反应详情

To a solution of 2-(4,6-difluoro-1-methyl-1H-indazol-3-yl)-5-(2-trimethylsilanylethoxymethyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid (115 mg, 0.23 mmol), HOBt (92 mg, 0.55 mmol) and EDC (105 mg, 0.55 mmol) in DMF (3 ml) was added isopropylamine (41 ul, 0.48 mmol) and N,N-diisopropylethylamine (0.17 ml, 0.95 mmol). The reaction mixture was stirred at room temperature overnight then quenched with water and extracted with EtOAc (2×). The combined organic layers were washed with 10% citric acid, sat NaHCO3, sat LiCl, and brine then dried over MgSO4 and concentrated. The residue was chromatographed over silica gel with 20% to 100% EtOAc/heptane to afford 98 mg (78%) of 2-(6-fluoro-1-oxetan-3-yl-1H-indazol-3-yl)-5-(2-trimethylsilanyl-ethoxymethyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid isopropylamide as a white solid.

1. customthen quenched with water
2. extractionextracted with EtOAc (2×)
3. washThe combined organic layers were washed with 10% citric acid
4. dry with materialthen dried over MgSO4
5. concentrationconcentrated
6. customThe residue was chromatographed over silica gel with 20% to 100% EtOAc/heptane