反应详情

温度

70 °C

2-(Tetrahydro-2H-pyran-2-yl)-6-[4-(tetrahydro-2H-pyran-2-yloxy)phenyl]-2H-indazol-4-amine (500 mg, 1.27 mmol), 6-bromo-2-pyridinecarboxylic acid (272 mg, 1.35 mmol), HATU (531 mg, 1.35 mmol) and DIPEA (0.442 ml, 2.54 mmol) were combined in DMF (10 ml) and heated at 70° C. overnight. The solvent was removed in vacuo and the residue was purified by silica gel chromatography, eluting with DCM:MeOH:ammonia. Appropriate fractions were combined and the solvent was removed in vacuo. The residue was dissolved in Methanol (20 ml) and 4 M HCl in dioxane (2 ml) and stirred at RT for 5 days. A small amount of the reaction mixture was removed (2 ml), the solvent was removed in vacuo and the residue purified by MDAP (Method B) to give the title compound.

1. customThe solvent was removed in vacuo
2. customthe residue was purified by silica gel chromatography
3. washeluting with DCM
4. customthe solvent was removed in vacuo
5. dissolutionThe residue was dissolved in Methanol (20 ml)
6. customA small amount of the reaction mixture was removed (2 ml)
7. customthe solvent was removed in vacuo
8. customthe residue purified by MDAP (Method B)