1,3-diMethyl-5-(4,4,5,5-tetraMethyl-1,3,2-dioxaborolan-2-yl)pyridin-2(1H)-one

51417-13-1

73183-34-3

1425045-01-7

The general procedure for the synthesis of 1,3-dimethylpyridin-2(1H)-one-5-pinacol borate from 5-bromo-1,3-dimethylpyridin-2(1H)-one and pinacol bis(boronic acid) ester was carried out as follows: firstly, nitrogen was vented into dioxane for degassing. Subsequently, the degassed dioxane solution (2.0 mL) was added to a mixture containing 5-bromo-1,3-dimethylpyridin-2(1H)-one (75 mg, 0.37 mmol), bis(pinacolato)diboron (113 mg, 0.445 mmol) and KOAc (109 mg, 1.11 mmol). Next, the catalyst PdCl2(dppf)-CH2Cl2 (30 mg, 0.037 mmol) was added. The reaction mixture was heated and reacted at 85 °C for 16 hours. After completion of the reaction, the reaction mixture was diluted with EtOAc and filtered through a Celite pad. Finally, the filtrate was concentrated under vacuum to afford the crude product 1,3-dimethylpyridin-2(1H)-one-5-pinacol borate (169 mg, 0.678 mmol, quantitative yield) as a brown oil.