反应详情

温度

100 °C

To a mixture of [4-azidomethyl-1-hydroxy-6-(pyrazin-2-yloxy)-1,3-dihydro-benzo[c][1,2]oxaborol-3-yl]-acetic acid ethyl ester (200 mg, 0.54 mmol) was added 1N HCl (5 mL) and AcOH (20 mL). The mixture was heated at 100° C. for 4 h. The acid was removed under vacuum and the crude product was purified by HPLC, yielded 100 mg of desire product. 1H NMR (300 MHz, CD3CN) δ 8.59 (s, 1H), 8.44 (s, 1H), 8.23 (s, 1H), 8.20 (s, 1H), 7.59 (s, 1H), 7.43 (s, 1H), 5.81 (dd, 1H), 4.54-4.72 (m, 2H), 3.23-3.29 (m, 2H), 2.49-2.58 (dd, 2H), 2.08 (t, 3H).

1. customThe acid was removed under vacuum
2. customthe crude product was purified by HPLC
3. customyielded 100 mg of desire product