反应详情

温度

80 °C

A solution of ethyl 2-chloro-1,3-oxazole-4-carboxylate (0.59 g, 3.36 mmol) in dioxane was treated with 4-(hydroxymethyl)phenyl boronic acid (0.766 g, 5.04 mmol), K2CO3 (0.929 g, 6.72 mmol), t-Bu3PhBF4 (0.049 g, 0.168 mmol) heated to 80° C. then treated with Pd2(dba)3 (0.154 g 0.168 mmol) and stirred overnight at 90° C. The reaction mixture was diluted with EtOAc, washed with water, saturated sodium chloride, dried over MgSO4 and concentrated in in vacuo. The resultant residue was purified by flash chromatography (silica, EtOAc:hexanes 20→50%) to give the title product in 70% yield, identified by NMR and mass spectral analyses. LCMS (ESI+) 248 (MH+).

1. washwashed with water, saturated sodium chloride
2. dry with materialdried over MgSO4
3. concentrationconcentrated in in vacuo
4. customThe resultant residue was purified by flash chromatography (silica, EtOAc:hexanes 20→50%)