2-Methoxyethanol → 4-{(S)-3-[2-Chloro-4-(2-methoxy-ethoxy)-benzenesulfonyl]-pyrrolidin-1-yl}-2-methylsulfanyl-6-trifluoromethyl-pyrimidine

Participants

Reaction Conditions

Reaction Steps

4-[(S)-3-(2-Chloro-4-fluoro-benzenesulfonyl)-pyrrolidin-1-yl]-2-methylsulfanyl-6-trifluoromethyl-pyrimidine (Intermediate of example 42; 300 mg) was dissolved in DMF (5.0 mL). Cs2CO3 (429 mg) and 2-methoxy-ethanol (0.10 mL) were added. The reaction mixture was stirred for 24 h at 25° C. After that, the reaction mixture was diluted with ethyl acetate (20 mL) and extracted with water (10 mL). The organic layers were dried over Na2SO4, filtrated and evaporated to dryness. The crude material was purified by flash chromatography (50 g silica gel; ethyl acetate/n-heptane) to yield a colorless waxy solid (170 mg; 50%) MS: m/z=512.2 [M+H]+.

Provenance & Evidence