反应详情

tert-Butyl 4-(1H-pyrrolo[2,3-b]pyridin-3-yl)-5,6-dihydropyridine-1(2H)-carboxylate (1.35 g, 4.51 mmol), ammonium formate (1.42 g, 22.55 mmol) and 5% palladium on activated carbon (50 mg) in ethanol (25 mL) were stirred and refluxed for 1 hour. The resulting mixture was cooled to room temperature and filtered through diatomaceous earth. The filtrate was concentrated by evaporation then treated with dilute aqueous ammonium chloride (50 mL) and extracted with DCM. The extract was washed with water, dried over MgSO4 and evaporated to a colourless solid. The solid was triturated with ether then collected by filtration and dried under vacuum to give tert-butyl 4-(1H-pyrrolo[2,3-b]pyridin-3-yl)piperidine-1-carboxylate (1.088 g, 80%) as a colourless solid.

1. temperaturerefluxed for 1 hour
2. filtrationfiltered through diatomaceous earth
3. concentrationThe filtrate was concentrated by evaporation
4. additionthen treated with dilute aqueous ammonium chloride (50 mL)
5. extractionextracted with DCM
6. washThe extract was washed with water
7. dry with materialdried over MgSO4
8. customevaporated to a colourless solid
9. customThe solid was triturated with ether
10. filtrationthen collected by filtration
11. customdried under vacuum