Chloroacetone → 6-Bromo-2-methylimidazo[1,2-a]pyrimidine

Participants

Reaction Conditions

Reaction Steps

To a solution of 5-bromopyrimidin-2-amine (170.0 g, 0.98 mol) in i-PrOH (2 L) and DMF (500 mL) was added 1-chloropropan-2-one (606 g, 6.53 mol), then the mixture was stirred at 10° C. for 16 h. TLC (petroleum ether:ethyl acetate=1:2) showed the reaction was complete. The reaction mixture was quenched by Na2CO3 and filtered. The filtrate was concentrated in vacuo and the residue was purified by column chromatography (petroleum ether:ethyl acetate=5:1) to afford compound B-8-2 (10.0 g, 4.8%) as a yellow solid.

Provenance & Evidence