反应详情

温度

120 °C

A mixture of 6-((6-bromo-1H-[1,2,3]triazolo[4,5-b]pyrazin-1-yl)methyl)quinoline, (350 mg, 1.03 mmol), potassium carbonate (436 mg, 3.16 mmol), and 3-pyrrolidine carboxylic acid (236 mg, 2.05 mmol) in n-butanol (10.0 mL) was heated in the microwave at 120° C. for 60 minutes. The reaction mixture was cooled to room temperature, filtered, rinsed with ethyl acetate, and the filtrate was concentrated. The crude product was purified by flash chromatography using a Horizon purification system on a 25S column eluting with chloroform containing 0.1% acetic acid/methanol (0.5-7%) to afford 1-[1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl]pyrrolidine-3-carboxylic acid (152 mg, 39%).

1. temperatureThe reaction mixture was cooled to room temperature
2. filtrationfiltered
3. washrinsed with ethyl acetate
4. concentrationthe filtrate was concentrated
5. customThe crude product was purified by flash chromatography
6. customa Horizon purification system on a 25S column
7. washeluting with chloroform containing 0.1% acetic acid/methanol (0.5-7%)