Diisopropylethylamine → 1-(2-Hydroxy-2-methyl-propyl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxylic acid [4-(6-oxo-5,6-dihydro-benzo[c][1,8]naphthyridin-1-yloxy)-phenyl]-amide

関与物質

反応手順

Compound 137 (50 mg, 0.16 mmol), 1-(2-hydroxy-2-methyl-propyl)-5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxylic acid (57 mg, 0.26 mmol), BOP-Cl (63 mg, 0.25 mmol), and DIEA (0.08 mL, 0.49 mmol) were suspended in dioxane (2 mL), and stirred overnight at room temperature. The reaction mixture was diluted with EtOAc/H2O, and filtered through an Extrelut column. The column was washed with EtOAc and the filtrate was concentrated. The crude material was purified via Biotage eluting with a gradient of 0 to 10% MeOH in CH2Cl2 to provide 209 (28 mg, 30% yield) as a white solid. LC-MS (M+H=576, obsd.=576).

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