反应详情

温度

90 °C

The mixture of 2-chloro-4-iodo-5-(trifluoromethyl)pyridine (0.615 g, 2.0 mmol, 1.0 eq), 3-amino-N-methylpicolinamide (0.303 g, 1.2 eq), Pd2(dba)3 (0.183 g, 0.1 eq), Xantphos (0.347 g, 0.3 eq), Cs2CO3 (1.3 g, 2.0 eq) in dioxane (15 mL) was stirred at 90° C. in an oil bath overnight. The mixture was cooled to room temperature and filtered through a celite pad. The celite pad was washed with methanol. The solvent was removed to obtain the crude which was purified by silica gel chromatography (20%˜80% EtOAc/Hex) to obtain the desired product (0.146 g, isolated yield 22%).

1. temperatureThe mixture was cooled to room temperature
2. filtrationfiltered through a celite pad
3. washThe celite pad was washed with methanol
4. customThe solvent was removed
5. customto obtain the crude which
6. customwas purified by silica gel chromatography (20%˜80% EtOAc/Hex)