1-Hydroxybenzotriazole → 4-{3-[(4'-{[1-Methoxy-3-(methylamino)-1,3-dioxopropan-2-yl](methyl)carbamoyl}biphenyl-4-yl)oxy]propyl}morpholine

Beteiligte Stoffe

Reaktionsschritte

Intermediate 5-2 (0.24 g), WSC.HCl (0.29 g), HOBt.H2O (0.20 g), and DIPEA (0.27 mL) were added to a DMF (5.0 mL) solution of 4′-[3-(morpholin-4-yl)propoxy]biphenyl-4-carboxylic acid (0.34 g) as obtained in Example 4-(3), and the mixture was stirred for 2 hours at room temperature. Then, an aqueous solution of sodium hydrogen carbonate was added to the reaction mixture, and the mixture was extracted with ethyl acetate. The organic layer was washed with brine, and dried over anhydrous magnesium sulfate. Then, the desiccant was filtered out, and the solvent was distilled off under reduced pressure. The resulting residue was purified by NH type silica gel chromatography (gradient elution with hexane/ethyl acetate=50/50→0/100) to obtain 4-{3-[(4′-{[1-methoxy-3-(methylamino)-1,3-dioxopropan-2-yl](methyl)carbamoyl}biphenyl-4-yl)oxy]propyl}morpholine (colorless oil) (0.11 g, 23%).

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