反应详情

To a stirred solution of 3-amino-6-bromo-5-trifluoromethyl-pyrazine-2-carboxylic acid (5-trifluoromethyl-2H-pyrazol-3-yl)-amide (Example 1) (40 mg, 0.095 mmol) in dry THF (2 ml) was added pyrrolidine (7.89 μL, 0.095 mmol). The resulting mixture was heated using microwave radiation at 120° C. for 35 minutes. The reaction mixture was partitioned between EtOAc (50 ml) and water (30 ml) and the organic portion was separated, (MgSO4) and concentrated in vacuo to give the crude product as an orange oil. The crude product was purified using preparative TLC eluting with DCM: 1% MeOH to afford the title compound as an orange solid.

1. temperatureThe resulting mixture was heated
2. customat 120° C.
3. customfor 35 minutes
4. customThe reaction mixture was partitioned between EtOAc (50 ml) and water (30 ml)
5. customthe organic portion was separated
6. concentration(MgSO4) and concentrated in vacuo
7. customto give the crude product as an orange oil
8. customThe crude product was purified
9. washeluting with DCM