反应详情

温度

90 °C

To a crude 3-({[tert-butyl(dimethyl)silyl]oxy}methyl)-2-chloro-6-(2,6-difluorobenzyl)pyridine (from Step C above) in DME was added 2,4-difluorophenylboronic acid (6.5 g), tetrakis(triphenylphosphine)palladium (2 g) and 2N Na2CO3 (40 mL), and heated to 90° C. for a couple of hours until reaction completed. The mixture was cooled to room temperature and filtered through celite. The mixture was diluted with ethyl acetate, washed with water, brine, dried over MgSO4 and concentrated. The residue was purified by silica gel (100% methylene chloride) to give title compound (4.81 g).

1. temperatureThe mixture was cooled to room temperature
2. filtrationfiltered through celite
3. additionThe mixture was diluted with ethyl acetate
4. washwashed with water, brine
5. dry with materialdried over MgSO4
6. concentrationconcentrated
7. customThe residue was purified by silica gel (100% methylene chloride)