反应详情

WSC hydrochloride (69.0 mg, 0.36 mmol) was added to a mixture of 4-(benzo[b]thiophen-2-yl)benzoic acid (76.3 mg, 0.300 mmol), 6-(tetrazol-5-yl)spiro[chroman-2,4′-piperidin]-4-one hydrochloride (96.5 mg, 0.300 mmol), HOBT (45.9 mg, 0.300 mmol), triethylamine (0.042 mL, 0.300 mmol) and NMP (1.5 mL), and stirred at room temperature for 20 hours. The reaction mixture was concentrated under reduced pressure, and the residue was purified through high-performance preparative liquid chromatography (0.1% TFA, water/acetonitrile) to obtain the title compound as a pale yellow solid. 1H-NMR (400 MHz, DMSO-d6) δ: 8.44 (1H, d J=2.2 Hz), 8.25 (11, dd, J=8.5, 2.2 z), 8.00 (1H, d, J=8.3 Hz), 7.96 (1H, s), 7.89-7.83 (3H, m), 7.54 (2H, d, J=7.8 Hz), 7.44-7.33 (3H, m), 4.37-4.18 (1H, m), 3.65-3.18 (3H, m), 3.00 (2H, s), 2.13-1.75 (4H, m). MS [M−H]−=520.

1. concentrationThe reaction mixture was concentrated under reduced pressure
2. customthe residue was purified through high-performance preparative liquid chromatography (0.1% TFA, water/acetonitrile)