反应详情

The above prepared (2-chloro-6-phenyl-pyrimidin-4-yl)-(5-methyl-2H-pyrazol-3-yl)-amine. (60 mg, 0.21 mmol) is combined with 4-acetamidothiophenol (176 mg, 1.05 mmol) in tert-butanol (5 mL) and the mixture heated at reflux for 20 hours. The reaction mixture is cooled to room temperature and partitioned between ethyl acetate and aqueous NaHCO3. The organic layer is washed with brine, dried over MgSO4 and concentrated in vacuo. The resulting residue is purified by flash chromatography (SiO2, DCM/MeOH gradient) to afford [2-(4-acetamido-phenylsulfanyl)-6-phenyl-pyrimidin-4-yl]-(5-methyl-2H-pyrazol-3-yl)-amine (74 mg, 85%)

1. temperaturethe mixture heated
2. temperatureat reflux for 20 hours
3. custompartitioned between ethyl acetate and aqueous NaHCO3
4. washThe organic layer is washed with brine
5. dry with materialdried over MgSO4
6. concentrationconcentrated in vacuo
7. customThe resulting residue is purified by flash chromatography (SiO2, DCM/MeOH gradient)