反应详情

Dimethylamine hydrochloride (43 mg), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (121 mg), 1-hydroxybenzotriazole monohydrate (97 mg) and triethylamine were added to a mixed solution of 4-{(E)-1-(5-chloro-6-methoxypyridin-2-yl)-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}benzoic acid (131 mg) in chloroform and N,N-dimethylformamide (4 mL, 3:1), and the mixture was stirred at room temperature for three hours. The reaction solution was concentrated and the resulting residue was purified by silica gel chromatography (chloroform:methanol=100:0→80:20) to give 4-{(E)-1-(5-chloro-6-methoxypyridin-2-yl)-2-[(2R)-5-oxopyrrolidin-2-yl]ethenyl}-N,N-dimethylbenzamide as a brown oil (139 mg, 99%).

1. concentrationThe reaction solution was concentrated
2. customthe resulting residue was purified by silica gel chromatography (chloroform:methanol=100:0→80:20)