反应详情

A mixture of N-benzyl-3-(benzyloxy)-6-(2-(4-fluorophenyl)-3-(methylcarbamoyl)-6-(N-methylmethylsulfonamido)benzofuran-5-yl)picolinamide (200 mg, 0.29 mmol) and Pd/C (10 mg) in CH3OH (10 mL) was stirred at room temperature overnight under H2 atmosphere (50 psi). The mixture was filtered and the filtrate was concentrated in vacuum. The residue was purified by prep-TLC (DCM:EtOAc=5:1) to give the product of N-benzyl-6-(2-(4-fluorophenyl)-3-(methylcarbamoyl)-6-(N-methylmethylsulfonamido)benzofuran-5-yl)-3-hydroxypicolinamide (125 mg, yield: 71.8%). 1H-NMR (CDCl3, 400 MHz) δ 8.73 (br s, 1H), 7.84˜7.87 (m, 3H), 7.63 (d, J=8.4 Hz, 1H), 7.49 (s, 1H), 7.44 (d, J=8.4 Hz, 1H), 7.30˜7.36 (m, 4H), 7.26 (d, J=6.0 Hz, 1H), 7.19 (t, J=8.0 Hz, 2H), 6.39 (br s, 1H), 4.60 (d, J=4.8 Hz, 2H), 3.04 (s, 3H), 2.93 (d, J=3.2 Hz, 3H), 2.87 (s, 3H). MS (M+H)+: 603.

1. filtrationThe mixture was filtered
2. concentrationthe filtrate was concentrated in vacuum
3. customThe residue was purified by prep-TLC (DCM:EtOAc=5:1)