反应详情

To a solution of 5-(m-tolyl)oxazole-4-carboxylic acid (550 mg, 2.71 mmol) in DCM (15 mL), TBTU (1.303 g, 4.06 mmol) and DIPEA (1.39 mL, 8.12 mmol) was added. After stirring for 40 min at rt, 2-(4-amino-3,5-dimethyl-1H-pyrazol-1-yl)ethanol (420 mg, 2.71 mmol) dissolved in DCM (5 mL) was added to the solution and the resulting mixture was stirred at rt for 1 h. The reaction mixture was diluted with DCM and water, the organic layer was separated and the aq. layer was extracted with DCM (2×). The combined org. layers were washed with brine, dried (MgSO4), filtered and the solvent was removed under reduced pressure. Purification by FC (DCM/MeOH 92:8) yielded the title compound as a white solid. LC-MS conditions A: tR=0.70 min, [M+H]+=341.46.

1. additionwas added to the solution
2. stirringthe resulting mixture was stirred at rt for 1 h
3. customthe organic layer was separated
4. extractionthe aq. layer was extracted with DCM (2×)
5. washlayers were washed with brine
6. dry with materialdried (MgSO4)
7. filtrationfiltered
8. customthe solvent was removed under reduced pressure
9. customPurification by FC (DCM/MeOH 92:8)