2,2,2-Trifluoroethanol → 5-Cyclobutylaminomethyl-pyrazin-2-ylamine
Reaction equation
[CH:1]1([NH:5][CH2:6][C:7]2[N:8]=[CH:9][C:10]([NH:13]C(=O)OC(C)(C)C)=[N:11][CH:12]=2)[CH2:4][CH2:3][CH2:2]1.FC(F)(F)CO>>[CH:1]1([NH:5][CH2:6][C:7]2[N:8]=[CH:9][C:10]([NH2:13])=[N:11][CH:12]=2)[CH2:2][CH2:3][CH2:4]1Participants
3
Conditions
- Temperature
- 150 °C
Procedure
In a 15 mL microwave tube was dissolved tert-butyl 5-((cyclobutylamino)methyl)pyrazin-2-ylcarbamate (330 mg, 1.19 mmol, Eq: 1.00) in 2,2,2-trifluoroethanol (119 mg, 12 ml, 1.19 mmol, Eq: 1.00) and the resulting mixture was heated in seal tube at 150° C. for 3 hrs. The crude reaction mixture was concentrated in vacuo, treated with MeOH and re-concentrated to remove residual trifluoroethanol. The material was azeotroped with toluene to afford 200 mg (95%) of the title compound.