反应详情

Into a round bottom flask charged with 6-(2,4-difluorophenyl)-imidazo[2,1-b]oxazole (5.0 g, 23 mmol; prepared using A from 6-(2,4-difluorophenyl)-imidazo[2,1-b]oxazole [prepared according to WO2004110990A2, Example 1, Steps 1-3 using 2-bromo-1-(2,4-difluorophenyl)-ethanone in place of 2-bromo-1-(4-fluorophenyl)-ethanone]) and DMF (100 mL) was added a solution of NIS (5.4 g, 24 mmol) in DMF (20 mL) at ambient temperature. The reaction was allowed to stir at ambient temperature for about 1 h upon which time it was poured into water (800 mL). The resulting precipitate was filtered, washed with water (2×20 mL), and dried in a vacuum oven for about 16 h to provide the title compound (7.5 g, 95%) as a light yellow solid: LC/MS (Table 1, Method a) Rt=2.04 min; MS m/z/z: 347.0 (M+H)+.

1. customprepared
2. filtrationThe resulting precipitate was filtered
3. washwashed with water (2×20 mL)
4. customdried in a vacuum oven for about 16 h