反应详情

A solution of 399 (scheme 87) (700 mg, 1.68 mmol), Cs2CO3 (1.12 g, 3.43 mmol), 3-methoxyaniline (190 μL, 206 mg, 1.68 mmol), Pd(OAc)2 (70 mg, 0.17 mmol) and Xantphos (1.43 g, 2.52 mmol) (J. Org. Chem., 1999, 64, 6019-6022) in dioxane (15 mL) was heated to reflux for 5 hrs. The reaction mixture was cooled, concentrated and the residue was purified by flash chromatography using 80% EtOAc in hexanes as the eluent, to afford 403 (408 mg, 59% yield). MS (m/z): (M+1) 412.0 (100%).

1. temperatureto reflux for 5 hrs
2. temperatureThe reaction mixture was cooled
3. concentrationconcentrated
4. customthe residue was purified by flash chromatography