反应详情

To a solution of 67A (245 mg, 1 mmol) and 66A (268 mg, 1.05 mmol) in DMF (4 mL), was added EDCI (288 mg, 1.5 mmol), HOAt (14 mg, 0.1 mmol) and DIEA (0.54 mL, 3 mmol). The mixture was stirred rt for 16 h, then was quenched with water and extracted with EtOAc (3×20 mL). The organic layer washed by brine, dried (Na2SO4) and concentrated. Purification via flash chromatography (0-40% EtOAc in hexanes) gave 67B (300 mg, 62%). MS (ESI) m/z 483.3 (M+H)+.

1. customwas quenched with water
2. extractionextracted with EtOAc (3×20 mL)
3. washThe organic layer washed by brine
4. dry with materialdried (Na2SO4)
5. concentrationconcentrated
6. customPurification via flash chromatography (0-40% EtOAc in hexanes)