反应详情

温度

80 °C

A suspension of 1-[1-(quinolin-6-ylmethyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl]pyrrolidin-3-one (50 mg, 0.15 mmol) and 3,3-difluoropyrrolidine (42 mg, 0.29 mmol) in tetrahydrofuran/methanol/dimethylacetamide (1.0 mL each) was heated to 80° C. for 2 hours then NaBCNH3 (18 mg, 0.29 mmol) was added. After 2 hours the solution was cooled to room temperature and concentrated. The crude product was purified by flash chromatography using a Horizon purification system on a 25S column eluting with chloroform/acetone (5-50%) followed by a second column on a 12M cartridge eluting with chloroform/ethyl acetate (25-100%) to afford the title compound (25 mg, 40%).

1. additionNaBCNH3 (18 mg, 0.29 mmol) was added
2. temperatureAfter 2 hours the solution was cooled to room temperature
3. concentrationconcentrated
4. customThe crude product was purified by flash chromatography
5. customa Horizon purification system on a 25S column
6. washeluting with chloroform/acetone (5-50%)
7. washeluting with chloroform/ethyl acetate (25-100%)