Sodium Carbonate → 3-({[Tert-butyl(dimethyl)silyl]oxy}methyl)-6-(2,6-difluorobenzyl)-2-(2,4-difluorophenyl)pyridine

Participants

Reaction Conditions

Reaction Steps

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).

Provenance & Evidence