Reaktion #4560

ord-0e96676273d2437282408c24a90f4b9f

Lösungsmittel

Reaktionsbedingungen

Detaillierte Bedingungen
See reaction.notes.procedure_details.

Aufarbeitung

  1. 1
    Temperaturwas warmed
  2. 2
    Temperaturat reflux for 3 hours
  3. 3
    TemperaturThe resulting mixture was warmed
  4. 4
    Temperaturat reflux for 2.5 hours
  5. 5
    SonstigeThe organic layer was separated
  6. 6
    Trocknendried over MgSO4
  7. 7
    Sonstigeevaporated to dryness
  8. 8
    SonstigeThe residue was purified by prep LC
  9. 9
    Wascheneluting with 4:1 hexane
  10. 10
    Extraktionextracted with two portions of 1% aqueous NaOH
  11. 11
    Extraktionextracted with ether
  12. 12
    SonstigeThe ether layer was evaporated to dryness
  13. 13
    Sonstigethe residue again purified by prep LC
  14. 14
    Wascheneluting with 85:15 hexane
  15. 15
    SonstigeThis gave a yellow oil which
  16. 16
    Sonstigewas thoroughly dried

Vorschrift

A mixture of 1.7 g (17 mmol) of 2,4-pentanedione, 30 ml of benzene and 0.26 g (11.3 mmol) of sodium was warmed at reflux for 3 hours. The reaction mixture was cooled to room temperature and a solution of 10 mmol of 2-(4-(4-bromo-2-fluorophenoxy)phenoxy)propanoyl chloride was added dropwise. The resulting mixture was warmed at reflux for 2.5 hours, stirred at room temperature overnight and poured into water and ether. The organic layer was separated, dried over MgSO4 and evaporated to dryness. The residue was purified by prep LC, eluting with 4:1 hexane:acetone. The product was taken up in ether and extracted with two portions of 1% aqueous NaOH. The combined aqueous layers were made acidic with aqueous HCl and extracted with ether. The ether layer was evaporated to dryness and the residue again purified by prep LC, eluting with 85:15 hexane:acetone. This gave a yellow oil which was thoroughly dried to leave 0.70 g product. Calc for C20H18BrFO5 : C, 54.93, H, 4.15. Found: C, 54.13, H, 4.30.

Quelle

DOI: 10.6084/m9.figshare.5104873.v1Patent: US04725683uspto-grants-1988_02