反应详情

To a suspension of tert-butyl(2-(4-(5-(m-tolyl)oxazole-4-carboxamido)-1H-pyrazol-1-yl)ethyl)carbamate (4.29 g, 10.426 mmol) in DCM (60 mL), TFA (12 mL, 156.39 mmol) was added at 0° C. After strring for 1 h at rt, the reaction mixture was concentrated. The residue was dissolved in DCM and 2 N aq. NaOH-solution was added. The org. layer was separated and the aq. layer was extracted with DCM (2×). The combined org. layers were dried (MgSO4), filtered and the solvent removed to yield the title compound as a white solid, which was used in the next step without further purification. LC-MS conditions B: tR=0.54 min, [M+H]+=312.31.

1. additionwas added at 0° C
2. concentrationthe reaction mixture was concentrated
3. dissolutionThe residue was dissolved in DCM
4. addition2 N aq. NaOH-solution was added
5. customlayer was separated
6. extractionthe aq. layer was extracted with DCM (2×)
7. dry with materiallayers were dried (MgSO4)
8. filtrationfiltered
9. customthe solvent removed