反应详情

2,2,2-Trifluoroethanol (1.5 ml) was added to a 10 mL vial charged with 4 N HCl in dioxane (0.135 ml, 0.54 mmol), 2-methoxy-4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)aniline (0.082 g, 0.27 mmol), and 3-(2,5-dichloropyrimidin-4-yl)-1-methyl-1H-indole (INTERMEDIATE 49, 0.075 g, 0.27 mmol). The reaction was stirred at RT for 5 min and then microwaved at 150° C. for 50 min. Concentration in vacuo gave a crude residue, and it was purified by silica gel chromatography (10% methanol andl% ammonium hydroxide in DCM) to give the product (0.105 g, 66.8%). The product was stirred in 20 mL of 0.5 N HCl in methanol for 1 min and then concentrated under reduced pressure to give the title product. (yellow solid).

1. custommicrowaved at 150° C. for 50 min
2. concentrationConcentration in vacuo
3. customgave a crude residue, and it
4. customwas purified by silica gel chromatography (10% methanol andl% ammonium hydroxide in DCM)