反应详情

(2-Amino-5-bromo-pyridin-3-ylmethoxy)-acetic acid ethyl ester (381 mg, 1.3 mmol) is dissolved in 15 mL of DMSO and 60% sodium hydride (53 mg, 1.3 mmol) is added. The mixture is stirred for 4 hrs and then ice-cold water (100 mL) is added into reaction. The solid formed is filtered and rinsed with more water (2×50 mL) and 50% EtOAc in heptane (30 mL). Then it is dried to give 205 mg of 3-bromo-5,9-dihydro-6-oxa-1,9-diaza-benzocyclohepten-8-one which is used without purification.

1. customThe solid formed
2. filtrationis filtered
3. washrinsed with more water (2×50 mL) and 50% EtOAc in heptane (30 mL)
4. customThen it is dried