反应详情

To a solution of tert-butyl 2-(6-(cyanomethoxy)-1-hydroxy-4-methyl-1,3-dihydrobenzo[c][1,2]oxaborol-3-yl)acetate (120 mg, 0.38 mmol) in 5 ml DCM was added TFA (5 mL) at 0° C. The reaction mixture was stirred for 30 min at room temperature and concentrated to dryness. The residue was purified by prep HPLC to give the title compound as a white solid (60 mg, yield: 60.8%). 1H NMR (400 MHz, DMSO-d) δ12.31 (s, 1H), 9.24 (s, 1H), 7.16 (d, J=2.4 Hz, 1H), 6.97 (d, J=2.4 Hz, 1H), 5.48-5.45 (m, 1H), 5.15 (s, 2H), 3.06-3.02 (m, 1H), 2.28 (s, 3H), 2.12-2.05 (m, 1H); MS (ESI) m/z=262 [M+H]+.

1. concentrationconcentrated to dryness
2. customThe residue was purified by prep HPLC