Diisopropylethylamine → 1-(4-{[4-(2-Oxo-2,3-dihydro-1H-benzimidazol-1-yl)piperidin-1-yl]methyl}phenyl)-2-phenylethane-1,2-dione

Participants

Reaction Steps

A mixture of 1-[4-(bromomethyl)phenyl]-2-phenylethane-1,2-dione (6.06 g, 20.0 mmol), 1-piperidin-4-yl-1,3-dihydro-2H-benzimidazol-2-one (4.56 g, 21.0 mmol), PS-DIEA (20 g, 74 mmol), and TEA (50 mg, 0.5 mmol) was stirred overnight at rt in THF-MeOH (1:1, 300 mL). After this time, the resin (PS-DIEA) was filtered and washed with MeOH (2×100 mL). The combined solution was concentrated to afford the desired product. This product is pure enough (by LCMS) for next step reaction. Analytical LCMS: single peak (ELSD), 2.483 min.

Provenance & Evidence