反应详情

The method described in Example 152 was used to treat 1-(4-amino-7-bromo-2-ethyl-1H-imidazo[4,5-c][1,5]naphthyridin-1-yl)-2-methylpropan-2-ol (1.0 g, 2.7 mmol) and 3-quinolineboronic acid (0.52 g, 3.0 mmol) in 1-propanol (10 mL) with triphenylphosphine (21.6 mg, 0.0820 mmol), aqueous sodium carbonate (4.1 mL of 2 M), water (2 mL), and palladium (II) acetate (6.2 mg, 0.027 mmol) with the following modifications. The reaction mixture was heated at reflux for four hours. The crude product was purified by recrystallization from ethyl acetate to provide 0.58 g of 1-[4-amino-2-ethyl-7-(quinolin-3-yl)-1H-imidazo[4,5-c][1,5]naphthyridin-1-yl)-2-methylpropan-2-ol as beige needles, mp >270° C.

1. temperatureThe reaction mixture was heated
2. temperatureat reflux for four hours
3. customThe crude product was purified by recrystallization from ethyl acetate