反应详情

To a mixture of 4-pyrrolidin-1-ylbenzoic acid (2.0 g, 10.5 mmol), (4-aminomethylphenyl)methanol (4.3 g, 31.4 mmol), 1-hydroxybenzotriazole (1.7 g, 12.6 mmol), and DMAP (256 mg, 2.1 mmol) in pyridine (50 mL) was added EDC (3.0 g, 15.7 mmol), and the mixture was stirred at room temperature overnight. The reaction mixture was concentrated under reduced pressure, and an aqueous NaHCO3 solution (50 mL) was added. The mixture was extracted with 5% MeOH in CHCl3 (150 mL×2), and the organic layer was dried (MgSO4) and evaporated under reduced pressure. The crude product was purified by MPLC on silica gel (3% MeOH in CHCl3) to afford the titled compound (2.56 g, 79%) as a white solid.

1. concentrationThe reaction mixture was concentrated under reduced pressure
2. additionan aqueous NaHCO3 solution (50 mL) was added
3. extractionThe mixture was extracted with 5% MeOH in CHCl3 (150 mL×2)
4. dry with materialthe organic layer was dried (MgSO4)
5. customevaporated under reduced pressure
6. customThe crude product was purified by MPLC on silica gel (3% MeOH in CHCl3)