Water → 4-[(Difluoromethyl)thio]-6-methoxy-2-pyrimidinamine

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Reaction Steps

Gaseous difluorochloromethane is introduced for 11/2 hours at 60° to 65° C. into a suspension of 7.8 g of 2-amino-4-mercapto-6-methoxy-pyrimidine and 30 ml of concentrated sodium hydroxide solution in 100 ml of dioxane. By the addition of water, extraction with ethyl acetate, concentration of the organic phase by evaporation and crystallisation from methanol at -78° C., there are obtained 6.4 g of 2-amino-4-difluoromethylthio-6-methoxy-pyrimidine, m.p. 83° to 84° C. (compound No. 1.13).

Provenance & Evidence