反应详情

温度

55 °C

To a mixture of (5-bromo-2-chloro-pyrimidin-4-yl)-(1-ethyl-propyl)-amine (0.44 g, 1.58 mmol), Pd(Ph3P)2Cl2 (0.11 g, 0.16 mmol), and CuI (0.03 g, 0.16 mmol) in DMF (14 mL) is added 3-butyn-2-ol (0.19 mL, 2.37 mmol) and triethylamine (0.44 mL, 3.16 mmol). The reaction mixture is stirred at 55° C. for 16 h, diluted with CH2Cl2, filtered through a pad of Celite, and concentrated in vacuo. Purification by flash chromatography (SiO2, EtOAc/Hexane 1:3) gave 0.23 g of 4-[2-chloro-4-(1-ethyl-propylamino)-pyrimidin-5-yl]-but-3-yn-2-ol as yellowish oil.

1. filtrationfiltered through a pad of Celite
2. concentrationconcentrated in vacuo
3. customPurification by flash chromatography (SiO2, EtOAc/Hexane 1:3)