反应详情

1.65 g (3.30 mmol) of (RS)-S-[4-({5-bromo-4-[(R)-(2-hydroxy-1,2-dimethylpropyl)amino]pyrimidin-2-yl}amino)phenyl]-N-(ethoxycarbonyl)-S-methyl sulfoximide in 6.5 ml of ethanol is mixed with 19.1 ml (6.69 mmol) of a 0.35 molar solution of NaOEt in ethanol and stirred under reflux for 5 hours. The batch is stirred overnight at room temperature and then added to a saturated NaCl solution. It is extracted with ethyl acetate, and the combined organic phases are dried (Na2SO4), filtered and concentrated by evaporation. The remaining residue is purified by chromatography (DCM/EtOH 9:1). 0.95 g (2.22 mmol, corresponding to 67% of theory) of the product is obtained.

1. temperatureunder reflux for 5 hours
2. stirringThe batch is stirred overnight at room temperature
3. extractionIt is extracted with ethyl acetate
4. dry with materialthe combined organic phases are dried (Na2SO4)
5. filtrationfiltered
6. concentrationconcentrated by evaporation
7. customThe remaining residue is purified by chromatography (DCM/EtOH 9:1)
8. custom0.95 g (2.22 mmol, corresponding to 67% of theory) of the product is obtained