反应详情

N-iodosuccinimide (73.4 mg, 0.33 mmol) was added to a stirred solution of 6-(4-fluoro-phenyl)-2-phenoxymethyl-7,8-dihydro-6H-imidazo[1,2-c]pyrimidin-5-one (0.1 g, 0.3 mmol) in a mixture of ACN (2 mL) and acetic acid (2 mL). The mixture was stirred at RT for 3 days. The mixture was diluted with DCM and washed with a saturated solution of Na2CO3. The organic layer was separated, dried (Na2SO4), filtered and the solvents evaporated in vacuo. The crude product was triturated with MeOH to yield 6-(4-fluoro-phenyl)-3-iodo-2-phenoxymethyl-7,8-dihydro-6H-imidazo[1,2-c]pyrimidin-5-one (46 mg, 56% yield) as a brown solid, that was used in the next step without further purification.

1. washwashed with a saturated solution of Na2CO3
2. customThe organic layer was separated
3. dry with materialdried (Na2SO4)
4. filtrationfiltered
5. customthe solvents evaporated in vacuo
6. customThe crude product was triturated with MeOH