反応 #11247

ord-5d80c8c706d54d52b27d08212a2f23ba

反応条件

温度
60°CELSIUS
詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    温度The reaction mixture was cooled to room temperature
  2. 2
    その他the tetrahydrofuran was removed
  3. 3
    workup.ADDITIONWater (50 mL) was added
  4. 4
    抽出the mixture was extracted with ethyl acetate (3×100 mL)
  5. 5
    洗浄The combined ethyl acetate extracts were washed with brine (50 mL)
  6. 6
    乾燥dried over magnesium sulphate
  7. 7
    ろ過filtered
  8. 8
    濃縮concentrated to dryness
  9. 9
    その他Trituration with diethyl ether (20 mL) gave solid material which
  10. 10
    洗浄was further washed with diethyl ether (20 ml)
  11. 11
    濃縮The liquors were concentrated
  12. 12
    その他triturated with diethyl ether (10 mL)
  13. 13
    その他the solid being collected

実験手順

To a solution of diethyl 2-chlorobenzylphosphonate (4.91 g, 0.018 mol) and 7-bromo-5-methoxybenzofuran-2-carbaldehyde (11.27 g, 0.016 mol) in tetrahydrofuran (80 mL) was added sodium hydride (60% dispersion in mineral oil, 0.74 g, 0.0185 mol). After 5 min. the reaction mixture was warmed to 60° C. for 1 h. The reaction mixture was cooled to room temperature, water (10 mL) was carefully added and the tetrahydrofuran was removed. Water (50 mL) was added and the mixture was extracted with ethyl acetate (3×100 mL). The combined ethyl acetate extracts were washed with brine (50 mL), dried over magnesium sulphate, filtered and concentrated to dryness. Trituration with diethyl ether (20 mL) gave solid material which was further washed with diethyl ether (20 ml). The liquors were concentrated and triturated with diethyl ether (10 mL), the solid being collected. The combined solids gave (859) (4.89 g, 84%). 1H NMR δ (CDCl3) 7.70 (d, J=16 Hz, 1H), 7.65 (dd, J=7.7, 1.5 Hz, 1H), 7.4 (dd, J=6.0, 1 Hz, 1H), 7.23 (m, 2H), 7.05 (d, J=2.3 Hz, 1H), 6.94 (d, J=16 Hz, 1H), 6.92 (d, J=2.3 Hz, 1H), 6.72 (s, 1H), 3.82 (s, 3H); MH+:364.9, 362.9 MH−:362.9, 360.9.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US07094798B1uspto-grants-2006_08