反应详情

To a solution of INT 7 (700 mg, 2.43 mmol) and azetidine-3-carboxylic acid (248 mg, 2.92 mmol) in MeOH (24 mL) was added HOAc (0.14 mL, 2.43 mmol) followed by PS—CNBH3 (2.5 mmol/g, 1.95 g, 4.86 mmol). The reaction mixture was stirred at room temperature for 3 days. The mixture was filtered over Celite. The filtrate was concentrated. The residue was purified by preparative HPLC (H2O/CH3CN) to give the title compound Example 3.

1. filtrationThe mixture was filtered over Celite
2. concentrationThe filtrate was concentrated
3. customThe residue was purified by preparative HPLC (H2O/CH3CN)