2-[(6-Chloro-3,4-dihydro-3-Methyl-2,4-dioxo-1(2h)-pyriMidinyl)Methyl]benzonitrile

4318-56-3

22115-41-9

865758-96-9

Under stirring conditions, 20.8 g of dichloromethane, 3.21 g of 6-chloro-3-methyluracil, 4.51 g of 2-cyanobenzyl bromide and 5.16 g of DIPEA were sequentially added to the reaction flask.The reaction system was warmed up to refluxing temperature (40-45 °C) and the progress of the reaction was monitored by HPLC until the complete disappearance of 3-methyl-6-chlorouracil. Upon completion of the reaction, the reaction system was cooled to 20-25 °C and the dichloromethane was removed by distillation under reduced pressure. Water was added to the residue, stirred for 1 hour and filtered. The filter cake was washed with water, followed by ethanol and stirred at 20-25 °C for 1 hour. After filtration again, the filter cake was washed with ethanol and dried under reduced pressure at 60-70 °C to afford 5.28 g of white crystalline solid, i.e., the target product 2-((6-chloro-3-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)benzonitrile (hereinafter referred to as the intermediate), in 95.8% yield.