反应详情

To (S)-2-{4′-[(5-acetyl-4-methoxy-3-methyl-benzofuran-2-carbonyl)-amino]-biphenyl-4-sulfonylamino}-3-methyl-butyric acid methyl ester (89 mg) was added 1 mL of THF and 3 mL of LiOH solution (3.6 g LiOH/50 mL MeOH/50 mL H2O). The mixture was stirred at room temperature for 2 days. The solvents were removed under vacuum and the residue was triturated with 4 mL of 2N HCl and filtered. The solid product was dried under vacuum to give 54 mg of (S)-2-{4′-[(5-acetyl-4-methoxy-3-methyl-benzofuran-2-carbonyl)-amino]-biphenyl-4-sulfonylamino}-3-methyl-butyric acid was obtained as an off-white solid. 1H NMR (400 MHz, DMSO-d6) δ ppm 0.8 (dd, J=12.9, 6.8 Hz, 6 H) 2.0 (m, 1 H) 2.7 (s, 3 H) 2.9 (s, 3 H) 3.6 (dd, J=9.3, 6.1 Hz, 1 H) 4.0 (s, 3 H) 7.0 (d, J=8.8 Hz, 1 H) 7.8 (m, 4 H) 7.9 (m, 4 H) 8.0 (d, J=8.6 Hz, 1 H) 8.1 (d, J=9.3 Hz, 1 H) 10.3 (s, 1 H) 12.6 (s, 1 H).

1. customThe solvents were removed under vacuum
2. customthe residue was triturated with 4 mL of 2N HCl
3. filtrationfiltered
4. customThe solid product was dried under vacuum