反应详情

A mixture of 2-(4-fluorophenyl)-6-[(2-fluorophenyl)sulfonyl]naphthalene (110 mg, 0.29 mmol), imidazole (30 mg, 0.44 mmol), potassium carbonate (100 mg, 0.72 mmol) and dimethyl sulfoxide (1.5 mL) was reacted in a microwave at 150° C. for 20 minutes. The mixture was poured into water (100 mL) and extracted with ethyl acetate (2×50 mL). These extracts were washed with water and saturated brine then dried (MgSO4), filtered and solvent removed in vacuo. Purification by flash column chromatography eluting with 40% ethyl acetate/isohexane then 80% ethyl acetate/isohexane gave 1-(2-{[6-(4-fluorophenyl)-2-naphthyl]sulfonyl}phenyl)-1H-imidazole (104 mg, 84%). 1H NMR (500 MHz, CDCl3) δ 8.55 (1H, dd, J=1.7, 7.8 Hz), 7.96 (1H, s), 7.91 (1H, d, J=8.6 Hz), 7.89 (1H, s), 7.83 (1H, d, J=8.7 Hz), 7.80 (1H, dd, J=1.7, 8.5 Hz), 7.75-7.65 (4H, m), 7.42 (1H, dd, J=1.8, 8.6 Hz), 7.29 (1H, s), 7.23-7.17 (3H, m), 6.97 (1H, s), 6.75 (1H, s); m/z (ES+) 429 [MH+].

1. customwas reacted in a microwave at 150° C. for 20 minutes
2. extractionextracted with ethyl acetate (2×50 mL)
3. washThese extracts were washed with water and saturated brine
4. dry with materialthen dried (MgSO4)
5. filtrationfiltered
6. customsolvent removed in vacuo
7. customPurification by flash column chromatography
8. washeluting with 40% ethyl acetate/isohexane