反应详情

4-(5-Bromo-[1,2,4]triazolo[1,5-a]pyrazin-8-ylamino)-benzoic acid methyl ester (460 mg, 1.32 mmol) is suspended in THF (11 mL) and a solution of lithium hydroxide monohydrate (554 mg, 13.2 mmol) in water (11 mL) is added. The reaction mixture is stirred at room temperature for 4 hours then methanol (11 mL) is added and the mixture is stirred at 50° C. for 24 hours. The mixture is partitioned between water and DCM, the aqueous phase is acidified with 2M HCl (pH 2) and a yellow precipitate is formed. The precipitate is collected by filtration, washed with water and diethyl ether and dried to afford the title compound (215 mg, 49%).

1. stirringthe mixture is stirred at 50° C. for 24 hours
2. customThe mixture is partitioned between water and DCM
3. customa yellow precipitate is formed
4. filtrationThe precipitate is collected by filtration
5. washwashed with water and diethyl ether
6. customdried