反应详情

TFA (60 mL) was added 1-(tert-butoxycarbonyl)-4-fluoro-1H-indol-2-ylboronic acid (10 g, 35.83 mmol) in portions at 0° C. and then the mixture was stirred at room temperature for 3 hours. The mixture was poured into ice water, stirred for 10 minutes and filtered through a pad to give the crude 4-fluoro-1H-indol-2-ylboronic acid (6.0 g, yield: 94%) without further purification. 1H-NMR (DMSO-d6, 400 MHz) δ 11.09 (s, 1H), 8.35 (br s, 2H), 7.22 (d, J=8.00 Hz, 1H), 7.02˜7.07 (m, 2H), 6.68˜6.72 (m, 1H). MS (M+H)+: 180.

1. stirringstirred for 10 minutes
2. filtrationfiltered through a pad