反应详情

温度

5 °C

To a 5° C. stirring suspension of MeNH2.HCl (70 mg, 1.04 mmol) in benzene (1 ml) was added Me3Al (2M in toluene, 0.52 ml, 1.04 mmol) dropwise. The reaction mixture was stirred at RT for 1 h and a solution of 3-(1H-indol-6-yl)-3-(3-methoxy-phenyl)-propionic acid methyl ester XXXI (160 mg, 0.52 mmol) in benzene (5 ml) was added. The mixture was stirred at 90° C. for 4 h, cooled to RT, and diluted with HCl (5% in water, 6 ml). The resulting mixture was extracted 3 times with EtOAc. The organic layers were combined, washed with H2O (20 ml) and brine (10 ml), dried over MgSO4, filtered, and concentrated to provide 3-(1H-indol-6-yl)-3-(3-methoxy-phenyl)-N-methyl-propionamide XXXII (160 mg, quantitative yield) as a yellow film.

1. stirringThe reaction mixture was stirred at RT for 1 h
2. stirringThe mixture was stirred at 90° C. for 4 h
3. temperaturecooled to RT
4. extractionThe resulting mixture was extracted 3 times with EtOAc
5. washwashed with H2O (20 ml) and brine (10 ml)
6. dry with materialdried over MgSO4
7. filtrationfiltered
8. concentrationconcentrated