反应详情

温度

20 °C

i-PrMgCl (0.44 mL of a 2 mmol/mL solution in THF, 0.88 mmol) was added dropwise to a stirred solution of oxazolo[4,5-c]pyridine (105 mg, 0.87 mmol) in anhydrous THF (3 mL) at 0° C. After 1 h, a solution of 4-(2-oxo-ethyl)piperidine-1-carboxylic acid tert-butyl ester (198 mg, 0.87 mmol) in anhydrous THF (2 mL) was added, then the mixture was allowed to warm to 20° C. over 16 h, before being quenched with saturated aqueous NH4Cl (10 mL). The layers were separated, then the aqueous phase was extracted with EtOAc (3×15 mL). The combined organic extracts were dried (MgSO4), filtered, and concentrated in vacuo. Flash chromatography (EtOAc) of the residue furnished the title compound: m/z (ES+)=348.1 [M+H]+.

1. custombefore being quenched with saturated aqueous NH4Cl (10 mL)
2. customThe layers were separated
3. extractionthe aqueous phase was extracted with EtOAc (3×15 mL)
4. dry with materialThe combined organic extracts were dried (MgSO4)
5. filtrationfiltered
6. concentrationconcentrated in vacuo