反应详情

To 4-[6-Bromo-2-(4-dimethylamino-phenyl)-3H-imidazo[4,5-b]pyridin-7-yl]-piperazine-1-carboxylic acid tert-butyl ester (0.380 g, 0.75 mmol) in dichloromethane (20 mL) at 0° C. was added slowly TFA (2 mL) and the reaction mixture was stirred at rt for 30 mins. TFA (1 mL) was added and the reaction mixture was stirred at room temperature for 1 h. The reaction mixture was concentrated in vacuo and TFA was co-evaporated with CH3CN. The crude product was run trough a 5 g SCX cartridge and eluted with 0.1M NH3 in methanol. The compound was further triturated in ether/methanol 9/1 to give the title compound as a solid (0.228 g, 75%);

1. stirringthe reaction mixture was stirred at room temperature for 1 h
2. concentrationThe reaction mixture was concentrated in vacuo and TFA
3. washeluted with 0.1M NH3 in methanol
4. customThe compound was further triturated in ether/methanol 9/1