1H-indole (456 mg, 2.17 mmol; Intermediate 28), benzenesulfonyl chloride (306 μg, 2.39 mmol) and tetrabutylammonium hydrogen sulfate (74 mg, 0.22 mmol) in DCM (30 mL). The reaction mixture was stirred 1 h, combined with an earlier batch of this intermediate (followed this experimental and starting with 4-bromo-3-methyl-1H-indole, 100 mg, 0.48 mmol; Intermediate 28), washed twice with water, dried and concentrated. The crude product was purified by flash column chromatography (DCM/hexane 1:3). The product (650 mg, 70%) was obtained as a white solid. MS (ESI+) for C15H12BrNO2S m/z 350 (Monoisotop+H)+.

1. washIntermediate 28), washed twice with water
2. customdried
3. concentrationconcentrated
4. customThe crude product was purified by flash column chromatography (DCM/hexane 1:3)