110100-00-0

122372-20-7

110100-00-0

The general procedure for the synthesis of 1-(2-chloropyrimidin-5-yl)ethanone from the compound (CAS: 122372-20-7) is as follows: 1M hydrochloric acid (122 mL, 1.5 eq.) was slowly added to a solution of tetrahydrofuran (200 mL) containing Example 72-1 (15 g, 81.25 mmol, 1.0 eq.). The reaction mixture was stirred at 20 °C for 2 hours. Upon completion of the reaction, the solvent was removed by concentration under reduced pressure and the residue was partitioned between saturated aqueous sodium bicarbonate solution (150 mL) and ethyl acetate (100 mL). The organic layer was separated and washed with brine (50 mL x 3) and subsequently dried over anhydrous sodium sulfate. After filtration, the organic phase was concentrated under reduced pressure to give the crude product. The crude product was purified by column chromatography (silica gel as stationary phase and petroleum ether/ethyl acetate = 10/1 to 5/1 as eluent) to give 1-(2-chloropyrimidin-5-yl)ethanone (10 g, 79% yield) as a light yellow solid. The product was characterized by 1H NMR (400 MHz, CDCl3): δ 9.10 (s, 2H), 2.64 (s, 3H).