5-Bromo-2-chloropyrimidine → (S)-1-(5-bromopyrimidin-2-yl)-pyrrolidine-3-amine

Participants

Reaction Steps

Combine 2-chloro-5-bromopyrimidine (20.0 g, 1.0 eq) and isopropanol (200 mL). Add (S)-3-aminopyrrolidine (8.91 g, 1.0 eq) dropwise over about 30 minutes. Add isopropanol (10 mL) and heat to 50° C.-60′. After 4 hours, cool to 20° C.-25° C. over about 1 hour, stir for about 1 hour, and then collect the solid by filtration. Rinse the solid with isopropanol (2×25 mL) and dry under vacuum at about 40° C. to give (S)-1-(5-bromopyrimidin-2-yl)-pyrrolidine-3-amine as its hydrochloride salt.

Provenance & Evidence