2,4-Dichloro-6-methylpyrimidine → 1-(2-Chloro-6-methylpyrimidin-4-yl)-1'-(5-methylpyrazin-2-yl)-4,4'-bipiperidine

Participants

Reaction Conditions

Reaction Steps

The 1-(5-methylpyrazin-2-yl)-4,4′-bipiperidine (720 mg, 2.8 mmol) and 2,4-dichloro-6-methyl-pyrimidine (502 mg, 3.1 mmol) were dissolved in NMP (30 mL), and the solution cooled to −20° C. The 1,8-diazabicyclo[5.4.0]-undec-7-ene (4.2 mL, 28 mmol) was added drop-wise and the solution stirred for 10 minutes. The mixture was diluted with ethyl acetate (50 mL), washed with brine (30 mL×2), dried over magnesium sulfate, filtered and concentrated in vac. The residue was purified by chromatography on silica gel with 30% acetone: hexanes to yield the title compound.

Provenance & Evidence