反应详情

A mixture of 5-(2,6-diethyl-phenyl)-1H-pyrrolo[2,3-c]pyridine (200 mg, 0.90 mmol), 4-oxo-piperidine-1-carboxylic acid tert-butyl ester (358 mg, 1.8 mmol), Cs2CO3 (586 mg, 1.8 mmol), and MeOH (6 mL) is refluxed for 18 h. MeOH is removed under reduced pressure. The residue is treated with acetic acid (0.5 mL) and water (3 mL) and is extracted with EtOAc. The combined organic extracts are washed with brine, dried over Na2SO4, and concentrated under reduced pressure. Chromatography of the residue affords 4-[5-(2,6-Diethyl-phenyl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-3,6-dihydro-2H-pyridine-1-carboxylic acid tert-butyl ester as colorless oil.

1. temperatureis refluxed for 18 h
2. customMeOH is removed under reduced pressure
3. additionThe residue is treated with acetic acid (0.5 mL) and water (3 mL)
4. extractionis extracted with EtOAc
5. washThe combined organic extracts are washed with brine
6. dry with materialdried over Na2SO4
7. concentrationconcentrated under reduced pressure