반응 #11247

ord-5d80c8c706d54d52b27d08212a2f23ba

반응 조건

온도
60°CELSIUS
상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    온도The reaction mixture was cooled to room temperature
  2. 2
    기타the tetrahydrofuran was removed
  3. 3
    workup.ADDITIONWater (50 mL) was added
  4. 4
    추출the mixture was extracted with ethyl acetate (3×100 mL)
  5. 5
    세척The combined ethyl acetate extracts were washed with brine (50 mL)
  6. 6
    건조dried over magnesium sulphate
  7. 7
    여과filtered
  8. 8
    농축concentrated to dryness
  9. 9
    기타Trituration with diethyl ether (20 mL) gave solid material which
  10. 10
    세척was further washed with diethyl ether (20 ml)
  11. 11
    농축The liquors were concentrated
  12. 12
    기타triturated with diethyl ether (10 mL)
  13. 13
    기타the solid being collected

실험 절차

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.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US07094798B1uspto-grants-2006_08