反应详情

2-(6-tert-butoxycarbonylamino-pyridin-3-ylmethyl)-acrylic acid ethyl ester (0.49 g, 1.60 mmol) and triethylamine (0.17 g, 1.64 mmol) were added to thioacetic acid (3 mL) at 0° C. The mixture was stirred at room temperature for 6 h. The mixture was poured onto ice-water and extracted with CH2Cl2. The organic phase was washed with saturated NaHCO3 and dried. The crude product was purified by flash chromatography (MeOH/CH2Cl2, 2.5:100) to give 2-acetylsulfanylmethyl-3-(6-tert-butoxycarbonylamino-pyridin-3-yl)-propionic acid ethyl ester (0.36 g, 61%).

1. additionThe mixture was poured onto ice-water
2. extractionextracted with CH2Cl2
3. washThe organic phase was washed with saturated NaHCO3
4. customdried
5. customThe crude product was purified by flash chromatography (MeOH/CH2Cl2, 2.5:100)