反応 #86210

反応方程式

1-(6-bromo-2-pyridyl)-6-chloro-pyrazolo[4,3-c]pyridine

tert-butyl N-[(3S)-2-oxo-3-piperidyl]carbamate

Potassium carbonate

N,N′-Dimethylethylenediamine

→

desired product

収率 47.2%

tert-butyl N-[(3S)-1-[6-(6-chloropyrazolo[4,3-c]pyridin-1-yl)-2-pyridyl]-2-oxo-3-piperidyl]carbamate

収率 47.2%

反応条件

後処理

1. 1
   その他4 h
2. 2
   ろ過The reaction was filtered through celite
3. 3
   濃縮concentrated
4. 4
   その他The crude product purified by isco column (EtOAc/Hep eluted at 70% EtOAc)

実験手順

A solution containing 1-(6-bromo-2-pyridyl)-6-chloro-pyrazolo[4,3-c]pyridine (200 mg, 0.646 mmol), tert-butyl N-[(3S)-2-oxo-3-piperidyl]carbamate (166 mg, 0.775 mmol), Copper(I) iodide (123 mg, 0.646 mmol), Potassium carbonate (107 mg, 0.775 mmol) and N,N′-Dimethylethylenediamine (114 mg, 1.29 mmol) was stirred at 110° C. 4 h. The reaction was filtered through celite and concentrated. The crude product purified by isco column (EtOAc/Hep eluted at 70% EtOAc) to give the desired product 135 mg 47% yield. MS (ESI) m/z: 443.1.

出典