925422-06-6

799842-07-2

General procedure for the synthesis of 5-(bromomethyl)-4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidines from compound (CAS:925422-06-6): 1. N-[5-hydroxymethyl-4-(4-fluorophenyl)-6-isopropylpyrimidin-2-yl]-N-methylmethanesulfonamide (50.0 g) and 48% aqueous hydrogen bromide solution (130.0 mL) were added to the reactor. 2. The reaction mixture was stirred at 80 °C for 15 h. The progress of the reaction was monitored by thin-layer chromatography (unfolding agent: ethyl acetate/hexane=1:2). 3. Upon completion of the reaction, the mixture was cooled to 20 °C and stirring was continued for 1 h at this temperature. 4. The product was collected by filtration under reduced pressure and the resulting white solid was washed with deionized water (500.0 mL). 5. The washed solid was dried under reduced pressure to afford N-[5-bromomethyl-4-(4-fluorophenyl)-6-isopropylpyrimidin-2-yl]-N-methylmethanesulfonamide as a white solid (55.3 g, 94% yield). 6. The structure of the product was confirmed by 1H-NMR (400 MHz, CDCl3) with the following chemical shifts (ppm): 1.35 (d, 6H), 3.48 (m, 1H), 3.49 (s, 3H), 3.56 (s, 3H), 4.48 (q, 2H), 7.23 (t, 2H), 7.81 (q, 2H).