反应详情

3-(2-Chloropyrimidin-4-yl)-7-(1-methyl-1-triethylsilanyloxyethyl)-imidazo[1,2-α]pyrimidine (from Example 34) (403 mg, 1.0 mmol), 4-tributylstannylpyridine (736 mg, 2.0 mmol), tetrakis(triphenylphosphine)palladium(0) (115 mg, 10 mol %) and copper(I) iodide (115 mg) in 1,4-dioxane (20 ml) were heated at reflux overnight. Purification by column chromatography on silica using 3-6% MeOH/CH2Cl2 as the eluent afforded 7-(1-methyl-1-triethylsilanyloxyethyl)-3-[2-(pyridin-4-yl)pyrimidin-4-yl]imidazo[1,2-α]pyrimidine: 1H NMR (400 MHz, d6-DMSO) δ 10.23 (1H, d, J 7.3), 8.98 (1H, d, J 5.4), 8.89 (1H, s), 8.85-8.80 (2H, m), 8.36 (2H, d, J 5.9), 8.14 (1H, d, J 5.5), 7.70 (1H, d, J 7.3), 1.65 (6H, s), 0.95 (9H, t, J 7.8), 0.66 (6H, q, J 7.8).

1. temperatureat reflux overnight
2. customPurification by column chromatography on silica using 3-6% MeOH/CH2Cl2 as the eluent