反应详情

温度

100 °C

(S)-3-(2-fluoro-4-(5-methyl-1,3,4-oxadiazol-2-yl)phenoxy)-1-(piperidin-4-yl)pyrrolidin-2-one 2,2,2-trifluoroacetate (150 mg, 0.316 mmol) was dissolved in DMSO (3 mL) and 2,5-dichloropyrazine (70.7 mg, 0.474 mmol) and N-ethyl-N-isopropylpropan-2-amine (138 μL, 0.790 mmol) were added and the reaction heated to 100° C. overnight. The reaction was cooled and diluted with water, extracted with EtOAc, washed with brine, dried over Na2SO4, filtered and concentrated. The residue was purified twice over silica gel (100% EtOAc) to afford (S)-1-(1-(5-chloropyrazin-2-yl)piperidin-4-yl)-3-(2-fluoro-4-(5-methyl-1,3,4-oxadiazol-2-yl)phenoxy)pyrrolidin-2-one (15.2 mg, 0.0321 mmol, 10.2% yield) as a red solid. Mass spectrum (apci) m/z=473.1 (M+H).

1. temperatureThe reaction was cooled
2. extractionextracted with EtOAc
3. washwashed with brine
4. dry with materialdried over Na2SO4
5. filtrationfiltered
6. concentrationconcentrated
7. customThe residue was purified twice over silica gel (100% EtOAc)