反应详情

温度

25 °C

To a solution of [(4-chlorophenyl)-(3-methoxy-benzenesulfonyl)-amino]-acetic acid (250 mg, 0.7 mmol) in dry dichloromethane (20 mL) were sequentially added EDCI (202 mg, 1.05 mmol), HOBT (142.4 mg, 1.05 mmol), and DIPEA (0.23 mL, 1.40 mmol). The reaction mixture was allowed to stir for 30 minutes under nitrogen at 25° C. 2-Phenyl-pyrrolidine (104 mg, 0.7 mmol) was added and the mixture was stirred at 25° C. for 12 h. The reaction mixture was diluted with dichloromethane (20 mL), washed with saturated aqueous ammonium chloride solution, saturated aqueous sodium bicarbonate solution and water. The organic layer was dried (Na2SO4) and evaporated under reduced pressure. The residue was purified by column chromatography over silica gel (30-40% ethyl acetate/hexane) to yield the title compound.

1. stirringthe mixture was stirred at 25° C. for 12 h
2. washwashed with saturated aqueous ammonium chloride solution, saturated aqueous sodium bicarbonate solution and water
3. dry with materialThe organic layer was dried (Na2SO4)
4. customevaporated under reduced pressure
5. customThe residue was purified by column chromatography over silica gel (30-40% ethyl acetate/hexane)