反应详情

温度

130 °C

To a solution of 2-(5-fluorobenzofuran-2-yl)-3-[methyl(propan-2-yl)amino]quinoxaline-6-carbonitrile (150 mg, 0.42 mmol) in DMSO (30 ml) and water (2 ml) was added ZnBr2 (46.9 mg, 0.21 mmol) and NaN3 (81.3 mg, 1.25 mmol), and the resulting mixture was stirred for 48 h at 130° C. The reaction mixture was quenched with water (100 ml) and adjusted to pH 3 with HCl (2N), extracted with ethyl acetate (4×60 ml), and the organic layers combined and concentrated in vacuo to give the residue, which was purified by silica gel column chromatography (12% methanol in dichloromethane) to afford 3-(5-fluorobenzofuran-2-yl)-N-methyl-N-(propan-2-yl)-7-(1H-tetrazol-5-yl)quinoxalin-2-amine as a yellow solid (62.6 mg, 37%).

1. customThe reaction mixture was quenched with water (100 ml)
2. extractionextracted with ethyl acetate (4×60 ml)
3. concentrationconcentrated in vacuo
4. customto give the residue, which
5. customwas purified by silica gel column chromatography (12% methanol in dichloromethane)