Sodium Cyanide → 3-(4-cyano-5-ethylsulfonylamino-2-fluorophenyl)-1-methyl-6-trifluoromethyl-2,4(1H,3H)-pyrimidinedione

Participants

Reaction Steps

0.5 g (1.0 mmol) of 3-(4-bromo-5-ethylsulfonylamino-2-fluorophenyl)-1-methyl-6-trifluoromethyl-2,4(1H,3H)pyrimidinedione was dissolved in 10 ml of 5-ethyl-2-picoline, to which 0.04 g of sodium hydride was added under cooling with ice, and the mixture was stirred for 5 minutes. Next, 0.04 g of palladium acetate and 0.16 g of 1,4-bis(diphenylphosphino)ethane were added to the mixture, which was then stirred at 90° C. under an argon atmosphere for 1 hour. After the mixture was allowed to cool, 0.03 g of zinc chloride and 0.06 g of sodium cyanide were added to the mixture, which was then stirred for further 4 hours. After the reaction was completed, 61% of the title compound was detected as the relative area value in liquid chromatography.

Provenance & Evidence