反应详情

A solution of 175 mg of {4-[5-(2-fluoro-phenoxy)-oxazolo[5,4-d]pyrimidin-2-yl]-2,6-dimethyl-phenoxy}-acetyl chloride in 2 ml of dichloromethane was added slowly to a suspension of 102 mg of proline tert-butyl ester hydrochloride and 170 μl of triethylamine in 5 ml of dichloromethane. After stirring for 2 h, the solvent was removed in vacuo. 1.6 ml of trifluoroacetic acid were added and the mixture was stirred for 2 h at room temperature. Then 10 ml water were added and the aqueous layer was extracted three times with 15 ml of a dichloromethane/isopropanol mixture (3:1). After drying with sodium sulfate and filtration, the solvents were removed in vacuo and the title compound was isolated via preparative HPLC. Yield: 56 mg of a white solid.

1. customthe solvent was removed in vacuo
2. addition1.6 ml of trifluoroacetic acid were added
3. stirringthe mixture was stirred for 2 h at room temperature
4. additionThen 10 ml water were added
5. extractionthe aqueous layer was extracted three times with 15 ml of a dichloromethane/isopropanol mixture (3:1)
6. dry with materialAfter drying with sodium sulfate and filtration
7. customthe solvents were removed in vacuo