反应详情

2-Methyl-6-[(1-propionylpyrrolidin-3-yl)oxy]pyridin-3-amine (340 mg) was dissolved in pyridine (3.3 mL) and 4-isopropylbenzenesulfonyl chloride (358 mg) was slowly added under stirring. After 19 h stirring at room temperature, the reaction mixture was diluted with dichloromethane and 2 M aqueous NaOH was added. After stirring for 1 h at room temperature the phases were separated. The organic phase was dried (sodium sulfate), concentrated and the crude product purified by flash chromatography (silica, dichloromethane, 0.5 to 5% methanol gradient). Yield: 460 mg (78%, pale yellow oil).

1. stirringAfter 19 h stirring at room temperature
2. additionwas added
3. stirringAfter stirring for 1 h at room temperature the phases
4. customwere separated
5. dry with materialThe organic phase was dried (sodium sulfate)
6. concentrationconcentrated
7. customthe crude product purified by flash chromatography (silica, dichloromethane, 0.5 to 5% methanol gradient)