反应详情

A solution of 7-iodo-1H-pyrazolo[4,3-b]pyridine (76 mg, 0.310 mmol) in DMF (4 ml) was cooled in an ice bath. Sodium hydride (16.13 mg, 0.403 mmol) was added and the reaction was stirred for 5 minutes. 4-Bromomethyl-piperidine-1-carboxylic acid tert-butyl ester (104 mg, 0.372 mmol) was added and the reaction was warmed to room temperature and then to 65° C. for 20 minutes. The reaction was then cooled, quenched with water and saturated NH4Cl solution and extracted with EtOAc. The organic layer were separated, dried over Na2SO4, filtered, and concentrated in vacuo to give tert-butyl 4-((7-iodo-2H-pyrazolo[4,3-b]pyridin-2-yl)methyl)piperidine-1-carboxylate which was used in the next step without further purification.

1. waitto 65° C. for 20 minutes
2. temperatureThe reaction was then cooled
3. customquenched with water and saturated NH4Cl solution
4. extractionextracted with EtOAc
5. customThe organic layer were separated
6. dry with materialdried over Na2SO4
7. filtrationfiltered
8. concentrationconcentrated in vacuo