反应详情

According to Scheme 6, Step 2: NCS (8.14 mmol, 1.09 g) was added to a solution of 4-(1-(4-methoxybenzyl)-1H-pyrazol-4-yl)thiazol-2-amine (8.14 mmol, 2.33 g) in acetonitrile (20 mL) and the reaction mixture was stirred under reflux for 1.5 hour. After evaporation of the solvent, the crude residue was diluted in EtOAc. The organic phase was washed with water and brine, was dried over Na2SO4, was filtered and was concentrated. The crude mixture was purified by flash chromatography over silica gel using DCM/MeOH (100:0 to 90:10) as eluent to yield 4-(1-(4-methoxybenzyl)-1H-pyrazol-4-yl)-5-chlorothiazol-2-amine (2.35 mmol, 755 mg, 29%).

1. temperatureunder reflux for 1.5 hour
2. customAfter evaporation of the solvent
3. additionthe crude residue was diluted in EtOAc
4. washThe organic phase was washed with water and brine
5. dry with materialwas dried over Na2SO4
6. filtrationwas filtered
7. concentrationwas concentrated
8. customThe crude mixture was purified by flash chromatography over silica gel