反应详情

To a mixture of (S)-6-methoxy-4-methyl-N-(pyrrolidin-3-yl)quinolin-2-amine (0.50 g), 1-(4-chlorophenyl)-1-cyclobutane carboxylic acid (0.41 g), and DMF (6 mL) were added HOBt (0.39 g) and EDC.HCl (0.56 g), and the mixture was stirred at room temperature for 12 h. The reaction mixture was diluted with ethyl acetate and water, followed by addition of a saturated sodium hydrogencarbonate solution to extract the mixture. The organic layer was dried with anhydrous magnesium sulfate, then the desiccant was removed by filtration, the filtrate was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (silica gel, chloroform/methanol, and NH silica gel, ethyl acetate) to obtain colorless amorphous (S)-(1-(4-chlorophenyl)cyclobutyl)-(3-(6-methoxy-4-methylquinolin-2-ylamino)pyrrolidin-1-yl)methanone (0.67 g).

1. extractionto extract the mixture
2. dry with materialThe organic layer was dried with anhydrous magnesium sulfate
3. customthe desiccant was removed by filtration
4. concentrationthe filtrate was concentrated under reduced pressure
5. customthe residue was purified by silica gel column chromatography (silica gel, chloroform/methanol, and NH silica gel, ethyl acetate)