反应详情

温度

80 °C

To a solution of (Z)-ethyl 3-(2,6-dimethoxypyridin-3-yl)-3-((2-hydroxyethyl)amino)acrylate (100 mg, 0.34 mmol) in 2-MeTHF (1.0 mL) was added (trimethylsilyl)isothiocyanate (0.30 mL, 2.0 mmol) and the reaction mixture was heated at 80° C. for 4 hours. The cooled reaction mixture was diluted with EtOAc and washed with a saturated aqueous sodium bicarbonate solution. The layers were separated and the organic layer was concentrated in vacuo. The residue was triturated with MeOH and the resulting solids were collected by vacuum filtration to give the title compound (16 mg, 16%) as a white solid.

1. customThe cooled reaction mixture
2. washwashed with a saturated aqueous sodium bicarbonate solution
3. customThe layers were separated
4. concentrationthe organic layer was concentrated in vacuo
5. customThe residue was triturated with MeOH
6. filtrationthe resulting solids were collected by vacuum filtration