反应详情

A stirred suspension of 3,4-diamino-6-(4-ethoxy-3-trifluoromethyl-phenyl)-pyridine-2-carbonitrile (4.4 g, 13.7 mmol), ytterbium triflate (173 mg, 2 mol %), triethylorthoformate (6.08 g, 41.1 mmol) and acetonitrile (50 ml) was heated to reflux for 30 minutes. The solid precipitate was collected by filtration and washed sparingly with acetonitrile to afford 6-(4-ethoxy-3-trifluoromethyl-phenyl)-1H-imidazo[4,5-c]pyridine-4-carbonitrile (2.6 g). 1H NMR (DMSO): δ 8.67 (s, 1H), 8.47 (s, 1H), 8.36 (m, 2H), 7,49 (d, 1H), 4.26 (q, 2H), 1.38 (t, 3H). MS m/z 333.3(M+1).

1. temperaturewas heated
2. temperatureto reflux for 30 minutes
3. filtrationThe solid precipitate was collected by filtration
4. washwashed sparingly with acetonitrile