4-Chloro-2-(methylsulfanyl)-6-(trifluoromethyl)pyrimidine → 2-Methylsulfanyl-4-trifluoromethyl-6-[(S)-3-(2-trifluoromethyl-benzenesulfonyl)-pyrrolidin-1-yl]-pyrimidine

Participants

Reaction Steps

(S)-3-(2-Trifluoromethyl-benzenesulfonyl)-pyrrolidine (500 mg) was dissolved in acetonitrile (3.5 mL) in a microwave tube. 4-Chloro-2-(methylsulfanyl)-6-(trifluoromethyl)pyrimidine (450 mg), TEA (0.75 mL) and KF (10 mg) were added. The reaction mixture was irradiated in the microwave oven at 150° C. for 1.5 h. The reaction mixture was evaporated to dryness and purified by flash chromatography (50 g silica gel, ethyl acetate/n-heptane:0:1→1:0) to yield a light yellow oil (790 mg; 94%) MS: m/z=472.2 [M+H]+.

Provenance & Evidence