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With caesium carbonate In N,N-dimethyl-formamide at 20℃; Inert atmosphere;
39.1 Step 1: 1-Benzyl-2-oxo-1,2-dihydropyridin-4-ylboronic acid
General procedure: To a solution of 30 mg (0.14 mmol) of 4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-1H-pyridin-2-one and 66 mg (0.20 mmol) of cesium carbonate in 1 ml of anhydrous DMF, are added 18 μl (0.15 mmol) of benzyl bromide at ambient temperature. The reaction is stirred overnight under argon. Reaction mixture is then diluted with ethyl acetate, and the precipitate is filtered and rinsed with a small amount of ethyl acetate. The filtrate is concentrated under vacuum and directly purified by flash chromatography with a 30 g C18 column and a water/acetonitrile mixture as eluent. 20 mg of the title compound are obtained. Yield: 65%. The compound is obtained by the procedure described in example 25 step 1, using 50 mg (0.23 mmol) of4-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-1H-pyridin-2-one, 184 mg (0.57 mmol) of cesium carbonate and 65 mg(0.25 mmol) of 3-(bromomethyl)pyridine hydrobromide instead of benzyl bromide. 11 mg of the title compound areobtained. Yield: 21%. MH+: 231.1.
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