反应详情

A solution of 1-(4-amino-2-fluorophenyl)-2,3-dihydro-1H-pyridin-4-one (Step 4, 0.412 g, 2.0 mmol) and oxirane-2(R)-carboxylic acid ethyl ester (0.394 g, 3.4 mmol) with lithium triflate (0.360 g, 3.0 mmol) in dry acetonitrile (5.0 mL) is heated at 50–60° C. for 24 h. Volatiles are removed under vacuum, and the crude material purified by silica gel flash chromatography (eluent: 5% acetone in CH2Cl2) to afford the title compound (290 mg, 45%) as a viscous yellow oil, MS (m/z): 323 [M+H]+.

1. customVolatiles are removed under vacuum
2. customthe crude material purified by silica gel flash chromatography (eluent: 5% acetone in CH2Cl2)