1-Hydroxybenzotriazole → (E)-3-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl]-N-(2-oxopiperidin-1-yl)acrylamide

関与物質

反応手順

IPEA (0.26 ml), HOBT (121 mg) and EDC (172 mg) were sequentially added to a suspension of 1-aminopiperidin-2-one hydrochloride (92 mg) and (E)-3-[3-methoxy-4-(4-methyl-1H-imidazol-1-yl)phenyl]acrylic acid (CAS No. 870839-41-1, 150 mg) in DMF (4 ml), and the reaction solution was stirred at room temperature overnight. Ethyl acetate and water were added to the reaction solution, and the organic layer was separated. The organic layer was sequentially washed with a saturated sodium bicarbonate solution and brine. The combined aqueous layers were reextracted with ethyl acetate (twice). The combined organic layers were dried over anhydrous magnesium sulfate and concentrated under reduced pressure. The resulting residue was triturated with ethyl acetate to obtain 97 mg of the title compound. The property values of the compound are as follows.

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