Water → (3S)-1-(5-bromopyrimidin-2-yl)-N-[(2,4-dichlorophenyl)methyl]pyrrolidin-3-amine

Participants

Reaction Conditions

Reaction Steps

Add to a solution of (2,4-dichlorobenzyl)-(S)-pyrrolidin-3-ylamine (300 g, 1.22 mol) in acetonitrile (2.25 L) at room temperature diisopropylethylamine (237 g, 1.83 mol) and 5-bromo-2-chloropyrimidine (237 g, 1.23 mol). Reflux for 1 hour. Cool the mixture to 20° C. Add water (45 mL, 2.5 mol) dropwise to give a solid. Stir for 17 h., filter the suspension, and wash the cake with acetonitrile (250 mL), and dry under vacuum at room temperature to give the title compound as a tan solid (377 g, 83%).

Provenance & Evidence