反应详情

Intermediate (12a) (0.5 g, 1.7 mmol) was added to N-hydroxysuccinimide (290 mg, 2.6 mmol) and EDC (320 mg, 1.7 mmol) and dissolved in MeCN (6 mL). The mixture was stirred overnight at room temperature and then partitioned between EtOAc and 10% aqueous citric acid. The organic layer was separated, washed with saturated aqueous NaCl, dried over MgSO4, filtered and concentrated to provide intermediate (12b) as a foam (0.8 g, 2 mmol).

1. custompartitioned between EtOAc and 10% aqueous citric acid
2. customThe organic layer was separated
3. washwashed with saturated aqueous NaCl
4. dry with materialdried over MgSO4
5. filtrationfiltered
6. concentrationconcentrated