反应详情

Added MCPBA (70% wet, 3330 mg, 13.5 mmol) in portions to an ice-cooled suspension of 2-((2-chloro-5-cyano-3-vinylphenyl)amino)-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile (Example 399)(339 mg, 0.900 mmol) in CHCl3 (90 mL). The bath was removed and the reaction was left stirring at room temperature for 2 days. This was diluted with CHCl3 and washed with 5% aq. NaHSO3 solution and then 3 times 1 N Na2CO3 solution. After drying with sodium sulfate, the solvent was removed and radial silica gel chromatography eluting with DCM containing 0 to 10% EtOAc afforded 2-((2-chloro-5-cyano-3-(oxiran-2-yl)phenyl)amino)-4-(cyclopropylamino)imidazo[2,1-f][1,2,4]triazine-7-carbonitrile (293 mg) as a white solid.

1. temperaturecooled
2. customThe bath was removed
3. waitthe reaction was left
4. additionThis was diluted with CHCl3
5. washwashed with 5% aq. NaHSO3 solution
6. dry with materialAfter drying with sodium sulfate
7. customthe solvent was removed
8. washradial silica gel chromatography eluting with DCM containing 0 to 10% EtOAc