Cesium carbonate → ethyl 5-[4-(6-isopropyloxy-2,4-dimethylpyridin-3-yl)-2-nitrophenyl]-1-[(S)-tetrahydrofuran-3-yl]-1H-pyrazole-4-carboxylate

Participants

Reaction Conditions

Reaction Steps

Ethyl 5-[2-nitro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]-1-[(S)-tetrahydrofuran-3-yl]-1H-pyrazole-4-carboxylate obtained in Preparation Example 7-(2) (70 mg) was dissolved in a mixed solution of 1,4-dioxane (1 mL) and water (0.2 mL), and 3-bromo-6-isopropyloxy-2,4-dimethylpyridine (41.1 mg), Pd(PPh3)4 (17.7 mg) and cesium carbonate (150 mg) were added. The reaction mixture was stirred at 110° C. overnight. After returning the reaction mixture to room temperature, the reaction mixture was purified by silica gel column chromatography (ethyl acetate/n-heptane, 10 to 50% to 100%) to give the title compound (66.5 mg).

Provenance & Evidence