N-[5-(Diphenylphosphinoylmethyl)-4-(4-fluorophenyl)-6-isopropylpyrimidin-2-yl]-N-methylmethanesulfonamide

799842-07-2

719-80-2

289042-10-0

Under argon protection, ethyldiphenylphosphite (12.6 g, 55 mmol) was added to a solution of 5-(bromomethyl)-4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidine (15.2 g, 36.6 mmol) in toluene (370 mL), and the reaction mixture was stirred for 3 hours at 60 °C. Upon completion of the reaction, the mixture was concentrated. The residue was dissolved in toluene (10 mL), hexane (10 mL) was added and the product N-[5-(diphenylphosphinoylmethyl)-4-(4-fluorophenyl)-6-isopropylpyrimidin-2-yl]-N-methylmethanesulfonamide precipitated as a colorless powder, which was collected by filtration to give 14.3 g (73% yield). The product was structurally confirmed by nuclear magnetic resonance hydrogen (1H NMR, 300 MHz, CDCl3), carbon (13C NMR, 75 MHz, CDCl3) and phosphorus (31P NMR, 121 MHz, CDCl3) spectra.