反应详情

温度

115 °C

The product from Example 68A (40 mg, 0.16 mmol) was mixed with tert-butyl hexahydro-1H-pyrrolo[3,4-c]pyridine-5(6H)-carboxylate (55 mg, 0.24 mmol) and to this was added 2-methoxyethanol (0.65 mL), and N,N-diisopropylethylamine (0.20 mL, 1.2 mmol); the reaction was heated at 115° C. for 16 hours, cooled, diluted with CH2Cl2 (25 mL) and washed with 1 M NaOH (10 mL). The aqueous layer was extracted with CH2Cl2 (15 mL). The combined organics were dried (MgSO4), filtered, concentrated and chromatographed and eluted with a gradient of 1:0 to 0:1 CH2Cl2:EtOAc to provide the title compound.

1. temperaturecooled
2. washwashed with 1 M NaOH (10 mL)
3. extractionThe aqueous layer was extracted with CH2Cl2 (15 mL)
4. dry with materialThe combined organics were dried (MgSO4)
5. filtrationfiltered
6. concentrationconcentrated
7. customchromatographed
8. washeluted with a gradient of 1:0 to 0:1 CH2Cl2